Pharmacognosy 2
Pharmacognosy 2
Pharmacognosy 2
COLUMN CHROMATOGRAPHY
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
Mobile Phase
– They act as solvent, developer & eluent. The function of a mobile phase
are:
– As developing agent
– To introduce the mixture into the column – as solvent
– To developing agent
– To remove pure components out of the column – as eluent
– The choice of the solvent is depend on the solubility characteristics of the
mixture. The solvents should also have sufficiently low boiling points to
permit ready recovery of eluted material.
– However, polarity as seen the most important factor in adsorption
chromatography.
– Different mobile phases used: ( in increasing order of polarity)
– Petroleum ether, carbon tetrachloride, cyclohexane, ether, acetone,
benzene, toluene, esters, water, etc
– It can b e used in either pure form or as mixture of solvents
COLUMN CHARACTERISTICS:
– The main function of all the columns is to support the stationary phase.
– The material of the column is mostly good quality neutral glass since it
shouldn’t be affected by solvents. An ordinary burette can also be used as
column for separation.
– Column dimensions - length & diameter ratio (10:1,30:1 or 100:1)
– Various accessories are attached to the top and bottom of the column for
maintenance of the elution process.
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
– The entire sample is introduced into the column at once and get adsorbed
on the top portion of the column.
– From this zone, individual sample can be separated by a process of
elution.
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
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1.SEPARATION AND ISOLATION OF PLANT CONSTITUENTS (BSM)
Carbohydrates
The Germans first and foremost introduced the word ‘kohlenhydrates’ which
was later on coined to carbohydrates. The name obviously suggests that these
compounds are essentially the hydrates of carbon
• Carbohydrates, were defined as a group of compounds composed of
carbon, hydrogen and oxygen in which the latter two elements are in
the same proportion as in water and were expressed by a formula
(CH2O)n, that is, hydrates of carbon.
• All organic compounds containing hydrogen and oxygen in the
proportion found in water are not carbohydrates.
• For example, formaldehyde HCHO for the present purpose can be written
as C(H2O); acetic acid CH3COOH written as C3(H2O)2; and lactic acid
CH3CHOHCOOH written as C3(H2O)3 are not carbohydrates.
• Also, a large number of carbohydrates such as rhamnose (C6H12O5),
cymarose (C7H14O4), digitoxose (C6H12O4), etc., are known which do
not contain the usual proportions of hydrogen to oxygen.
• From the discussion, it can be concluded that the definitions described is
not correct; however, carbohydrates are now defined chemically as
Polyhydroxy aldehyde or Polyhydroxy ketones or compound that on
hydrolyses produce either of the above.
• Carbohydrates are among the first products that are form as a result of
photosynthesis.
• They constitute a large proportion of the plant biomass and are
responsible, as cellulose, for the rigid cellular framework and, as starch,
for providing an important food reserve.
• Of special pharmacognostic importance is the fact that sugars unites with
a wide variety of other compounds to form glycosides and secondary
metabolites.
• Mucilage act as water-retaining vehicles, where as gums and mucilage,
which are similar in composition and properties, are formed in the plant
by injury or stress and usually appear as solidified exudates; both are
typically composed of uronic acid and sugar units.
• Low molecular weight carbohydrates are crystalline, soluble in water and
sweet in taste, for example, glucose, fructose, sucrose, etc.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
CLASSIFICATION
Monosaccharides
• The term ‘monosaccharides’ is employed for such sugars that on
hydrolysis yield no further, lower sugars.
• The monosaccharides are subdivided as bioses, trioses, tetroses, pentoses,
hexoses, heptoses, depending upon the number of carbon atoms they
possess.
Bioses
• They contain two carbon atoms. They do not occur free in nature.
Trioses
• They contain three carbon atoms ,for example, glyceraldehydes.
Tetroses
• They contain four carbon atoms, for example, erythrose, threose, etc.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Pentoses
• They are very common in plants and are the products of hydrolysis of
polysaccharides like hamicelluloses, mucilages and gums, for example,
ribose, arabinose and xylose.
Hexoses
• They are monosaccharides containing six carbon atoms and are
abundantly available carbohydrates of plant kingdom. They are further
divided into two types: aldoses and ketoses. They may be obtained by
hydrolysis of
• Aldoses : Glucose, galactose
• Ketoses : Fructose and sorbose
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2.CARBOHYDRATES NOTES BY BILAL MALIK
• Heptoses
They contain seven carbon atoms, vitally important in the photosynthesis
of plant and glucose metabolism of animals and are rarely found accumulated in
plants, for example, glucoheptose and manoheptose.
Disaccharides:
• Carbohydrates, which upon hydrolysis yield two molecules of
monosaccharides, are called as disaccharides.
• Sucrose Hydrolysis Glucose + fructose (sugarcane), Maltose Hydrolysis
Glucose + Glucose (malt sugar), Lactose Hydrolysis Glucose + Galactose
(cow’s milk).
Trisaccharides:
• These liberate three molecules of monosaccharides on hydrolysis.
• Raffinose Hydrolysis Glucose + fructose + galactose (in beet)
(sugarcane),
Gentianose Hydrolysis Glucose + Glucose + fructose (gentian roots).
Tetra-saccharides
• Stachyose, a tetrasaccharide, yields on hydrolysis, four molecules of
monosaccharide, found in manna.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Polysaccharides:
• On hydrolysis they give an indefinite number of monosaccharides.
• By condensation, with the elimination of water, polysaccharides are
produced from monosaccharides.
• Depending upon the type of product of hydrolysis these are further
classified as Pentosans and Hexosans.
• Xylan is pentosan, whereas starch, insulin and cellulose are the examples
of hexosans.
• Cellulose is composed of glucose units joined by β-1, 4 linkages, whereas
starch contains glucose units connected with α- 1, 4 and α- 1, 6 units.
• Polyuronides, gums and mucilages are the other pharmaceutically
important polysaccharide derivatives.
SUCROSE:
It is called table sugar.
It is formed by combination of 2 units of monosaccharide Fructose &
Glucose.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
SUGAR CANE:
Common names:
Sugar cane, noble cane (English), sarkara (Sanskrit), paunda (Hindi).
Botanical name:
Saccharum officinarum L.
Family:
Poaceae (grass family)
Part used:
Thick, joined fibrous stalks.
Habitat
Hot humid tropics, in moist soils.
Brazil is the largest producer of Sugar cane in world. It is also cultivated in
Pakistan, India, China, Thailand & Mexico.
DESCRIPTION:
Tropical, perennial grass, that form lateral shoots.
Sweet in taste , outer surface is greenish brown, while inner surface is
yellowish white.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
CULTIVATION:
It is cultivated in Tropic & Sub tropic areas with plentiful supply of water
& Sun light for continuous period of more then 6 month each year.
It grows on highly fertile soil.
It is harvested by hand or mechanically.
In hand harvesting, the field is first set on fire,
Fire burns dry leaves & kills the insects etc leaving stalks & roots harm
less & then they are Cut just above the ground level.
In mechanical harvesting, Sugar cane harvester is used.
PROCESSING:
Two stages
1. Milling, 2. Refining.
1. MILLING:
In this stage, the cane juice is extracted by different techniques.
2.REFINING
The juice is centrifuged to remove impurities.
After this the sugar solution is clarified by adding phosphoric acid and
Ca. hydroxide.
After filtering the syrup is decolorized by activated carbon.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Uses:
Used as table sugar.
Used as sweetening agent in syrups.
Used as demulcent.
Used as bacteriostatic and preservative.
Used to mask disagreeable tastes in troches and tablets.
Used to relive low B.P.
Used to treat diarrhea.
It is also used as taste enhancer and preservative in food industry.
SUGAR BEET:
Synonyms-
Spinach Beet. Sea Beet. Garden Beet. White Beet.
BOTANICAL NAME :
Beta vulgaris (Linn.)
FAMILY :
Chenopodiaceae.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
https://www.youtube.com/watch?v=ZVxPkv0r7JY
DESCRIPTION :
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Dextrose:
D-glucose
D(+)-glucopyranose
Naturally present in grapes and other fruits.
Preparation
Usually obtained by hydrolysis of starch.
Heating at 45 lb presure for 35 min.
Dextrose is then crystalized,washed and dried.
99-100% pure.
Uses:
NUTRIENT ( mouth, enema, injection)
Dextrose and NaCl inj
Present in anticoagulant citrate phosphate dextrose soln (storage of
blood).
Food industry
Liquid Glucose:
Obtained by incomplete hydrolysis of starch
Composed of Dextrose, also contains Dextrin, Maltose and Water.
Preparation
Corn starch is mixed with dil HCl at 30 lb pressure for 22 min
Centrifuged and filtered
Evaporated to syrupy liquid.
Description:
Thick colourless or yellowish liquid
Odourless and sweet in taste.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Uses:
Sweetning agent in pharma industry
Substitute of sucrose in syrup
Tablet binder and coating agent.
Fructose:
D-fructose,
Levulose ,
D(-) fructopyranose,
Fruit sugar.
Description:
Colourless crystals or white crystalline powder
Odourless and sweet in taste
Soluble in water
Uses:
Food for diabetic people
Diabetic acidosis
Infant feeding formulas
Ingredient in electrolyte replinsher, given parentrally.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
HONEY:
Synonyms
Madhu, Madh, Mel, Purified Honey.
Biological Source
Honey is a viscid and sweet secretion stored in the honey comb by various
species of bees, such as Apis mellifera, Apis dorsata, Apis florea, Apis indica
belonging to family Apideae.
Geographical Source
Honey is available in abundance in Africa, India, Jamaica, Australia,
California, Chili, Great Britain and New Zealand.
HONEY
Morphology:
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2.CARBOHYDRATES NOTES BY BILAL MALIK
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Uses:
Honey shows mild laxative, bactericidal, sedative, antiseptic and
alkaline characters.
It is used for cold, cough, fever, sore eye and throat, tongue and duodenal
ulcers, liver disorders, kidney and other urinary disorders, pulmonary
tuberculosis, marasmus, rickets, scurvy and insomnia.
It is applied as a remedy on open wounds after surgery.
It is also useful in healing of carbuncles other and skin inflammation.
Honey, mixed with onion juice, is a good remedy for arteriosclerosis in
brain.
Diet rich in honey is recommended for infants, convalescents, diabetic
patients and invalids.
Honey is an important ingredient of certain lotions, cosmetics, soaps and
creams.
Honey is used as an ingredient in various cough preparations.
It is also used to treat asthma.
Adulterant and Substitutes:
Due to the relatively high price of pure honey, it is invariably adulterated
ether with artificial invert sugar or simply with cane-sugar syrup.
These adulterants or cheaper substituents not only alter the optical
property of honey but also its natural aroma and fragrance.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
STARCH:
Synonyms
Amylum.
Biological Source
Starch consists of polysaccharide granules obtained from the grains of
Maize (Zea mays Linn.);
Rice (Oryza sativa Linn.)
Wheat (Triticum aestivum Linn.); belonging to family Gramineae .
Potato (Solanum tuberosum Linn.), family Solanaceae.
Geographical Source
Most of tropical, as well as, sub-tropical countries prepare starch
commercially.
Preparation of Starch
Potato Starch:
The potatoes are washed to remove the earthy matter.
They are crushed or cut and converted into slurry.
Slurry is filtered to remove the cellular matter.
After filtration, the milky slurry containing starch is purified by
centrifugation and washing.
Then, it is dried and sent to the market.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Rice Starch :
The broken pieces of rice resulted during the polishing are used for
processing.
The pieces of rice are soaked in water with dilute sodium hydroxide
solution (0.5%), which causes softening and dissolution of the gluten
(general name for wheat or rice protein).
The soaked rice pieces are crushed and starch prepared as preceeded in
potato.
Corn starch:
Maize grains are washed thoroughly with water to remove the adhered
organic matter.
They are softened by keeping in warm water for 2–3 days.
Sufficient sulphur dioxide is passed to the medium to prevent
fermentation.( Fermentation is a metabolic process that converts sugar
to acids, gases, or alcohol. Endosperm is a tissue produced inside the
seeds of most of the flowering plants following fertilization. It surrounds
the embryo and provides nutrition in the form of starch, though it can
also contain oils and protein)
The swollen kernels are passed through attrition mill to break the grains,
so as to separate the endosperm and outermost coating.
The starchy material contains gluten; most of this is removed by simple
sieving and then by washing several times with cold water.
Then centrifuged or filter-pressed and finally, dried in flash dryers on a
moving belt dryer to get starch.
Wheat Starch:
The wheat flour is converted into dough(Dough= Flour mixed with
water) and kept for a while.
The gluten in the dough swells and the masses are taken to grooved
rollers, wherein water is added with constant shaking.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Microscopic Characters:
Rice Starch:
The granules are simple or compound.
Simple granules are polyhedral while compound granules are ovoid.
Rice starch
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Wheat Starch:
Wheat starch
Maize Starch:
Granules are polyhedral or rounded, with distinct cavity in the centre or
two to five rays cleft.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Potato Starch:
Generally, found in the form of simple granules, which are sub-
spherical, somewhat flattened irregularly ovoid in shape.
Hilum is present near the narrower end with well-marked.
Chemical Constituents:
Chemically starch contains two different polysaccharides,
Amylose (β-amylose) and
Amylopectin (α-amylose).
Amylose is water soluble and amylopectin is water insoluble, but swells
in water and is responsible for the gelatinizing (Starch gelatinization is a
process of breaking down the intermolecular bonds of starch molecules
in the presence of water and heat ) property of the starch.
Amylose gives blue colour with iodine, while amylopectin yields bluish
black colouration.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Identification Tests:
1. 1 g of starch is boiled with 15 ml of water and cool. The translucent
viscous jelly is produced.
2. The jelly turns deep blue by the addition of solution of iodine.
Uses:
As a nutritive, demulcent, protective and as an absorbent.
In the preparation of dusting talcum powder for application over the
skin.
As antidote in iodine poisoning.
As a disintegrating agent in tablets
As diluent in dry extracts of crude drug and is a diagnostic aid in the
identification of crude drugs.
As a starting material for the commercial manufacture of liquid glucose,
dextrose and dextrin(Dextrins are a group of low-molecular-weight
carbohydrates produced by the hydrolysis of starch or glycogen).
Cellulose:
Cellulose (C6H10O5)n is a long-chain polysaccharide carbohydrate, of beta-
glucose.
It forms the primary structural component of plants and is not digestible
by humans
Structure of Cellulose
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2.CARBOHYDRATES NOTES BY BILAL MALIK
History:
Being found as the principal component of cell walls in higher plants
where it provides the main structural feature. Therefore,
Cellulose is considered as the most abundant naturally occurring organic
substance on earth.
It was first noted as such in 1838 by Anselm Payen.
It occurs in almost pure form in cotton fibre at 98% in combination with
lignin and hemicellulose.
Cellulose is the most abundant form of living terrestrial biomass.
Applications:
Cellulose is processed to make cellophane and rayon.
Cellophane has several applications in pharmaceutical packaging due to
its suitable characteristics such as good compatibility, durability,
transparency and elasticity.
Cellulose is also used within the laboratory as a solid-state substrate for
thin layer chromatography.
Cellulose is a major constituent of paper.
Derivatives:
The hydroxyl groups of cellulose can be partially or fully reacted with
various chemicals to provide derivatives with useful properties.
They have the general formula
Cellulose-O-R
Cellulose esters and cellulose ethers are the most important commercial
materials.
Among the esters are cellulose acetate and triacetate, which are used in
cosmetics.
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Uses of Cellulose:
Anticake agents
Emulsifier
Stabiliser
Dispersing agent
Thickener
Gelling agent
Microcrystalline cellulose (MCC) is the most known cellulose which
extensively used in pharmaceutical industries. MCC grades are
multifunctional pharmaceutical excipients which can be used as
compressibility enhancer,
binder in wet and dry granulation processes,
thickener and viscosity builder in liquid dosage forms
and free-flowing agents in solid dosage forms.
Application in bioadhesive and mucoadhesive drug delivery systems.
Bioadhesives are considered as novel drug delivery systems. These
dosage forms are formulated to use on the skin and mucus membranes
of gastrointestinal, ear, nose, eye, rectum and vagina.
The main excipients of these formulations are adhesive and film-former
polymer(s).
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2.CARBOHYDRATES NOTES BY BILAL MALIK
Ethyl cellulose
Aqueous dispersions of ethyl cellulose or its organic solutions can be
used for coating of extended release formulations. After ingestion of
these formulations, an insoluble viscose gel is forming around the tablet
which doesn’t allow to drug to freely release from dosage form.
Because of water insolubility of EC, it is often used in conjunction with
water soluble polymers such as MC
It is the lightest and most expensive of the cellulosics.
Methyl cellulose
It is used in the food, cosmetic, and pharmaceutical industries.
Is non toxic, non-allargic and is a weak adhesive.
Methylcellulose is used as
a tablet and capsule disintegrant,
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2.CARBOHYDRATES NOTES BY BILAL MALIK
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3.ALKALOIDS BY BILAL MALIK
Alkaloids:
1. Primary metabolites
2. Secondary metabolites
Alkaloids are very important group of chemical compounds; approximately
12,000 in number, having application in different areas of the economy,
industry, trade, and services.
A precise definition of the term 'alkaloid' (alkali-like) is somewhat
difficult because there is no clear-cut boundary between alkaloids and
naturally occurring complex amines.
Types of Alkaloids:
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3.ALKALOIDS BY BILAL MALIK
TRUE
PROTOALKALOIDS PSEUDOALKALOIDS
ALKALOIDS
False alkaloids are non alkaloids give false positive reaction with alkaloidal reagents.
New Definition:
Alkaloids are cyclic organic compounds containing nitrogen in a negative state
of oxidation with limited distribution among living organisms.
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3.ALKALOIDS BY BILAL MALIK
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3.ALKALOIDS BY BILAL MALIK
Nomenclature:
The name of all alkaloids should end with the suffix ‘-ine’.
The names of the alkaloids are obtained in various ways:
1. From the generic name of the plant yielding them, e.g. atropine.
2 From the specific name of the plant yielding them, e.g. cocaine.
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3.ALKALOIDS BY BILAL MALIK
3 From the common name of the drug yielding them, e.g. ergotamine.
4 From their physiologic activity, e.g. emetine. that acts as emetic.
5 From the discoverer, e.g. pelletierine.
6 A prominent physical character, such as Hygrine that is hygroscopic.
Physical Properties:
I- Condition:
Most alkaloids are crystalline solids.
Few alkaloids are amorphous solids e.g. emetine.
Some are oxygen-free and are liquids that are either:
Volatile e.g. nicotine and coniine, or
Non-volatile e.g. pilocarpine and hyoscine.
II- Color:
The majority of alkaloids are colorless but some are colored e.g.
Colchicine and berberine are yellow.
Canadine is orange.
III- Solubility:
Both alkaloidal bases and their salts are soluble in alcohol.
Generally, the bases are soluble in organic solvents and insoluble in
water
Exceptions:
Bases soluble in water: caffeine, ephedrine, codeine, colchicine,
pilocarpine and quaternary ammonium bases.
Bases insoluble or sparingly soluble in certain organic solvents:
morphine in ether, theobromine and theophylline in benzene.
Salts are usually soluble in water and, insoluble or sparingly soluble in
organic solvents.
Exceptions:
Salts insoluble in water: quinine monosulphate.
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3.ALKALOIDS BY BILAL MALIK
Physico-chemical properties:
Most alkaloids are well-defined crystalline substances which unite with
acids to form salts.
In the plant they may exist in the free state, as salts or as N-oxides.
In addition to the elements carbon, hydrogen and nitrogen, most alkaloids
contain oxygen.
Coniine and nicotine are oxygen-free and are liquids
Although colored alkaloids are rare, berberine, for example, is yellow
and the salts of sanguinarine are copper-red.
As a general rule, alkaloids as bases are not soluble or are sparingly
soluble in water, soluble in apolar or only slightly polar organic solvents.
Alkaloids test:
2 ml of each extract/fraction in 1% HCl solution and
added few drops of dragendorff reagent
which give orange colour precipitate indicates the presence of alkaloids.
Alkaloidal precipitating reagents
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3.ALKALOIDS BY BILAL MALIK
Detection of alkaloid:-
-Wagner's test: (I2/kI):Reddish brown precipitate .
-Mayer’s: (HgCl2 Creamy precipitate with True alkaloid.
-Hagger's test: (Picric acid) Yellow precipitate with True alkaloid.
-Dragendroff: (Potassium Bismuth Iodide) Reddish Brown precipitate .
Classification of Alkaloids:
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3.ALKALOIDS BY BILAL MALIK
Me
N
N N N
H H N
NH N NH
N NH N
H N N N
Isoquinoline Tetrahydro- Indole Imidazole Purine
isoquinoline
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3.ALKALOIDS BY BILAL MALIK
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3.ALKALOIDS BY BILAL MALIK
Biosynthetic origin:
Alkaloids are formed from amino acids some but other precursors like
terpenes or steroids, are often also built into the final alkaloidal skeleton.
The amino acids that most often serve as alkaloidal precursors include:
phenylalanine, tyrosine, tryptophan, histidine, anthranilic acid, lysine and
ornithine.
Extraction:
-The extraction is fractional extraction (From less Polar to more Polar).
-Defeating by non polar solvent (Petroleum Ether, benzene, alkane,….)
To get red of Chlorophyll, Wax, Volatile oil, Fixed oil.
-Filtration, For marc use methanol or ethanol 95%
Evaporate by rotary evaporator (to Concentrate)
-Add Tartaric acid 2% and Ethyl acetate will separate into two layer:
-Organic layer (For week or neutral alkaloid )
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3.ALKALOIDS BY BILAL MALIK
-Aqueous layer (acidic layer, Tartaric acid) which have alkaloidal salt. To
break the salt add NH3 or Sodium bicarbonate. then add ethyl acetate
again so will it separate into two layer again:
Aqueous layer (Quaternary alkaloids 4º )
Organic layer (For basic alkaloid 10,2º,3º)
EXTRACTION OF ALKALOIDS:
Any method which possessed following characteristics will be
considered as a good technique; if it will accelerate:
1. Wetting of the surface of the herb particles.
2. Permeability of cell walls.
3. Rate of dissolution of cell contents in the solvent.
4. Outward diffusion of the solution.
IDEAL PROPERTY OF SOLVENT:
1. It should be non-toxic and selective.
2. It should not cause the extract to complex or dissociate.
3. It should be preservative in action.
4. It should promote rapid physiologic absorption of the extract.
5. It should be easily evaporated at low heat.
NOTE:- Alcohol (Ethanol) will meet all above criteria.
SELECTION OF ALKALI:
1. use of strong alkali not recommended in case of fatty drug e.g. seeds
to avoid saponification, which results in strong emulsion during
extraction.
2. Salts of strong base with mineral acid need the use of stronger alkali.
3.Ammonia is a alkali of choice as it is sufficiently basic to liberate most
of alkaloid , as well as ,volatile and easily evaporate after extraction.
Solvents:
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3.ALKALOIDS BY BILAL MALIK
STAS-OTTO METHOD:
The technique involve the distribution of alkaloidal bases between acid or
aqueous solution and immiscible organic solvent.
Method I:
A). stage1:--Powdered material is moistened with water and mixed with
alkali like sodium & potassium carbonate , ammonia, lime. Make a paste
with water ,dry ,and then re-powder.
Lime(calcium hydroxide),combines with acid , tannins, and other
phenolic substances and sets free alkaloids.
B).Stage2:-- Extract the free alkaloids by hot continous percolation with
chloroform or any other organic solvents.
The free alkaloids dissolve together with other substances soluble in
solvent.
C).Stage3:--Agitate the chloroform soln. with successive portion of
dil.sulphuric acid separating the aqueous layer before adding the next
portion of acid.
D).Stage4:--Make the mixed aqueous liquid alkaline with ammonia,
collect the precipitate that forms, wash with water and dry.
Ammonia decomposes the alkaloidal sulphates forming ammonium
sulphates ,soluble in water ,and the free alkaloid which being practically
insoluble in water is precipitated.
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3.ALKALOIDS BY BILAL MALIK
Method II:
The powder is extracted with water soluble organic solvents such as
MeOH or EtOH which are good solvents for both salts and free bases.
And the resultant extract is submitted to same process as that of method1.
ADVANTAGE :-- This method requires no alkali, gives good
penetration of drug, therefore only 4 extraction may be needed , whereas
method1 requires 10-12 extraction, i.e. Economical.
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3.ALKALOIDS BY BILAL MALIK
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3.ALKALOIDS BY BILAL MALIK
Areca:
Synonyms: Areca nut or Betel Nut (Local: Paan Supari )
Botanical name: Areca catechu
Family : Palmae
Part used: Dried, ripe seeds.
Geo Location: Tropical Pacific, Asia, and parts of east Africa.
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3.ALKALOIDS BY BILAL MALIK
Description:
Areca- a Spanish and Portuguese term for betel nut
Catechu- East Indian name for an astringent extract or juice.
The seeds are cut into narrow pieces and rolled inside Betel leaf, rubbed
over with lime and chewed by the natives. They stain the lips and teeth
red and also the excrement, they are hot and acrid when chewed.
It is a medium-sized tree, growing straight to 20 m tall, with a trunk 10–
15 cm in diameter.
The leaves are 1.5–2 m long, pinnate, with numerous, crowded leaflets.
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3.ALKALOIDS BY BILAL MALIK
The areca nut is not a true nut, but rather a drupe. It is commercially
available in dried, cured and fresh forms.
While fresh, the husk is green and the nut inside is soft while in the ripe
fruit, the husk becomes yellow and nut becomes hard.
Areca mixed with lime, the leaves of Piper betle and occasionally
gambir is known as “PUNSUPARI”. This mixture is used as a stimulant
masticatory (chewing).
It Consists of 0.45% alkaloids, 15% tannins, lipids, volatile oils and gum.
Display of the items usually included in a chewing session: The betel
leaves are folded in different ways according to the country and most
have a little calcium hydroxide daubed inside. Slices of the dry areca nut
are on the upper left hand and slices of the tender areca nut on the upper
right. The pouch on the lower right contains tobacco, a relatively recent
introduction
Constituents:
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The medicinal components are primarily associated with the nut and
betel quid.
The nuts contain at least 9 structurally related pyridine alkaloids,
including arecoline, arecaidine, arecaine, arecolidine, guvacine,
isoguvacine, guvacoline, and coniin.
The most common is the parasympathetic stimulant alkaloid arecoline
(causes neurotoxicity through enhancement of oxidative stress and
suppression of the antioxidant protective system). It also responsible
for addiction.
The total alkaloid content can reach 0.45%.
TRADITIONAL USES:
In Ayurvedic medicine, betel nut is used as a diuretic, digestive,
anthelmintic, astringent, and cardiotonic.
The nuts are used in Traditional Chinese Medicine to treat diarrhoea, low
blood pressure, slow heart rate, and other intestinal troubles.
They use the root for liver disease and the fruit along with opium for the
treatment of intestinal troubles.
The betel nut can cause black stained teeth and gums to those who chew
it regularly, although it is excellent for maintaining a healthy digestive
tract, especially in disease-ridden areas.
However, it has been proposed that betel nut is a carcinogen. Though this
may be due to the common modern addition of tobacco products. Betel
nut can also cause bronchoconstriction, and so should be avoided by
asthmatics.
LOBELIA:
Synonyms: Indian tobacco, Puke-weed, Asthma-Weed
Bot: name: Lobelia inflata
Family : Lobeliaceae
Part used: The dried flowering herb, and seeds.
Geo Location: Dry places in the northern United States, Canada and in
English gardens.
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Description:
The herb is named after the botanist Matthias de Lobel, a native of Lille,
who died in London in 1616.
It is an erect annual or biennial herb, 1 to 2 feet high; flower are stalked
and pale violet-blue in colour.
Commercially, it is usually prepared in compressed, oblong packages,
the colour is a yellowish green, the odour irritating, the taste, after
chewing, very like that of tobacco, burning and acrid, causing a flow of
saliva.
Constituents:
Extracts of Lobelia contain 14 alkaloids which LOBELINE is the major
and most important. It has a pungent volatile oil, resin, lipids, and gum.
Lobeline or alpha lobeline
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This occurs as colorless crystals which are slightly soluble in water but
readily soluble in hot alcohol.
Pharmacological effects:
Similar but weaker pharmacological effects than nicotine on the
peripheral circulation, neuromuscular junctions, and CNS.
Lobeline improves acute lung injury in animal study.
It has antidepressant-like properties in mice.
Lobeline (10, 20 and 30 mg/kg, i.p.) significantly delayed and
antagonized the onset of Pentylenetetrazol -induced seizures.
Anti-smoking preparations
Lobeline sulfate incorporated in tablets or lozenges are smoking
deterrents.
Lobeline diminishes the behavioral and neurochemical effects of nicotine
and amphetamines, and is considered a potential pharmacotherapy for
drug abuse and addiction.
Lobeline had placebo effect on decreasing the physical craving for
cigarettes.
Traditional uses :
Traditionally used by the Native Americans for asthma
Chronic bronchitis
Injection of lobeline hydrochloride is used in the re-suscitation of
newborn infants.
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B) Tropane Alkaloids:
Introduction:
These are ester alkaloids resulted from the coupling of organic acids with
amino alcohol (Base).
The parent base is the “Tropane” base.
H
N
1
7 2
NH
6 5
4
3
1)Atropa belladonna:
The deadly nightshade
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Morphology:
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Active Compounds:
History of Uses:
Romans used plant as a “weapon”
Contaminated enemies food storage
Used to poison the troops of Marcus Antonius during the Parthian
Wars.
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Uses in Medicine:
Slows action of smooth muscle system
Parkinson’s symptoms
Irregularities in heart rate
Dilates pupils
Reduces salivation
Stomach and bladder cramps
Helps to relax pre-surgery patients
Combats infection and decreases pain when combined with methylene
blue, phenyl salicylate, and benzoic acid.
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2) Hyoscyamus niger :
Common Henbane
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History:
• Its botanical name Hyoscyamus is derived from the Greek words hyos
and cyamos, signifying 'the bean of the hog,' which animal is supposed to
eat it with impunity.
• An old AngloSaxon name for it was 'Belene,' probably from the bell-
shaped flowers; then it became known as 'Hen-bell,'
• and from the time that its poisonous properties were recognized this name
was changed to 'Henbane.
• It is also inclined that the name Henbane is derived from the Spanish
hinna (a mule), e.g. 'henna bell,' referring to the similarity of its seed-
vessel to the bell hung upon the neck of the mules.
• The medicinal uses of Henbane date from remote ages; it was well known
to the Ancients, being particularly commended by Dioscorides (first
century A.D.), who used it to procure sleep and allay pains.
• The annual and biennial form of henbane exist and both are used for
medicine but biennial is considered official
Morphology :
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3.DATURA
Jimson Weed
History :
The name “Jimson” comes from the word “Jamestown.” Early colonists
were known to have found the weed growing in abundance in Jamestown.
Dating and analysis of remains show 4000 years of use.
Was used as an aphrodisiac in the Middle Ages.
Very toxic and can cause hallucinations
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Description:
Grows to about 1.5m tall.
Annual shrub that grows mainly in the summer months (July – October).
Requires sunlight to grow.
Prefers neutral or basic, dry soils.
Large, white, funnel shaped flowers grow to about 5-10cm long.
Its fruits are large, thorny pods filled with seeds.
.
Traditional Uses:
Aphrodisiac
Wound and burn healer
Treating colds and asthma
Recent uses include treatments of epilepsy, acute mania
Over-the-counter powders and cigarettes were sold for asthma treatment.
Banned in 1968 as an over-the-counter drug.
Preparations:
Leaves are rolled into cigarettes for asthma treatment
Seeds can be crushed and used in drinks or teas
Flowers can be boiled
Leaf extracts or seeds can be made into pill form.
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Constituents:
Atropine
Scopolamine (main cause of hallucinations)
Hyoscyamine
Other tropanes.
Scopolamine:
Central nervous system depressant
Antimuscarinic effects similar to atropine
Commonly used to prevent motion sickness
Blocks short-term memory
Also used as a gastrointestinal and urinary antispasmodic
Hyoscyamine:
Has similar, but more potent, antimuscarinic effects as atropine and
scopolamine
Used as an adjunct in treatments of peptic ulcer disease and Zollinger-
Ellison syndrome
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C) Quinoline alkaloids
Quinoline alkaloids
Cinchona Alkaloids
It diverting to 4 main compounds
Quinine.
Cinchonine.
Cinchonidine.
Quindine.
Cinchona
Peruvian Bark
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Synonyms
Red Bark Cinchona Bark Peruvian Bark
Quina , Fever tree
Bot Name;
Cinchona officinalis
Family Rubiaceae
Part Used : Dried Bark from stem and branches.
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Constituents:
Alkaloids
Quinine,
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Cinchonidine,
Cinchonine,
Quinidine,
Quinamine,
Hydroquinine, and
Quinic acid
Quinidine
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Cinchonidine Cinchonine
Medicinal Uses:
Quinine has been used for the treatment of malaria and associated
febrile states
Febrifuge, tonic and astringent; valuable for influenza, neuralgia and
debility.
The liquid extract is useful as a cure for drunkenness. The powdered
bark is often used in tooth-powders, owing to its astringency
Cinchona in decoction is a useful gargle and a good throat astringent.
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D) Isoquinoline Alkaloids
Opium:
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Habitat-
The Opium Poppy is indigenous to Asia, and is cultivated largely in
European and Turkey, Persia, India and China for the production of Opium.
The term opium is from the Greek opion meaning poppy juice,
Papaver is the Latin name for the poppy
somniferum is Latin and means to produce sleep.
Description:
The plant is an erect, herbaceous annual, varying much in the colour of its
flowers, as well as in the shape of the fruit and colour of the seeds.
All parts of the plant, but particularly the walls of the capsules contain a
system of laticiferous vessels, filled with a white latex.
The flowers vary in colour from pure white to reddish purple.
The capsules vary in shape and size. They are usually hemispherical, but
depressed at the top, where the many-rayed stigma occupies the centre
The small kidney-shaped seeds, minute and very numerous, are attached
to lateral projections from the inner walls of the capsule and vary in
colour from whitish to slate.
Opium is extracted from the poppy heads before they have ripened.
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When the petals have fallen from the flowers, incisions are made in the
wall of the unripe capsules.
Care being taken not to penetrate to the interior.
The exuded juice, partially dried, is collected by scraping.
The scrapings being formed eventually into cakes, which are wrapped in
poppy leaves or paper and further dried in the sun.
The white milky juice darkening during the drying.
Raw opium
Collection:
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History:
The drug was known in very remote times and the Greeks and Romans
collected it.
It is probable that the physicians of the Arabian school introduced the
drug into India, as well as into Europe.
It was originally used only as a medicine, the practice of opium eating
having first arisen, probably in Persia.
Chemical constituents:
More than 30 alkaloids
Morphine (4 to 21%)
Codeine (0.8 to 2.5%) less active but more safer
Noscapine (4 to 8%) [noscapine is not sedative and has been used as
antitussive drug in various countries]
Papaverine (0.5 to 2.5%) [is an opium alkaloid antispasmodic drug,
used primarily in the treatment of visceral spasm, vasospasm (especially
those involving the heart and the brain, vasodilating agent and
occasionally in the treatment of erectile dysfunction]
Thebaine (0.5 to 2%). Thebaine is not used therapeutically, but as the
main alkaloid extracted it can be converted industrially into a variety of
compounds including oxycodone, oxymorphone,, naloxone.
Other include narceine, protopine, laudanine, codamine, cryptopine,
lanthopine and meconidine.
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Medicinal uses:
Acts on central nervous system. First stimulates and then depresses the
nerve response.
Relieve pain, diarrhea, dysentery and cough.
As antispasmodic
Antisecretory
Astringent
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E) Indole Alkaloids
1)Rauwolfia
2)Physostigma
3)Nux vomica
1) Rauvolfia serpentine:
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Common Names:-
Chota-Chand (Hindi)
Serpent wood (English)
Snake root (Hindi).
Bot name: Rauvolfia serpentina
Family:- Apocynaceae
Medicinally Important parts:- Roots and leaves.
Geo Location: It is mostly found in the decidous forest of Nepal, India,
Pakistan and Srilanka.
Description:
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Chemical Constituents:-
The major chemical constituents are:-
Serpentine
Reserpine
Ajmaline
Ajmalicine
Ricinn-amine
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Ajmalicine:-
Therapeutic Uses:
Fever
Constipation
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Joint pain
Hypnotic
As anti-hypertensives
As sedatives properties
Pharmacological action:
Reserpine is used to treat mild to moderate hypertension.
These are normally involved in controlling heart rate, force of contraction
and peripheral resistance.
The effects of reserpine include respiratory inhibition, stimulation of
peristalsis and influence on the temperature regulating centre.
Ethnomedical uses:
As the antidote against the bites of venomous reptiles, insect and
animal bites.
Used in the anxiety states.
Traditionally being used in the intestinal disorder.
2) Physostigma:
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• Synonyms:
Ordeal Bean, Calabar Bean
• Bot Name: Physostigma venenosum
• Family: Leguminosae (bean)
• Part Used: Seeds
• Habitat:
West Africa. Has been introduced into India and Brazil.
Description:
The plant came into notice in 1846 and was planted in the Edinburgh
Botanical Gardens, where it grew into a strong perennial creeper.
It is a great twining climber, pinnately trifoliate leaves, purplish bean-
like flowers; seeds are two or three together in dark brown pods.
The natives of Africa employ the bean as an ordeal owing to its very
poisonous qualities. They call it esere, and it is given to an accused
person to eat.
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3)Nux Vomica
Synonyms:
Poison Nut, Dog Button, Quaker Button
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The fruit are about the size of a large apple with a smooth and hard shell
which when ripened is a mild shade orange colour.
The flesh of the fruit is soft and white with a jelly-like pulp containing
five seeds covered with a soft woolly substance.
The seeds are removed from the fruit when ripe.
They are then cleaned, dried and sorted.
The seeds have the shape of a flattened disk completely covered with
hairs.
The seeds are hard.
Constituents:
Nux Vomica contains the alkaloids Strychnine , Brucine and traces of
strychnicine.
The glucoside Loganin, about 3 % fatty matter, caffeotannic acid and a
trace of copper.
The pulp of the fruit contains about 5 % of loganin together with the
alkaloid strychnicine.
Medical uses:
There are no uses in modern medicine, although it was widely used in
medicine before World War II.
The use of strychnine is highly regulated in many countries, and is mostly
used in baits to kill feral mammals including wild dogs, foxes, and
rodents.
Strychnine is a deadly poison with a lethal dose to humans of about 30 to
120 mg. LD50 = 16 mg/kg in humans, 1–2 mg/kg orally in rats.
https://www.youtube.com/watch?v=OLdCLJ_UqPM
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F)Imidazole Alkaloids
Pilocarpus:
• Synonyms:
Arrudabrava, Jamguarandi, Juarandi.
• Bot Name: Pilocarpus jaborandi
• Family: Rutaceae
• Part Used: Dried Leaves and roots.
• Habitat: South America.
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History:
• In sixteenth centaury it was first recorded that the Guarani Indians of
Brazil were using jaborandi to treat mouth ulcers, colds and flu, a remedy
against gonorrhea and kidney stones
• It was often used as an antidote to various poisons or toxins due to its
ability to promote sweating, urination and salivation.
Traditional uses:
In folk medicine systems in the tropics where it grows jaborandi has been used
as a natural remedy for epilepsy, convulsions, gonorrhea, fever, influenza,
pneumonia,
gastrointestinal inflammations, kidney disease, psoriasis, neurosis, and as an
agent to promote sweating.
• The introduction of jaborandi leaves to western medicine was in 1873,
when Symphronio Coutinho, a Brazilian doctor, went to Paris for a
European doctoral degree, taking with him samples of the leaves.
• The studies of a French Physician showed that jaborandi leaves
"increases enormously the perspiration and saliva, and, in a much less
degree, the secretion from the mucous membranes of the nose, the
bronchial tubes, and the stomach and intestines.
Description:
• The shrub grows from 4 to 5 feet high.
• The bark is smooth and greyish.
• The flowers are thick, small, and reddish-purple in colour.
Constituents:
• The principal constituents are the three alkaloids,
• Pilocarpine ,
• Isopilocarpine and
• Pilocarpidine.
• Pilocarpine, only in the proportion of 0.5% is found as a soft, viscous
mass yielding crystalline salts.
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G)Steroidal Alkaloids
The steroidal alkaloids represent a close structural relationship to sterols
i.e., they contain cyclopentanophenanthrene nucleus.
The steroidal alkaloids may be broadly classified into two major groups,
namely:
(a) Solanum Alkaloids
(b) Veratrum Alkaloids
Cyclo-pentano-phenanthrene nucleus:
Veratrum:
Synonyms: Hellebore
Bot. Name: Veratrum album
Family: Lilaceae
Parts Used: Rhizome, root.
Habitat: Europe, Does not occur in the British Isles.
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Description:
Veratrum album is distinguished by its yellowish-white flower.
The fresh rhizome has an alliaceous odour, but when dried it has no
marked smell.
Its taste is first sweet, then bitter and acrid, leaving the tongue tingling
and numb.
It is stated to have been one of the principal poisons used in Europe for
arrows, daggers, etc.
Constituents:
It contains
Jervine,
Pseudo-jervine,
Rubijervine,
Veratralbine and
Veratrine.
Recent: Jervine, veratramine, and their analogues as prostate cancer migration
and proliferation inhibitors
Medicinal Uses:
A violent, irritant poison. When snuffed up the nose it occasions profuse
running of the nose; when swallowed, severe vomiting and profuse
diarrhoea.
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1) Colchicum:
Common names: Meadow Saffron, Meadow Saffran, Autumn Crocus, Naked
Ladies, Upstart.
Biologcal source:
Colchicum autumnale Linn.
The dried ripe seeds, collected in early summer, as well as the (corm)
tubers (dried) are the medicinal parts of the plant.
The genus name is from Colchis on the black sea, where the plant
flourishes; autumnale refers to the season when the plant blooms.
Distribution:
Colchicum autumnale is primarily a central European plant found in
Northern Ireland, England, northern Germany, southern Poland, the
Ukraine, Bulgaria, Turkey, Albania and northern Spain. It also grows in
central Asia.
History:
Dioscorides mentions a colchicum
the Arabs recommended the use of the corm for gout in medieval times,
but the drug was abandoned because of its toxicity.
It again came into use in Europe about the middle of seventeenth century.
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Morphology:
Colchicum can grow to 40 cm in height.
The 3 to 4 broadly lanceolate leaves are tulip-like leaves appear together
with the fruit in spring.
They are 8 to 25 cm long, 2 to 4 cm wide and overlap at the base to form
a tube.
Characteristics: All parts of the plant are very poisonous and have a
disgustingly bitter and scratchy taste.
Collection:
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Medicinal uses:
• Gout
• Mediterranean fever(amilial Mediterranean fever (FMF), also known
as Armenian disease, is a hereditary inflammatory disorder).
The drug was previously used for skin tumors, psoriasis, necrotic
vasculitis(Necrotizing vasculitis is a rare condition that involves inflammation
of the blood vessel walls.), tendovaginitis(Tendovaginitis=an acute or chronic
inflammation of the tendon sheath, occurring in the region of the hand, the
wrist joint, the forearm (radial and ulnar tenobursitis), the foot, the ankle joint,
and the Achilles tendon (achillobursitis).), and inflammation of the
gastrointestinal tract, liver cirrhosis, acute and chronic leukemia; also for lice,
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Tea:
• Synonyms:
Thea sinensis, Thea Veridis, Thea bohea, Thea stricta Jassamica, Camellia
theifera.
• Bot Name: Camellia sinensis
Family: Camelliaceae
• Part Used: Dried leaf
• Habitat:
Assam; cultivated in Ceylon, Japan, Java, and elsewhere where climate
allows.
Description:
• A small evergreen shrub cultivated to a height of 7 to 8 feet. Bark is
rough and grey. Leaves are dark green, lanceolate margins shortly serrate,
young leaves hairy, older leaves are glabrous.
• Flowers solitary or two or three together on short branchlets.
• Fruit is a smooth, flattened, rounded, a size of a small nut.
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Production:
• Tea leaves are the fermented and/or dried leaves of Camellia sinensis.
• Green Tea is produced by steaming the fresh-cut leaf. Black Tea is
produced by allowing the leaves to oxidize. During oxidation, enzymes
present in the tea convert many of the polyphenolic therapeutic
substances to less active compounds.
• Oxidation does not occur with Green Tea because steaming process
inactivates enzymes responsible for oxidation.
• The anti-oxidant activity of Green Tea is six times greater than that of
Black Tea
• Constituents:
• Caffeine, tannin (10 to 20 per cent gallotannic acid), boheic acid,
volatile oil, aqueous extract, protein wax, resin, ash and theophylline.
• https://www.youtube.com/watch?v=YrjTQ9M0FFY
Medicinal Uses:
Black tea is used for improving mental alertness
Improve learning, memory and information processing skills
It is also used for treating headache and low blood pressure
Preventing heart disease, including “hardening of the arteries”
(atherosclerosis) and heart attack
Preventing Parkinson's Disease; and
reducing the risk of stomach and colon cancer, lung cancer, ovarian
cancer, and breast cancer
It is also used for type 2 diabetes, stomach disorders, vomiting, diarrhea,
and as a diuretic to increase urine flow.
Some people use black tea for preventing tooth decay and kidney stones
In combination with various other products, black tea is used for weight
loss
Taken moderately by healthy individuals it is harmless, but in excessive
quantities it will produce unpleasant nervous and dyspeptic symptoms, the
green variety being decidedly the more injurious.
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Glycosides
A glycoside is any molecule in which a sugar group is bonded through its
anomeric carbon to another group via glycosidic bond.
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CLASSIFICATION:
On the basis of glycone,
by the type of glycosidal linkage, and
by the aglycone
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Functions of glycosides:
Converting toxic materials to non or less toxic.
Source of energy (sugar reservoir).
Storing harmful products such as phenol.
Some glycosides have antibacterial activity, so they protect the plants
from bacteria and diseases.
Regulation for certain functions(growth).
Some have beautiful colours (pollenation process).
Like alkaloids, many plant glycosides possess physiological activity, e.g.
the cardiac glycosides are used medicinally.
Extraction and Isolation:
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Extraction of glycosides:
The plant material is macerated with water and then treated with lead
acetate to precipitate proteins and tannins.
It is then filtered and lead is removed as lead sulphide by a current of
hydrogen sulphide.
The solution is then shaken with ethanol or water in a Soxhlet extractor.
In the extract so obtained the enzyme is destroyed by heating it to a
temperature of about 65°C.
Then, the extract is concentrated to get the glycoside which is then
purified by employing usual methods.
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A)Cardioactive glycosides:
Steroid Glycosides
From a therapeutic perspective, this particular group of compounds may be
regarded as one of the most important of all naturally occurring plant products.
Cardio-active Glycosides:
Mechanism:
Increase the force of systolic contraction
Shorten length of systole
As a result
Heart have more time to rest between contraction.
Therapeutic activity depends upon;
1. Chemical nature of aglycone
2. Number of sugars
What are they used for?
Cardiac glycosides are cardiotonic drugs
Used in the treatment of congestive heart failure and cardiac arrhythmia
Aglycone is steroidal.
Aglycone may be;
Cardenolide (5-membered lactone at place of R)
Bufadinolide (6-membered lactone at place of R)
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17
17
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1 ) Digitalis:
Botanical Origin:
Digitalis purpurea
Digitalis lanata
Family:
Plantigenaceae
Part used:
Dried leaves
Collection:
Leaves collected from 2nd year growth of plant in June before opening of
flower.
Drying is done by applying artificial heat (temperature not more than 65°C).
Geographical Sources
It is mainly found in England, Germany, France, North America, India,
Iraq, Japan, Kurdistan, Mexico, Nepal, Spain, Turkey.
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Chemistry:
Four aglycons in Digitalis
Digitoxigenin
Gitoxigenin
Gitatoxigenin
Digoxigenin (only in Digitalis lanata)
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Digoxigenin Digoxin
Acetyl digoxin
Lanatoside C
(Acetyl digoxin + 1
glucose)
Deslanoside
(Digoxin + 1 glucose)
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2 ) Strophanthus:
Botanical Origin:
Strophanthus kombe
Strophanthus hispidus
Family:
Apocynaceae
Part used:
Dried ripe seeds
Collection:
Fruits are collected when fully ripen i.e. in June and July
Geographical Source
It is mainly found in East Africa near lakes of Nyasaland and
Tanganyika, Portuguese, Cameroon. The tribal are using this seeds as
arrow poison.
Chemistry:
Active constituent is Strophanthin.
Upon hydrolysis it yields;
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Strophanthidin
Sugars (alpha D-glucose + beta D-glucose + beta D-cymarose)
Apart from Strophanthin, there are;
30% fixed oils
Resin / Mucilage
Nitrogenous bases ( Trigonellin, Choline )
Uses:
Cardiac stimulant
Diuretic
3) White squill:
Botanical Origin:
Urginea maritima
Family:
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Liliaceae
Part used:
Dried fleshy scales of bulb
Collection:
Bulbs are collected in August. Outer scale is removed and inner scale is divided
into pieces and dried in sunlight.
Geographical Source:
It is found to be indigenous to those countries located near the
Mediterranean region, such as: France, Malta, Italy, Greece, Spain,
Algeria and Morocco.
Chemical Constituents
Squill has the following glycosides, namely:
Glucoscillaren A = Scillarenin + Rhamnose + Glucose + Glucose;
Scillaren A = Scillarenin + Rhamnose + Glucose;
Proscillaridin A = Scillarenin + Rhamnose.
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4)GLYCOSIDES BY BILAL MALIK
Uses:
Emetic
Expectorant
Cardiac tonic
Diuretic
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4)GLYCOSIDES BY BILAL MALIK
B) Anthraquinone Glycosides:
Anthracene Glycosides
Anthracene glycosides represent a major class of glycosides.
They are abundantly found in various dicot plant families, such as:
Ericaceae, Euphorbiaceae, Leguminoseae, Lythreaceae, Polygonaceae,
Rhamnaceae, Rubiaceae and Verbenaceae to name a few.
1)Aloe:
Synonym: Aloe
Biological Source:
Aloe is the dried latex of leaves of various species of Aloes, namely:
Aloe barbadensis Miller (Curacao Aloe);
Aloe ferox Miller (Cape Aloe);
Aloe perryi Baker ( Socotrine Aloe);
Aloe africana Miller and
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4)GLYCOSIDES BY BILAL MALIK
Geographical Source:
Curacao, Barbados, Aruba :
West Indian Islands, Cape Town (South Africa) :
Cape Aloes in Socotra and Zanzibar Islands
It is also cultivated in Europe and the North West Himmalayan region in
India.
Preparation:
General Method
The leaves are transversely cut at the base and the incised ends placed
downwards in a ‘V’ shaped trough(Trough= a long, narrow open
container) having a hole at its bottom.
The latex drains down the trough and is collected in individual containers
placed beneath.
The latex is evaporated in a kettle made of copper till it attains such a
consistency that it may be poured into metallic blocks where it gets
solidified.
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4)GLYCOSIDES BY BILAL MALIK
When the latex is concentrated gradually and then cooled slowly, it gives
rise to an opaque product. The aloe thus obtained is termed as ‘hepatic’ or
‘livery’ aloe.
If the latex is concentrated rapidly, followed by sudden cooling the
resulting product appears to be transparent and relatively brittle in nature.
The broken surface has a vitreous or glassy surface. Such a product is
commonly known as ‘vitreous’, ‘lucid’ or ‘glassy’ aloe.
Chemical Constituents:
Aloe-emodin occurs in the free state and as a glycosides in various
species of Aloe. Its concentration various in different species.
[Antidiabetic, protect the jejunum in rats with sepsis, antibacterial, radio-
protectant against radiation-induced intestinal injury, antiinflammtory
through multiple mechanism, skin disorders,
Aloin (barbaloin), antiinflammtory, anticancer, antibacterial and
cytotoxic,
Isobarbaloin (Curacao aloes), β-barbaloin (Cape aloes) .
Also contain Resin. The principal resin present in the aloes is known
as aloesin [aloesin, or aloe-gel exerts anti-inflammatory activity in a rat
colitis model; in vitro radical scavenging activity of different]
Uses:
Though, aloes is an official drug, that is mostly used as a purgative by
exerting its action mainly on colon.
Aloes find its usefulness as an external aid to painful inflammatory
manifestations.
It constitutes an important ingredient in the ‘Compound Tincture of
Benzoin’ ( Friar’s Balsam).
Aloe gel made from the mucilaginous latex of A. vera is frequently
employed in the treatment and cure of radiation burns to get immediate
relief from itching and pains.
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4)GLYCOSIDES BY BILAL MALIK
2) Rhubarb:
Synonyms:
Rheum; Radix rhei; Rhubarb rhizome.
Biological Source:
Rhubarb is the rhizome and roots of
Rheum officinale Bail.,
R. palmatum L.,
Rheum emodi Wall ;
R. webbianum Royle
Family Polygonaceae.
The rhizome and roots are mostly collected from 6-7 year old plants just
prior to the flowering season.
They are commercially available either with intact cortex or partially
decorticated.
Geographical Source
It is obtained largely from cultivated as well as wild species of Rhubarb
grown in regions extending from Tibet to South East China.
It is also found in Germany and several European countries.
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4)GLYCOSIDES BY BILAL MALIK
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4)GLYCOSIDES BY BILAL MALIK
Uses
It is used mainly in the form of an ointment in the treatment and cure of
chronic eczema, psoriasis and trichophytosis—as a potent keratolytic
agent. [https://www.youtube.com/watch?v=OMCU26CGkQg]
It is employed in the treatment of diarrhoea.
It is also used as a purgative.
Cascara Sagrada
Interestingly, the very name ‘cascara sagrada’ is Spanish for the sacred
bark;
Rhamnus is the ancient classical name for buckthorn, and Purshianus was
attributed as a mark of honour and respect to the great German botanist
Friedrich Pursch.
Synonyms Sacred bark; Chitten bark; Chittin bark; Purshiana bark;
Persian bark; Bearberry bark; Bearwood; Cascara bark; Cortex Rhamni
purshianae.
Biological Source Cascara sagrada is the dried bark of Rhamanus
purshiana DC., belonging to family Rhamnaceae, from which a naturally
occurring cathartic is extracted.
It is usually collected at least one year prior to its use.
Geograhical Source
It is invariably obtained from cultivated as well as wild shrubs and small
trees grown in Northern Idaho, West to Northern California, North
Carolina, Oregon, in Kenya and Western Canada.
Preparation
The bark is collected, during the dry season (April to August) from the 8
to 9 years old trees that have gained a height of 16-18 meters with their
stems having a diameter of 8 to 10 cm, by inflicting longitudinal incisions
on the fully developed stems.
The bark is carefully stripped off from the branches and the stems.
They are subsequently allowed to dry in shade by putting their inner-
surface facing the ground so as to permit the completion in the enzymatic
conversion of the anthranol derivative i.e., glycosides (an emetic
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4)GLYCOSIDES BY BILAL MALIK
C)Saponin Glycosides
- "Sapo" is Latin name for soap (soap-like)
-Group of organic compounds that form persistent froth when shaken with
water even in dilute solution.
Properties:
• - Soluble in water, alcohol and mixture of them.
• Form persistent froth with water.
• - Used as detergent (surfactant) and emulsifying agent
• - Cause haemolysis of RBC’s if reach the blood (injection).
• - Only small part absorbed when taken orally.
• - Enhance the absorption of other drugs.
• - Form precipitate with Ba(OH)2-
Classification of Saponins:
• According to the nature of the aglycone, saponins are classified into
Steroidal and Triterpenoidal saponins.
• According to sugar: monodesmoside (one sugar chain), Bidesmoside
(two sugar chains)
29 30
21 22 sugars 19 20
12 18 E
18 20
24 26 11 17
17 13
11 25 26
19 1 D 28
D 25 14
sugars 1 C sugars
14 27 8
10 A B
A B 3 27 sugars
3 7
7 HO 5
HO 5
23 24
Triterpenoidal Saponins:
- Very common in Dicot plants
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4)GLYCOSIDES BY BILAL MALIK
1) Liquorice
• Synonyms :
Glycyrrhiza; Liquorice root; Glycyrrhizae radix.
Biological Sources:
• Liquorice consists of subterranean peeled and unpeeled stolons, roots and
subterranean stems of Glycyrrhiza glabra Linn, and other species of
Glycyrrhiza, belonging to family Leguminosae.
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4)GLYCOSIDES BY BILAL MALIK
• The word Glycyrrhiza has been derived from the Greek origin that means
sweet root; and glabra means smooth and usually refers to the smooth,
pod-like fruit of this particular specie.
Geographical Sources:
• It is mainly found in China, Europe, India, Iraq, Japan,Kurdistan, Spain,
Turkey, and the United States.
Preparation:
The roots are usually harvested after 3 to 4 years from its plantation when
they mostly display enough growth.
The rhizomes and roots are normally harvested in the month of October,
particularly from all such plants that have not yet borne the fruits, thereby
ascertaining maximum sweetness of the sap.
The rootlets and buds are removed manually and the drug is washed with
running water.
The drug is first dried under the sun and subsequently under the shade till
it loses almost 50% of its initial weight.
The large thick roots of the Russian Liquorice are usually peeled before
drying.
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4)GLYCOSIDES BY BILAL MALIK
COO-
30
12
O
11
K+, Ca++
2 glucuronic acid O
Glycyrrhetic acid
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4)GLYCOSIDES BY BILAL MALIK
Side effects:
Salt and water retention, elevation of blood pressure in susceptible persons.
2)Sarsaparilla:
Botanical source
• Smilax aristolochiaefolia
• Smilax regelii
• Smilax febrifuga
• The plants produce numerous roots 3 m or so long which are attached to a
short rhizome.
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4)GLYCOSIDES BY BILAL MALIK
Morphology:
• These consist of long roots with or without pieces of rhizome and an
aerial stem.
• The commercial varieties differ from one another in colour, ridges and
furrows.
• The drug is nearly odourless but has somewhat sweetish and acrid taste.
Constituents:
• The main constituent is a saponin glycoside, sarsaponin which on
hydrolysis yields sarsasapogenin and dextrose.
• It also contains a small proportion of starch, sarsapic acid, and fatty acids,
palmitic, stearic, behenic, oleic and linolic.
Uses:
• In the treatment of syphilis, rheumatism and certain skin diseases
• Sarsaparilla is widely used as vehicle, and large quantities are employed
in the manufacture of non alcoholic drinks.
• The genins are used in the partial synthesis of cortisone and other
steroids.
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D)Cyanogenic Glycosides
Cyanophore glycosides
• The cyanogenic glycosides are named so because they yield either
hydrocyanic acid upon hydrolysis or they essentially possess a
hydrocyanic acid in the aglycone moiety.
• They are also designated as ‘cyanophore glycosides ’ [blue coloration].
• Rosaceae being the most prominent one amongst them.
• cyanogenic glycoside containing drug substances, as such do not exert
any specific therapeutic activity, but they are invariably employed as
viable pharmaceutical aids, such as: flavouring agents.
• A large number of cyanogenic glycosides were isolated and identified
from various plant sources, namely:
• Linamarin [impaired motor coordination in rats, neurotoxin, ]
• Linustatin
• Lotaustralin and
• Lucumin
• A few important examples of naturally occurring drug substances
containing cyanogenic glycosides are;
• Bitter almond,
• Wild cherry bark and
• Linseed.
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4)GLYCOSIDES BY BILAL MALIK
Geographical Source:
• Wild Cherry bark is found to be indigenous to the Eastern States of
USA and certain parts of Canada.
• However, in the United States it is found abundantly in Dakota, Florida,
Missisipi, North Carolina and Virginia.
Preparation:
It has been established that the wild cherry bark possesses the highest
potency only during the autumn.
As the inner layer of the bark contains a substantial amount of Hydrogen
cyanide(Hydrogen cyanide poisonous and flammable liquid that boils
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4)GLYCOSIDES BY BILAL MALIK
slightly above room temperature, at 25.6 °C (78.1 °F).), hence soon after
collection, it is necessary to get rid of the inner layer.
Consequently, after the removal of cork as well as a portion of the cortex,
give rise to an uniform dark brown coloured product, which is
commercially known as Rossed Bark.
The resulting Rossed bark is dried in the shade and stored carefully in a
dry place for onward transmission to several countries as a valued export
material.
Chemical Constituents:
• Wild cherry bark essentially contains a cyanogenic glycoside termed as
prunasin
(mandelonitrile glucoside)
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4)GLYCOSIDES BY BILAL MALIK
Uses:
The syrup of wild cherry is mostly employed as a flavoured vehicle in
cough syrup.
Wild cherry is used for colds, whooping cough, bronchitis and
other lung problems; diarrhea; gout; digestive disorders; pain; and cancer
It is also used in cough syrups because of its sedative, expectorant,
drying, and cough-suppressing effects.
E) Thioglycosides
• This specific group of glycosides is also referred to as ‘Thiocynate
Glycosides’ or ‘Sulphurated Glycosides’ or Isothiocyanate
Glycosides’ in various literatures.
• The aglycone portion of such glycoside essentially contains isothiocynate
residue having sulphur plus nitrogen atoms.
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4)GLYCOSIDES BY BILAL MALIK
1) Black Mustard:
Biological Sources :
These are dried ripe seeds of Brassica nigra Linn., or Brassica juncea Linn,
belonging to family Cruciferae.
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4)GLYCOSIDES BY BILAL MALIK
Geographical Sources:
• B. nigra is extensively cultivated in various parts of Europe and United
States.
• B. juncea is widely grown in different parts of India, Russia
Preparation:
• The thioglycoside sinigrin is obtained from the defatted black- mustard
seed by employing standard methods.
• It is usually present in the seeds to the extent of 4%.
• Black mustard seeds are powdered and defatted with petroleum ether.
• The defatted meal is boiled with ethanol to destroy the enzyme.
• The resulting marc is squeezed while hot, dried at 100°C and macerated
in cold water for 3-4 hours with constant stirring, since Sinigrin is fairly
soluble in cold water.
• The liquid content is decanted and maceration is repeated a number of
times to ensure complete extraction of the thioglycoside.
• The combined aqueous extract is collected and treated with mild alkalies,
such as : Barium carbonate, so as to neutralize any free acidity.
• The liquid is now concentrated under vaccum to a syrupy consistency.
• The resulting syrup is boiled with ethanol (95% w/v) for about 2-3 hours
to allow sinigrin to dissolve and at the same time to precipitate the
mucilage- components.
• The alcholoic extracts are filtered and allowed to cool slowly when
sinigrin crystallizes out (approximately 4%).
Chemical Constituents:
• The black mustard seed contains a thioglycoside i.e., sinigrin. It is also
known as myronate potassium or allyl glucosinolate
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4)GLYCOSIDES BY BILAL MALIK
Uses:
• A paste of black mustard seed is mostly in form of plaster or poultice as
rubefacient and counter irritant.
• In higher doses when administered internally it acts as an emetic.
• Black mustard seeds are invariably used as a widely accepted condiment
in the preparation of pickles, curries and vegetables.
• The fixed oil is widely employed as a popular edible oil.
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4)GLYCOSIDES BY BILAL MALIK
F) Aldehyde Glycosides
Vanilla:
• Synonyms
Vanilla beans, Vanilla pods.
• Biological Sources
Vanilla consists of the cured fully grown but unripe fruits of Vanilla
fragrans (Salis.), belonging to family Orchidaceae.
Geographical Sources:
• The plant is indigenous to the Eastern coast of Mexico.
• Presently, it is widely cultivated in West Indies, Java, Madagascar,
Ceylon, France, Indonesia, Uganda, Hawaii and India.
Preparation:
• The full grown and unripe fruits are hand picked at that particular stage
when their color changes from green to yellow.
Uses:
1. It is mostly used as a pharmaceutical aid for flavouring various liquid
preparations.
2. Vanillin enhances the chocolate flavor of cocoa based malted milk foods.
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4)GLYCOSIDES BY BILAL MALIK
• G)Lactone glycosides
Cantharidin
is an odorless, colorless
Biological Sources:
Cantharidin, a type of is a chemical compound secreted by many
species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria
belonging to the family Meloidae
• . It has been found that the soft parts of the insect are the chief seat of
cantharidin. Besides, cantharidincontain 0.5 to 0.95 of cantharidis.
Isolation:
• The various steps involved in the isolation of cantharidin are:
1. The dried insects are collected and powdered. Then treated with an acid
whereby the cantharidin gets liberated in the form of its corresponding
salts.
2. The resulting product is subjected to extraction, of both cantharidin and
fat, by the help of ethyl acetate in a Soxhlet apparatus.
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4)GLYCOSIDES BY BILAL MALIK
3. The solvent is removed carefully under reduced pressure and the crude
cantharidin crystallizes out.
4. The fat may be removed with the help of petroleum ether, in which
cantharidin is only negligibly soluble.
5. Ultimately, the crude defatted cantharidin is dissolved in a minimum
quantity of hot ethanol and allowed to cool when cantharidin crystallizes
out in its purest form.
Characteristic Features:
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4)GLYCOSIDES BY BILAL MALIK
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5)PLANT STEROIDS BY BILAL MALIK
PLANTS STEROIDS:
Contents:
• What are steroids?
• Sources
• Nomenclature
• Biosynthesis
• Plant steroids and their uses
Plant sterols
Cardiac glycosides
Steroidal sapogenins
Ecdysones
Withanolides
• Animal steroids and their uses
Steroid hormones (Sex hormones and adrenocortical
hormones)
Bile acids
Ecdysones
INTRODUCTION:
• Steroids comprise a natural product class of compounds widely
distributed throughout nature.
• A steroid is an organic compound with four rings arranged in a specific
configuration.
• Steroids have two principal biological functions: certain steroids (such as
cholesterol) are important components of cell membranes which alter
membrane fluidity, and many steroids are signaling molecules which
activate steroid hormone receptors.
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5)PLANT STEROIDS BY BILAL MALIK
• Hundreds of steroids are found in plants, animals and fungi. All steroids
are manufactured in cells from the sterols:
• lanosterol (animals and fungi) or
• cycloartenol (plants).
• Plant steroids (aka Phytosteroids) are naturally occuring steroids that are
found in plants.
• Examples include digoxin, digitoxin, diosgenin, and guggulsterone, as
well as phytosterols like β-sitosterol and other phytoestrogens like
isoflavones.
• Guggulsterone-E and guggulsterone-Z, are the potent hypolipidemic and
hypocholesterolemic bioactive molecules present in the gum resin of
Commiphora wightii.
• In plants, cholesterol is widely distributed but often present in minute
quantities; other steroids not found in animals (the Phytosterols) tend to
predominate.
NOMENCLATURE:
• A steroid is any compound that contains a cyclo-penta-noper-hydro-
phenanthrene nucleus.
• Each parent tetracyclic hydrocarbon bears a specific stem name. Steroids
are numbered and rings are lettered as indicated in the structural formula
for cholesterol.
• When the rings of a steroid are denoted as projections onto the plane of
the paper, an atom or group attached to a ring is termed α if it lies below
the plane and β if it lies above the plane.
• The use of a stem name implies that atoms or groups attached at the ring
junction positions 8,9,10,13 & 14 are oriented as shown (8α ,9α , 10β,
13β, 14α) and a carbon chain attached to position 17 is assumed to be β
oriented.
• The configuration of hydrogen or a subsyituent at the ring-junction
position 5 is always designated by adding α or β after the numeral 5. This
numeral and letter are placed immediately before the stem name.
• For example, the chemical name of cholic acid is 3α, 7α, 12α-
trihydroxy-5β-cholan-24-oic acid.
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5)PLANT STEROIDS BY BILAL MALIK
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5)PLANT STEROIDS BY BILAL MALIK
BIOSYNTHESIS:
• The hundreds of steroids found in animals, fungi, and plants are made
from lanosterol (in animals and fungi) or cycloartenol (in plants).
• Lanosterol and cycloartenol derive from cyclization of the triterpenoid
squalene.
• In animals the biosynthesis of steroids follows the mevalonate pathway,
which uses acetyl-CoA as building blocks for dimethylallyl
pyrophosphate (DMAPP) and isopentenyl pyrophosphate (IPP). In
subsequent steps DMAPP and IPP join to form geranyl pyrophosphate
(GPP), which synthesizes the steroid lanosterol.
• In plants, the non-mevalonate pathway uses pyruvate and glyceraldehyde
3-phosphate as substrates.
• Squalene Squalene oxide Protosteryl cation
Cycloartenol Sitosterol Stigmasterol
• Steroids are formed biosynthetically from isopentenyl pyrophosphate
(active isoprene).
• Steroid biosynthesis in plants proceeds via mevalonate and FPP in the
cytosol but differs from the pathway in mammals and fungi because of
the intermediary of the unusual cyclopropane ring-containing sterol
cycloartenol. A series of intricately co-ordinated Wagner-Meerwein
rearrangements accompanies the cascade of cyclization events which
produce the cycloartenol skeleton.
• Formation of cholesterol may be considered as a general mechanism of
steroid biosynthesis:
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5)PLANT STEROIDS BY BILAL MALIK
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5)PLANT STEROIDS BY BILAL MALIK
Pyruvate +
Acetyl-CoA
Glyceraldehyde
phosphate
Acetoacetyl-CoA
Deoxy xylose phosphate
HMG-CoA
2-C-methyl-D-erthritol
4-phosphate
Mevalonate
Various erythitol
phosphate
Mevalonate intermediates
pyrophosphate
2-methylbutane-1,4-diol
IsoPentenyl
diphosphate
pyrophosphate (IPP)
+ Dimethylallyl
pyrophosphate Isopentenyl
pyrophosphate+
Dimethylallyl
Squalene pyrophosphate
Lanosterol Squalene
Cholesterol Cycloartenol
1) PLANT STEROLS:
• The first steroid isolated from nature were a series of C27-C29 alcohols
that were found in the lipid fractions of many tissues. These compounds
were solids and therefore named sterols from the greek stereos- meaning
solid.
• The most widely occuring sterol is cholesterol. It has been identified in
animals, algae, fungi, actinomycetes, bacteria, ferns and higher plants.
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5)PLANT STEROIDS BY BILAL MALIK
• The plant sterols are similar to cholesterol and vary only in carbon side
chains and/or presence or absence of a double bond. More than 200
sterols and related compounds have been identified.
• The most common sterol in plants is β-sitosterol, a C29 compound.
• Closely related to β-sitosterol is stigmasterol, first isolated from calabar
beans but is also found in soybean oil.
• Stanols are saturated sterols, having no double bonds in the sterol ring
structure.
• Free phytosterols extracted from oils are insoluble in water, relatively
insoluble in oil, and soluble in alcohols.
• The richest naturally occurring sources of phytosterols are vegetable oils
and products made from them.
• Phytosterols are currently approved by the U.S FDA for use as a food
additive; however, there is some concern that they may block absorption
not only of cholesterol (thus helping to reduce cholesterol), but of other
important nutrients as well.
• At present, the American Heart Association has recommended that
supplemental plant sterols be taken only by those diagnosed with elevated
cholesterol, and has particularly recommended that they not be taken by
pregnant women or nursing mothers.
Sitosterols:
• Composition: The drug sitosterols is a mixture of β-sitosterols and
certain saturated sterols.
• It contains no less than 95% of total sterols and not less than 85% of
unsaturated sterols.
• Characteristics: It is a white, odourless, tasteless powder that is
practically insoluble in water.
• Source: They are widely distributed throughout the plant kingdom and
may be obtained from wheat germ oil, rye germ oil, cottonseed oil, corn
oil and other seed oils.
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5)PLANT STEROIDS BY BILAL MALIK
2) STEROIDAL SAPOGENINS:
• Sapogenins are the aglycones, or non-saccharide, portions of the family
of natural products known as saponins. Steroidal sapogenins contain
steroid framework as their key organic feature. Some steroidal sapogenins
can serve as a practical starting point for the semisynthesis of particular
steroid hormones.
• Occurrence:
• They are found in many monocotyledonous families. particularly the
Dioscoreacea (e.g. Dioscorea spp.) Agavaceae (e.g. Agave and Yucca
spp.) and Smilacacea (smilax spp.).
• In the dicotyledons the occurrence of diosgenin in Fenugreek
(Leguminosae) and of steroidal alkaloids in Solanum (Solanaceae) is of
potential importance. Some species of Strophanthus and Digitalis contain
both steroidal saponins and cardiac glycosides.
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5)PLANT STEROIDS BY BILAL MALIK
Uses:
• Steroidal saponins are of great pharmaceutical importance because of
their relationship to compounds such as the sex hormones, cortisone,
diuretic steroids, vitamin D and the cardiac glycosides.
• Some plant saponins can weakly mimic the human hormones that they
resemble. For example, yam (Dioscorea spp.) contains variable amounts
of a saponin called diosgenin, which can be converted into hormones
such as progesterone and estrogen. In fact, Mexican yam (D. composita)
has been used to make oral contraceptives
• Hecogenin (steroid isolated from Agave sisalana) with C-ring
substitution provides a practical starting material for the synthesis of
corticosteroids.
• Solanum species are noted for the production of C27 steroidal alkaloids.
Some of these alkaloids are the nitrogen analogues of Solasodine &
diosgenin etc. They are employed in the partial synthesis of steroidal
drugs.
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5)PLANT STEROIDS BY BILAL MALIK
3) CARDIAC GLYCOSIDES:
• Occurrence:
• These glycosides are found in the plant genera Digitalis, Scilla, and
Strophanthus. They are used in the treatment of heart diseases, e.g.,
congestive heart failure and arrhythmia.
• A considerable number of plants throughout the plant kingdom contain
steroidal glycosides which exert on the failing heart a slowing and
strengthening effect. These steroids occur as glycosides with sugars
attached at the 3-position of the steroid nucleus.
• Structure of glycosides
• Two types of genin may be distinguished: cardenolides (C23 steroids)
and bufanolides (C24 steroids).
• The sugar moieties, attached to the aglycone by a C-3, B-linkage are
composed of upto four sugar units.
• Bufalin, ouabain and digoxin are a few toxic cardiac glycosides. Digoxin
from the foxglove plant is used clinically, whereas bufalin and ouabain
are used only experimentally due to their extremely high potency.
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5)PLANT STEROIDS BY BILAL MALIK
4) STEROID HORMONES:
• The steroid hormones can be divided into two classes:
• The sex hormones and the adrenocortical hormones.
• Sex hormones are produced in the gonads and fall into 3 chemically and
physiologically distinct categories:
• The estrogens & progestins (regulates various functions of female
reproductive tract) and androgens (stimulates development of the male
reproductive organs)
• The adrenocortical hormones are produced by the outer cortical portion of
the adrenal glands and they are divided into 2 classes, depending on their
biologic activity:
• Mineralocorticoids (affects the excretion of fluid and electrolytes) and
glucocorticoids (affects intermediary metabolism)
Commercial Production of Steroids:
• At the present time, the principal source of the steroid chemical nucleus
used in the drug industry is the plant kingdom.
• Initially, the source of steroid hormones was from gonads and adrenal
glands of animals but the amount of hormones present in these glands
was extremely small and large quantities of glands were required to
isolate mg quantities of hormones.
• A vast amount of research has resulted in extension and improvement of
the basic procedure of isolation.
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5)PLANT STEROIDS BY BILAL MALIK
5) BILE ACIDS:
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5)PLANT STEROIDS BY BILAL MALIK
• In the liver of man and other animals the side chain of cholesterol is
degraded to C24 steroids, which possess a C-24 carboxyl. These steroids
are collected as the bile, therefore they are referred to as bile acids.
• Primary bile acids formed in the liver of man are: Cholic acid and
chenodesoxycholic acid.
• Des-oxycholic acid and lithocholic acid are produced in the intestinal
tract by the action of microorganisms.
• Generally, bile acids are conjugated to glycine or taurine through a
peptide bond. The conjugated bile aids are discharged into the duodenum
to where they act as emulsifying agents to aid in the absorption of fats.
Functions of Bile Acids:
• Eliminates cholesterol from the body,
• Drives the flow of bile to eliminate certain catabolites (including
bilirubin)
• Emulsifies fat-soluble vitamins to enable their absorption,
• Aids in motility and the reduction of the bacteria flora found in the small
intestine and biliary tract.
• Bile acids also act as steroid hormones having various direct metabolic
actions in the body through the nuclear receptor Farnesoid X receptor
(FXR)
Ox bile extract:
• Bile salts are the sodium salts of the conjugated acids and are the
principal constituent of ox bile extract.
• Preparation:
1. Partial evaporation of fresh ox bile
2. Precipitation of the mucus and albuminous matter with alcohol
3. Filteration
4. Washing
5. Evaporating the combined filtrates to dryness at a temperature not
exceeding 80 C.
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5)PLANT STEROIDS BY BILAL MALIK
6) WITHANOLIDES:
• Withanolides are a group of at least 300 naturally occurring steroids built
on an ergostane skeleton
• In 1968, the structure of a constituent lactone (withaferin A) of Withania
somnifera was determined, since then many more compounds have been
characterized.
• Other genera of the family in which they occur include: Aenistus, Datura,
Hyoscyamus, Iochroma, Jaborosa, Lycium, Nicandra, Physalis and
Solandra.
• The first report of a withanolide from the Labiatae concerns the
characterization of a new compound, ajugin, from ajuga parviflora whole
plants.
Examples and Uses:
• They have potential pharmacological value as sedatives, hypnotics,
antiseptics and anti-mitotics.
• Some withanolides are cell differentiation inducers- compounds of a new
type of anti tumour agent.
• Withaferin A acts as an anti angiogenic compound by inhibiting
Transcription Factors Sp1 and NF-κB. Withaferin A also inhibits
angiogenesis on chick chorioallantoic membrane. Withanalides inhibit
COX-2 and exhibit anti-inflammatory activity.
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5)PLANT STEROIDS BY BILAL MALIK
7) ECDYSONES:
• The ecdysis of insects relates to the moults which larvae undergo during
their transformation into an adult, a process controlled by complex
hormonal mechanisms.
• Ecdysones, insect-moulding hormones, are substances which stimulates
these changes and one example is ecdysone itself, first isolated from silk-
worm pupae.
• Ecdysone is a steroidal prohormone of the major insect molting hormone
20-hydroxyecdysone, which is secreted from the prothoracic glands
• In plants they occur in much greater variety and abundance, where they
appear mostly as protective agents against herbivorous insects.
• Insects do not themselves biosynthesize steroids de novo and rely on
plant materials for suitable precursors.
• Ecdysterone is also an example of one which has been obtained from
both plant and insect sources.
• In the plant, cholesterol is a precursor of insect-moulding hormones and
in one morphological group of helleborus, it has been shown that they are
formed together with bufadienolides and saponins.
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5)PLANT STEROIDS BY BILAL MALIK
162
6. LIPIDS NOTES BY BILAL MALIK
LIPIDS:
• Lipids (fixed oils, fats, and waxes) are esters of long-chain fatty acids
and alcohols, or of closely related derivatives.
• The chief difference between these substances is the type of alcohol;
• In fixed oils and fats, glycerol combines with the fatty acids;
• In waxes, the alcohol has a higher molecular weight, e.g.,
cetyl alcohol[CH3(CH2)15OH].
Fats and oils are made from two kinds of molecules:
• glycerol (a type of alcohol with a hydroxyl group on each of its three
carbons) and
• three fatty acids joined by dehydration synthesis. Since there are three
fatty acids attached, these are known as triglycerides.
Triglyceride:
O
H2C O C R
O
HC O C R'
O
H2C O C R''
• where R, R', and R" are long alkyl chains; the three fatty acids RCOOH,
R'COOH and R"COOH can be all different, all the same, or only two the
same.
• Fats, which are mostly from animal sources, have all single bonds
between the carbons in their fatty acid tails, thus all the carbons are also
bonded to the maximum number of hydrogens possible.
• Since the fatty acids in these triglycerides contain the maximum possible
amount of hydrogens, therefore are called saturated fats.
• The hydrocarbon chains in these fatty acids are, thus, fairly straight and
can pack closely together, making these fats solid at room temperature.
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6. LIPIDS NOTES BY BILAL MALIK
• Oils, mostly from plant sources, have some double bonds between some
of the carbons in the hydrocarbon tail, causing bends in the shape of the
molecules.
• Because some of the carbons share double bonds, they’re not bonded to
as many hydrogens as they could if they weren’t double bonded to each
other. Therefore these oils are called unsaturated fats.
• Because of the kinks in the hydrocarbon tails, unsaturated fats (or oils)
can’t pack as closely together, making them liquid at room temperature.
Production of fixed oils and fats:
Fixed oils and fats of vegetable origin are obtained by:
1. Extraction by expression
Fixed oils are obtained by expression in hydraulic presses. If the
expression is carried out in the cold, the oil is known as a "cold-pressed oil." In
contrast, if the expression is carried out in heat, the oil is known as a "hot-
pressed oil."
2. Extraction by solvents
Sometimes organic solvents are used for the extraction of oils.
• Animal fats are separated from other tissues by rendering with steam,
with or without pressure. The heat melts the fat, which rises to the top and
may be separated by decantation.
Biosynthesis of lipids:
• The biosynthesis of saturated and unsaturated fatty acids is from
combinations of acetate units (acetate pathway).
Applications of fixed oils and fats:
1. Soap manufacture
2. Suppositories, tablet coating
3. Dietary supplements
4. Emulsifying agents
5. Manufacture of paints, varnishes and lubricants
6. Therapeutic uses (castor oil).
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6. LIPIDS NOTES BY BILAL MALIK
Examples
Castor oil
Olive oil
Peanut oil
Soybean oil
Sesame oil
Almond oil
Cottonseed oil
Corn oil
Waxes:
• Like fats, waxes are esters of fatty acids. The alcohol, however, is not
glycerol but usually a long-chain, high-molecular weight alcohol.
• In plants, waxes are generally found covering the external parts, like the
epidermis of leaves and fruits, where their main function is to prevent the
loss of water.
• Wax is also produced by insects, e.g. the honeycombs of bees and wasps.
USES OF WAX
1. Wax is used in pharmacy to make soft ointments harder and to prepare
lips-salves, [lips balm].
2. The technical uses of waxes are substantial, e.g. in shoe polishes and car
waxes.
Examples:
• Jojoba wax (Simmondsia chinensis)
• Beeswax (Apis mellifera)
• Carnauba wax (Copernicia cerifera)
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6. LIPIDS NOTES BY BILAL MALIK
FIXED OILS:
PHYSICAL PROPERTIES:
Cannot be distilled (unless decomposed). This distinguishes fixed oils
from volatile oils.
Leaves a permanent, translucent stain on filter paper.
Specific gravity < 1.
All insoluble in water. Soluble in organic solvents.
Most develop a rancid odour when exposed to air, moisture & light for
prolonged periods of time (hydrolysis of esters & liberation of fatty acids)
All have characteristic odours.
Varying viscosities.
BEFORE EXTRACTION:
Plant material to be pressed undergoes strict quality control.
- absence of foreign matter & deterioration
GENERAL PRELIMINARY PROCEDURES:
- Cleaning & drying
SPECIFIC PRELIMINARY PROCEDURES (depends on the seeds’
botanical structure)
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6. LIPIDS NOTES BY BILAL MALIK
- Olives: washed
- Cotton: Delintering
- Castor seeds & ground nuts: decorticating.
- Peanuts, soybeans, sunflower seeds: Shelled.
METHODS OF EXTRACTION:
i. Extraction by Expression
- Cold Expression
- Hot Expression
ii. Extraction by Solvents
1. EXTRACTION BY EXPRESSION:
Screw presses are normally used to express oils from plant material
because they give a better yield than older hydraulic presses.
They also operate at higher pressure and continuously (not in batches).
Before undergoing expression, seeds rich in proteins are cooked at 90ºC
frees the oil by bursting the cell structures & coagulates the proteins.
A fast drying step normally follows.
a. COLD EXPRESSION:
Oils for medicinal uses are extracted at room temperature. Only a portion
of the oil is obtained.
Oil is normally less viscous with less odour than with hot expression
(better quality).
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6. LIPIDS NOTES BY BILAL MALIK
The remaining pressed material may then be ground, heated and pressed
to express any remaining oil.
b. HOT EXPRESSION:
The residue left after cold expression is broken down and treated with
steam. This causes the remaining oil cells to rupture.
Even after hot expression, 10 % of the oil remains in the plant material.
ii. EXTRACTION BY SOLVENTS:
This type of method is used only for technical oils (not medicinal oils).
Seeds used: Intact or partially extracted by expression.
Solvent: Normally hexane (BP: 65 ºC)
Method: Solvent is added to the cleaned, hulled & roughly milled seeds.
The organic phase is recovered. (Organic phase: solution containing the
oil in the solvent (called miscella) , and also solvent soaked defatted
meal).
Oil recovery: 95 – 99%
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6. LIPIDS NOTES BY BILAL MALIK
i)PHYSICAL CONSTANTS:
a. Specific Gravity
b. Melting / Congealing Point
c. Refractive Index
d. Viscosity
e. Optical Rotation
ii)CHEMICAL CONSTANTS:
a. Acid Values
b. Saponification Value
c. Ester Value
d. Iodine Value
e. Unsaponifiable Matter
f. Acetyl value.
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6. LIPIDS NOTES BY BILAL MALIK
CLASSIFICATION:
On the basis of their ability to absorb
oxygen from air;
• a)Drying oil
• b)Non-drying oil
• c)Semi-drying oil
a) Drying oil:
When exposed to air, undergo oxidation and form tough and hard film. These
are usually used in paints and varnishes.
For example;
Linseed oil
b) Non-Drying oil:
These oils neither undergo oxidation nor form tough and hard film.
For example;
Olive oil
c) Semi-Drying oil:
When exposed to air, undergo little bit oxidation and form tough and thin film.
For example;
Cottonseed oil
Inflammatory diseases
Facilitate wound healing
Skin repair based on this fatty acid mainly found in the Mediterranean
diet.
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6. LIPIDS NOTES BY BILAL MALIK
OLIVE OIL:
Olive oil is the oil expressed from the ripe fruits of Olea europea (Oleaceae
Family).
The latifolia variety bears larger fruit, but the longifolia variety yields the best
oil.
Common Names: Salad oil, sweet oil
Geographical Sources: Mediterranean, California, Spain, France, Greece &
Tunisia.
OLIVE OIL: CHARACTERISTICS:
Olive oil: Pale yellow liquid, sometimes with a green tint.
Oil has a slight odour & bland taste.
OLIVE OIL: CONSTITUENTS:
Oils from different sources differ slightly in their constituents (composition).
This may result due to the different varieties of olive used, or to climate
differences.
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6. LIPIDS NOTES BY BILAL MALIK
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6. LIPIDS NOTES BY BILAL MALIK
CASTOR OIL:
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6. LIPIDS NOTES BY BILAL MALIK
Definition: Castor oil is a fixed oil obtained from the seeds of ricinus
communis (Euphorbiaceae).
Geographical Sources: Native to India. Produced in Brazil, India, China,
Russia & Thailand.
BOTANICAL CHARACTERISTICS:
o Seeds show considerable difference in colour & size.
o They are oval, slightly compressed
o Colour: uniform grey, brown or black, mottled with brown or black.
o If grown in good conditions, they have very little odour & the taste is
slightly acrid.
o If the testa are broken, rancidity will develop.
CASTOR OIL: PREPARATION:
90% of the world’s castor oil is prepared in India & Brazil. Small amounts of
raw seeds are now exported.
Method of preparation: Seeds are removed from the testa. Kernels are cold-
pressed with a hydraulic press. Oil is then refined by steaming, filtration &
bleaching.
Cold-expression yields 33% of medicinal oil. Further amounts of lower quality
oil may be obtained by other methods
CASTOR OIL: CHARACTERISTICS:
Medicinal castor oil is a colourless or pale yellow liquid, with a slight odour &
faintly acrid taste.
Acid value: increases with age. If initially high – indicates the use of damaged
sees or careless extraction or storage.
Viscosity: Extremely high
CASTOR OIL: CONSTITUENTS:
Castor seeds contain 46-53 % fixed oil.
These fixed oils consist of the glycosides of
- Ricinoleic
- Isoricinoleic
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6. LIPIDS NOTES BY BILAL MALIK
- Steric
- Dihydroxystearic acids
The cake, after expression, contains extremely poisonous toxins (ricins)
CASTOR OIL: USES & ACTIONS:
Castor oil is used to treat constipation. It may also be used to clean out
the intestines before a bowel examination/surgery.
Castor oil is known as a stimulant laxative. It works by increasing the
movement of the intestines, helping the stool to come out.
Because of the ricin, the seeds have a much more violent action than
the oil and is not used as a purgative in the West.
ALMOND OIL:
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6. LIPIDS NOTES BY BILAL MALIK
Almond oil is the fixed oil obtained by expression from the seeds of
Prunus amygdalus (Roseceae)
Geographical Sources: Mediterranean countries: North Africa, France, Spain,
Italy.
Sweet and Bitter Almonds:
The sweet almond is 2–3 cm in length, rounded at one
end, and pointed at the other. The bitter almond is 1.5–2
cm in length but of similar breadth to the sweet almond.
Bitter almonds are sometimes found in samples of sweet almonds,
especially in those from N. Africa. Their presence may be detected the
sodium picrate test for cyanogenic glycosides.
ALMOND OIL: CONSTITUENTS:
Both varieties of almond contain 40–55% of fixed oil, about
20% of proteins, mucilage and emulsin.
Almond oil consists of a mixture of glycerides of oleic (62–86%), linoleic
(17%), palmitic (5%), myristic (1%), palmitoleic, margaric, stearic,
linolenic, arachidic, gadoleic, behenic and erucic acid. Bitter almond oil
contains benzaldehyde and 2–4% of hydrocyanic acid.,
and vitamins and antioxidants (mostly Vitamin E and Vitamin K).
Almond oil is a rich source of vitamin E.
Bitter almonds contain 2.5-4% cyanogenic glycoside, amygdalin.
ALMOND OIL: PRODUCTION & CHARACTERS:
Almond oils is produced by grinding the seeds & expressing them in a
canvas bag between slightly heated iron plates.
They are sometimes ground before expression .The oil is then clarified
by filtration.
Bitter almonds, after maceration on hydrolysis of amygdalin yield a
volatile oil that is used as a flavouring agent.
Oil is pale yellow liquid with a slight odour & bland, nutty taste.
ALMOND OIL: ACTIONS & USES:
‡ Hydrocyanic acid-free oil is used for flavouring purposes
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6. LIPIDS NOTES BY BILAL MALIK
‡ Almond oil is great for digestion, and can also prove to be an effective
laxative.
‡ as a vehicle for oily injection.
‡ Expressed almond oil is an emollient and an ingredient in
‡ Cosmetics.
‡ If applied directly, almond oil can often provide relief from muscular
pain[Applied to glandular swellings of the neck].
‡ Ingesting almond oil is also great for boosting the immune system, which
will in turn lessen chances of becoming ill.
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6. LIPIDS NOTES BY BILAL MALIK
During ripening, the fruits bury themselves in the sandy soil in which
the plants grow. Each fruit contains 1-3 red-brown seeds.
Fruits shelled by machine.
Kernels contain 40-50% fixed oil.
Because of the high oil content of the seeds, when crushed, it is
difficult to express. Therefore, after boiling, part of the oil is removed in
a low pressure expeller and the remaining cake is solvent extracted. The 2
oil fractions are then mixed together before undergoing purification.
ARACHIS OIL: CONSTITUENTS:
Glycosides of
- Oleic
- Linoleic
- Palmitic
- Arachidic
- Stearic
- Lignoceric
- And other acids
ARACHIS OIL: ACTIONS & USES:
Peanut oil is used to lower cholesterol and prevent heart disease.
It is also used to decrease appetite as an aid to weight loss. Some people
use it to help prevent cancer.
Peanut oil is sometimes applied directly to the skin for arthritis and joint
pain, dry skin and eczema.
Rectally, peanut oil is used in ointments and medicinal oils for treating
constipation.
Pharmaceutical companies use peanut oil in various products they prepare
for internal and external use.
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6. LIPIDS NOTES BY BILAL MALIK
LINSEED OIL:
LINSEED OIL:
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6. LIPIDS NOTES BY BILAL MALIK
Linseed oil is a yellow-brown oil with a characteristic odour & bland taste.
Extraction of linseed oil is done by hot expression of linseed seeds. The cake
is adjusted to leave in sufficient oil to make it suitable for cattle feed.
LINSEED OIL: CONSTITUENTS:
Linolenic acid
Linoleic acid
Oleic acid
Myristic
Stearic
Palmitic acids
182
6. LIPIDS NOTES BY BILAL MALIK
183
6. LIPIDS NOTES BY BILAL MALIK
THEOBROMA OIL:CONSTITUENTS:
2% Theobromine
40-60% solid fa
Mucilage
Glycerides of
- Stearic 34%
- Palmitic 25%
- Oleic 37%
- Arachidic and other acids
- Glyceride structure is responsible for nongreasiness of product.
It is the most expensive of all the fixed oils, and is commonly adulterated with
waxes, stearin, animal or vegetable tallows.
THEOBROMA OIL:CONSTANTS & USES:
Boiling point: 31-34 ºC. This makes it ideal for the use in the preparation
of suppositories.
It reduces the formation of stretch marks during pregnancy by keeping
the skin supple
It is used as an ingredient in cosmetic ointments and in pharmacy for
coating pills.
It has excellent emollient properties and is used to soften and protect
chapped hands and lips.
It is used as an ingredient in lotion bars, lip balms, body butters, soaps,
and belly balms for expectant mothers.
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6. LIPIDS NOTES BY BILAL MALIK
Diuretics .
COTTON-SEED OIL:
Botanical origin:
Gossypium herbaceum
Family: Malvaceae
Part used: Seeds
Geo Location:
Native to Asia and Africa. Now it is cultivated in Egypt, China, India, Turkey,
and southern US.
Collection:
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6. LIPIDS NOTES BY BILAL MALIK
Constituents:
Glycerides of;
• Linoleic acid
• Oleic acid
• Palmitic acid
• Stearic acid
• Arachidic acid
• Myristic acid
Uses:
Food
Emollient
Vehicle for injections
Preparation of hydrogenated vegetable oils
Soap manufacture
CORN OIL:
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6. LIPIDS NOTES BY BILAL MALIK
Botanical origin:
Zea mays
Family:
Gramineae
Part used:
Embryo
Production
Almost all corn oil is expeller pressed, then solvent extracted using
hexane. The solvent is evaporated from the corn oil, recovered, and re-
used.
After extraction, the corn oil is then refined by degumming and/or alkali
treatment, both of which remove phosphatides. Alkali treatment also
neutralizes free fatty acids and removes color (bleaching).
Final steps in refining include winterization (the removal of waxes), and
deodorization by steam distillation.
Constituents:
Glycerides of;
• Oleic acid
• Linoleic acid
• Stearic acid
• Arachidic acid
• Palmitic acid
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6. LIPIDS NOTES BY BILAL MALIK
• Myristic acid
• Lignoceric acid
Uses:
Vehicles in pharmaceutical and cosmetic preparation
Solvent for injections
Nutrient
COCONUT OIL:
Botanical origin:
Cocos nucifera
Family:
Palmae
Part used:
Dried solid part of Endosperm.
The tree rises upto height of 30 meters and bears 100 or more fruits
Production:
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6. LIPIDS NOTES BY BILAL MALIK
• Dry process
• Dry processing requires the meat to be extracted from the shell and dried
using fire, sunlight, or kilns to create copra.
• The copra is pressed or dissolved with solvents, producing the coconut
oil.
• A portion of the oil extracted from copra is lost to the process of
extraction.
Wet process
• The wet process uses raw coconut rather than dried copra, and the protein
in the coconut creates an emulsion of oil and water.
• The more critical step is breaking up the emulsion to recover the oil. This
is made by prolonged boiling, but this produces a discolored oil and is not
economical.
• Modern techniques use centrifuges and pre-treatments including cold,
heat, acids, salts etc or some combination of them
Constituents:
Glycerides of;
• Lauric acid
• Myristic acid
• Capric acid
• Caprylied acid
• Caproic acid
• Oleic acid
• Palmitic acid
• Stearic acid
Uses:
Nutrient
Confectionaries
Cosmetics
Ointment base
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MUSTARD OIL:
Botanical origin:
Brassica juncea
Family:
Cruciferae
Part used:
Seeds
• It is an annual plant with a much-branched stem, and lobed, roughly lyre-
shaped leaves, 16cm (6 in) long.
• Bright yellow flowers are produced in summer, followed by small, erect,
4-angled pods with dark brown seeds.
Extraction
• The seeds are to be dried in sun and then cleaned by shakers to remove
dust and foreign matter. The seeds are initially steamed and then passed
through the expeller and the process is repeated till the maximum oil is
extracted out of the seeds.
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6. LIPIDS NOTES BY BILAL MALIK
191
6. LIPIDS NOTES BY BILAL MALIK
Botanical origin:
Sesamum indicum
Family: Pedaliaceae
Part used: Seeds
Geo Location:
South Asia, Africa, West Indies, Southern US
• The plant is annual herb attaining a height of 1 meter.
• Seeds are small,flattend ,oval, shiny and whittish,yellowish or reddish.
• Fixed oil is obtained by expression.
• Oil is pale yellow, odourless and has bland taste
Constituents:
Glycerides of;
• Linoleic acid
• Oleic acid
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6. LIPIDS NOTES BY BILAL MALIK
• Stearic acid
• Palmitic acid
• Arachidic acid
And other components include;
• Sesamin
• sesamolin
Uses:
Solvent for intramuscular injection
Nutritive
Demulcent
Emollient
Laxative
SUNFLOWER OIL:
Botanical origin:
Helianthus annus
Family: Compositae
Part used: Seeds
Geo Location: Native to America. India Russia Argentina Ukraine
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6. LIPIDS NOTES BY BILAL MALIK
The name Helianthus, being derived from helios (the sun) and anthos (a
flower), has the same meaning as the English name Sunflower
it is an annual herb, with a rough, hairy stem, 3 to 12 feet high
The flower-heads are composed of many small tubular flowers arranged
compactly on a flattish disk
The oil pressed from the seeds is of a citron yellow colour and a sweet
taste
EXTRACTION:
For the extraction of the oil, the seeds are bruised, crushed and ground to
meal in a roller mill, under chilled iron or steel cylinders.
The mass, after being packed in bags, is placed in hydraulic presses,
under a pressure of 300 atmospheres or more, and allowed to remain
under pressure for about seven minutes. The oil thus obtained is known as
cold pressed oil.
Constituents:
Glycerides of;
• Palmitic acid
• Stearic acid
• Arachidic acid
• Oleic acid
• Linoleic acid
• Behenic acid
Uses:
Nutritive
Preparation of hydrogenated products
Sunflower oil is used for constipation and lowering “bad” LDL
cholesterol.
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WAXES:
“Wax” is sometimes used to describe hard paraffin (HC mixture), but it is best
confined to natural mixtures containing large amounts of esters derived from
higher monohydric alcohols of the methyl alcohol series combined with fatty
acids.
In this series the alcohols change from liquids to solids, become less soluble in
water & have higher melting points & MWs.
WAXES – EXAMPLES:
Vegetable products
(e.g. carnauba wax)
Animal products
e.g. beeswax & wool-fat.
Waxes are abundant in nature (epidermal surfaces) – but only a limited number
have commercial significance.
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6. LIPIDS NOTES BY BILAL MALIK
FATS VS WAXES:
Fats may be saponified by either aqueous or alcoholic alkali, but waxes are only
saponified by alcoholic alkali.
This is used to determine if fats were added to adulterate waxes.
WAXES – COMPOSITION:
Fats consists almost entirely of esters.
Waxes: esters (palmitate type), free acids, HC’s, free alcohols & sterols.
Acid values of waxes also tend to be higher than those of fats.
WOOL FAT:
DEFINITION: Wool fat (anhydrous lanolin) is a purified fat-like substance
prepared from the wool of the sheep, Ovis aries (Bovidae).
WOOL FAT: PREPARATION:
Raw wool contains considerable quantities of ‘wool grease’ or crude lanolin, the
potassium salts of fatty acids & earthy matter.
Raw lanolin is separated by ‘cracking’ with sulphuric acid & purified to be fit
for medicinal use. Purification may be done by centrifuging with water & by
bleaching.
WOOL FAT: CHARACTERS:
Wool fat is a pale yellow, tenacious substance with a faint but characteristic
odour.
It is insoluble in water.
Melting point: 36-42ºC
Soluble: in ether & chloroform.
Like other waxes, it is not readily saponified by aqueous alkali, but with a
alcoholic solution of alkali.
Saponification value: 90 – 105.
Iodine value: 18 – 32.
Acid value: not more than 1
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6. LIPIDS NOTES BY BILAL MALIK
BEESWAX:
DEFINITION: Beeswax is obtained by melting and purifying the honeycomb
of Apis mellifica and other bees.
Zoological origin:
Apis mellifera
Apis dosarta
Apis cerana
Apis indica
Apis florea
Family:
Apidae
Source:
Bee hives
GEOGRAPHICAL SOURCES: West Indies, California, Chile, Africa,
Madagascar & India.
Separate monographs exist for yellow and white beeswax.
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6. LIPIDS NOTES BY BILAL MALIK
Production:
Worker bees have eight wax-producing mirror glands. The size of these
wax glands depends on the age of the worker and after daily flights begin
these glands gradually atrophy. The new wax scales are initially glass-
clear and colorless becoming opaque afterwards.
The wax of honeycomb is nearly white, but becomes progressively more
yellow or brown by incorporation of pollen oils and propolis.
BEESWAX: PREPARATION:
Wax is secreted by worker bees in cells on the ventral surface of the last 4
segments of their abdomen. The wax passes out through pores in the chitinous
plates of the sternum & is used, particularly by the young workers, to form the
comb.
Honey bees use the beeswax to build honeycomb cells In which their young are
raised and honey and pollen Are stored.
For the wax-making bees to secrete wax, the
ambient temperature in the hive has to be 33 to 36°C
(91 to 97 °F).
To produce their wax, bees must consume about eight times as much honey by
mass.
When beekeeper extract the honey, they cut off the wax caps from each
honeycomb cell with an
uncapping knife or machine.
The wax may further be clarified by heating in water.
PREPARTION OF
YELLOW BEESWAX:
Yellow beeswax is prepared, after removal of the honey, by melting the comb
under water. This causes solid impurities to sink to the bottom while any
residual honey is dissolved). This is then strained and the wax is allowed to
solidify in suitable moulds.
PREPARATION OF WHITE BEESWAX:
White beeswax is prepared from yellow beeswax which is treated with charcoal,
potassium permangante, chromic acid, or chlorine, by the slow bleaching action
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6. LIPIDS NOTES BY BILAL MALIK
of light, air & moisture. In this method the melted wax is allowed to fall on a
revolving cylinder which is kept moist. This then slowly becomes bleached.
This is then repeated at least one more time. The wax is finally cast into circular
cakes.
BEESWAX: CHARACTERS:
Beeswax is a yellow-brown or yellow-white solid.
It breaks with a granular fracture & has a characteristic odour.
It is insoluble in water & slightly soluble in cold alcohol, but dissolves in
chloroform and also in warm fixed & volatile oils.
BEESWAX: CONSTITUENTS:
Beeswax is a true wax:
Beeswax is a tough wax formed from a mixture of
several compounds.
Consists of 80% myricin
(myricyl palmitate)
Contains a little myricyl stearate.
Free cerotic acid
Aromatic substances
Applications:
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6. LIPIDS NOTES BY BILAL MALIK
BEESWAX: ADULTERANTS:
Japan wax: not a true wax, but a fat (may be saponified by means of boiling
aqueous sodium hydroxide – waxes are unaffected by aqueous alkali).
Japan wax is prepared from the fruits of Rhus (Anacardiaceae).
BEESWAX: USES:
Beeswax is used for the preparation of plasters, ointments and polishes.
COOKING OILS:
Do not use fresh, unrefined, mechanically pressed, light & oxygen protected
EFA-rich seed oils for cooking.
Labels: “Cholesterol Free”.
Opened bottles should be kept in the fridge & used with 3-6 weeks. Olive oil
can keep well for up to 2 years.
NB: Cooking method influences the type of oil you use.
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6. LIPIDS NOTES BY BILAL MALIK
LENOLIN:
Lanolin is also called wool wax or wool grease. It is a yellow waxy substance
secreted by the sebaceous glands of wool bearing animals. Most lanolin used by
humans comes from domestic sheep.
Constituents:
A typical high purity grade of lanolin is
composed predominantly of;
Long chain waxy esters
lanolin alcohols
lanolin acids
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6. LIPIDS NOTES BY BILAL MALIK
lanolin hydrocarbons
It has been estimated that there may be between 8,000 and 20,000 different
types of lanolin ester present in lanolin .
Production:
o Lanolin is extracted by washing the wool in hot water with a special wool
scouring detergent to remove dirt, wool grease (crude lanolin), suint
(sweat salts), and anything else stuck to the wool.
o The wool grease is continuously removed during this washing process
by centrifugal separators, which concentrate the wool grease into a wax-
like substance melting at approximately 38 °C (100 °F).
Applications:
Lanolin and its many derivatives are used extensively in high value
cosmetics, facial cosmetics, lip products etc
Lanolin is used commercially in many industrial products ranging
from rust-proof coatings to lubricants.
Lanolin is often used as a raw material for producing cholecalciferol
(vitamin D3).
Anhydrous lanolin is also used as a lubricant for brass instrument tuning
slides.
Lanolin can also be restored to woolen garments to make them water and
dirt repellent.
JOJOBA OIL:
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6. LIPIDS NOTES BY BILAL MALIK
Botanical origin:
Simmondsia chinensis
Family:
Simmondsiaceae
Part used:
seeds
Constituents:
This oil is rare in that it is an extremely long
(C36-C46) straight-chain wax ester
Uses:
In cosmetics as a moisturizer
As a carrier oil for specialty fragrances
Bio-diesel fuel for cars and trucks
Biodegradable lubricant.
SPERMACETI:
Source:
Spermaceti is a wax present in the head cavities of the whale i.e. Physeter
macrocephalus.
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6. LIPIDS NOTES BY BILAL MALIK
Extraction:
Spermaceti is extracted from oil by
crystallization at 6 °C. When treated by pressure and
a chemical solution of caustic alkali, spermaceti
forms brilliant white crystals that are hard but oily to
the touch, and are devoid of taste or smell.
Uses:
Ingredient in cosmetics
Leather working
Lubricants
Making of candles
Dressing of fabrics
Pharmaceutical excipient (in ointments)
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6. LIPIDS NOTES BY BILAL MALIK
CARNAUBA WAX:
Botanical origin:
Copernicia cerifera
Copernicia prunifera
Family:
Arecaceae
Part used:
Leaves
Constituents:
Carnauba consists mostly of;
Aliphatic esters
Diesters of 4-hydroxycinnamic acid
ω-hydroxycarboxylic acids
Fatty acid alcohols
Methoxy cinnamic acid
Uses:
Automobile waxes
Shoe polishes
Dental floss
Food products such as sweets,
Floor and furniture waxes and polishes
Use for paper coatings
Emollient
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7. VOLATILE OILS NOTES BY BILAL MALIK
VOLATILE OILS
Volatile or essential oils, as their name implies. are volatile in steam
They differ entirely in both chemical and physical properties from
fixed oils. With the exception of oils such as oil of bitter almonds
which are produced by the hydrolysis of glycosides.
these oils are contained largely as such in the plant.
They are secreted in oil cells. In secretion ducts or cavities or in
glandular hairs.
They are frequently associated with other substances such as gums and
resins and themselves tend to resinify on exposure to air.
Volatile oils are sweet-smelling liquids, and they emit fragrance to the
food and are also slight bitter in taste. Thus, they help to enhance the
secretion of digestive enzyme in the alimentary tract
Volatile oils, when fresh, are colourless liquids. A few are crystalline or
amorphous solid.
On long standing, they become darker in colour, especially when exposed
to air and direct sunlight.
Volatile oil should, therefore, be stored in tightly closed amber-coloured
bottles in a cool, dry place.
Volatile oils are slightly soluble in water but are readily soluble in ether,
alcohol and most of organic solvents.
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7. VOLATILE OILS NOTES BY BILAL MALIK
CLASSIFICATION:
(a) Hydrocarbon volatile oils: Cubeb and Turpentine oil.
(b) Alcoholic volatile oils: Peppermint, Coriander and Cardamom.
(c) Aldehydic volatile oils: Bitter orange peel, Sweet orange peel, Lemon
Cinnamon and Bitter almond oil
(d) Ketonic volatile oils: Camphor, Spearmint, Caraway, Buchu
(e) Phenolic volatile oils: Clove, Thyme.
(f) Phenolic ether volatile oils: Fennel, Anise, Myristica.
(g) Oxide volatile oils: Eucalyptus, Chenopodium.
(h) Ester volatile oils: Rosemary.
(i) Miscellaneous volatile oils: Allium, Anethum.
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7. VOLATILE OILS NOTES BY BILAL MALIK
Constituents:
Volatile oil (10 - 18 %)
Resins
Amorphous cubebic acid
Colourless crystalline cubebin.
By extraction with ether yields oleo-resin (22%).
USES OF CUBEB:
Stimulant, carminative, aphrodisiac much used as a remedy for
gonorrhoea, after the first active inflammatory symptoms have subsided;
also used in leucorrhoea(Leucorrhoea: is a thick, whitish or yellowish vaginal
discharge. There are many causes of Leukorrhea, the usual one being estrogen
imbalance.), cystitis, urethritis, abscesses(An abscess (Latin: abscessus) is a
collection of pus that has built up within the tissue of the body. Signs and
symptoms of abscesses include redness, pain, warmth, and swelling. The
swelling may feel fluid filled when pressed) of the prostate gland, piles and
chronic bronchitis.
Cubeb was frequently used in the form of cigarettes for asthma, chronic
pharyngitis and hay fever
CUBEB OIL:
About 15% of a volatile oil is obtained by distilling cubebs with water
Monoterpenes:
• Sabinene 50%
• α-thujene
• Carene
Sesquiterpenes
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7. VOLATILE OILS NOTES BY BILAL MALIK
• Caryophyllene
• Copaene
• α- and β-Cubebene
• δ-Cadinene
• Germacrene
Oxides 1,4- and 1,8-cineole and the alcohol cubebol.
CUBEB OIL – USES:
Cubeb essential oil is pungent, slightly camphorous, with a touch of nutmeg. It
has
Stimulant,
Expectorant,
Carminative,
Antiseptic, and
Diuretic properties
COLLECTION:
• Pinus oleoresin is a normal i.e. physiological product of pine. The amount
produced is generally enhanced by injury or by treatment with 50%
H2SO4. It is secreted in plant tissues in specific cavities or resin ducts.
The cavities are themselves formed either in a schizogenous or lysigenous
fashion.
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7. VOLATILE OILS NOTES BY BILAL MALIK
i) EUCALYPTUS LEAF:
DEFINTION:
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7. VOLATILE OILS NOTES BY BILAL MALIK
Eucalyptus leaf consists of the whole or cut dried leaves of the older
branches of Eucalyptus globulus, (Myrtaceae).
GEOGRAPHICAL SOURCES
Portugal, Spain, China, Brazil, Australia, India, Pakistan & Paraguay.
Eucalyptus – DESCRIPTION:
MACROSCOPICAL
• Older dried leaves are grey-brown & have lateral veins.
• Secretory oil cells are visible in leaves held to the light.
MICROSCOPIC
• Epidermal cells have a thick cuticle.
• Mesophyll has schizogenous oil glands
• Calcium oxalate crystals.
EUCALYPTUS OIL:
Eucalyptus oil is the volatile oil obtained by the distillation of the fresh leaves
of Eucalyptus globulus and other species of Eucalyptus,
It is rectified, if necessary. It should contain not less than 65% of cineole.
Only a certain amount of species produce oil suitable for medicinal use – the
main criteria is a high cineole content and low amounts of phellandrene and
aldehydes.
CHARACTERISTICS:
Colourless or pale yellow liquid.
Aromatic & camphoraceous in odour.
Pungent & camphoraceous in taste, which is followed by a sensation of
cold.
It is soluble in 90% alcohol, fixed oils, fats and in paraffin and insoluble
in water.
CONSTITUENTS:
• At least 70 volatile oils: Chiefly contains cineole, also known as
eucalyptol (about 80%). Cineol (or eucalyptol) is by far the most
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7. VOLATILE OILS NOTES BY BILAL MALIK
important member of the family and virtually exists in a class of its own.
It is anesthetic, antiseptic, and works as an expectorant.
It also contains:
Pinene
Camphene
Traces of Phellandrene
Citronellal
Geranyl acetate
EUCALYPTUS OIL – USES:
Decreasing the symptoms of
nasopharyngeal infections
Treating coughs
Chronic bronchitis
Decongestant
Counter-irritant
Antiseptic
Expectorant
Official preparations
Mixtures, inhalations, Nasal Drops, lozenges; also applied externally as
ointments and liniments.
ii)CHENOPODIUM OIL:
DEFINTION: Chenopodium oil is a volatile oil obtained by steam distillation
from the fresh flowering and fruiting plants (except roots) of Chenopodium
ambrosioldes; var. anthelminticum Linn., Family: Chenopodiaceae
GEOGRAPHICAL SOURCES
Eastern and Central U.S.A, Caribbean islands, Europe, Maryland, Mexico,
Canada, India and Pakistan
Description:
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7. VOLATILE OILS NOTES BY BILAL MALIK
Uses:
• Use as anthelmintic
• Specifically for round-worms (Ascaris).
• Used to expel hook-worms and dwarf tape-worms.
• It has no action on large tape-worms.
• Used against intestinal amoebae and in veterinary practice.
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7. VOLATILE OILS NOTES BY BILAL MALIK
i)CLOVE:
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7. VOLATILE OILS NOTES BY BILAL MALIK
The flower buds are collected when the lower part turns green-crimson. The
cloves are dried in the open air on mats & separated from their peduncles
(forming clove stalks which are also sold commercially).
If left on the tree for too long, the buds open & the petals fall, leaving “brown
cloves”. Later the fruits (“mother cloves”) are produced.
MACROSCOPICAL FEATURES:
Cloves are 10-17.5 mm long.
The head consists of 4 slightly projecting calyx teeth, 4 membranous petals and
numerous incurved stamens around a large style.
Odour: Spicy & Pungent
Taste: Aromatic
MICROSCOPICAL FEATURES:
Heavy cuticularized epidermis
Numerous oil cells (shizolysigenous)
Calcium oxalates (cluster crystals & prisms)
Stomata (epidermis of sepals)
Starch (Fruit – “mother cloves”)
CONSTITUENTS:
14-21% Volatile oils
• Mainly eugenol & isoeugenol
• Sitosterol
• Stigmasterol
• Campesterol
Tannins
Triterpene acids & esters
Glycosides
USES OF CLOVE:
Stimulant aromatic
Spice
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7. VOLATILE OILS NOTES BY BILAL MALIK
It is an ancient herb used in medicine by the Greeks, the Egyptians and the
Romans.
Evergreen perennial shrub that grows up to 45 cm (18 inches) high
Woody root system
Much-branched stem
Small elliptical greenish gray aromatic leaves upto 12mm in length and
opposite.
leaves are almost stalkless with margins curved inwards and highly aromatic
Pale purple or white flowers
ACTIVE CONSTITUENTS:
The main chemical components are:
Thymol
Carvacrol
Linalol
Borneol
Camphene
α -thujone
α –pinene
β-pinene
p-cymene
α -terpinene
β-caryophyllene
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7. VOLATILE OILS NOTES BY BILAL MALIK
Other Constituents:
Flavonoids: Flavonone and Dihydroflavonals
Biphenyls, Rosmarinic acid, Tannins, Resins, Triterpenes
Thyme Oil:
• Thyme oil is extracted by hydro- distillation method
• It has a rather sweet, yet strongly herbal smell and is reddish-brown to
amber
• It is extracted from the fresh or partly dried flowering tops and leaves of
the plant by water or steam distillation and the yield is 0.7 -1.2 %.
ACTIONS & USES:
Culinary uses:
• Flavouring agent
(to flavour meats, soups, Lamb)
Medicinal use:
• The main component of the essential oil of thyme, thymol, is active
against Salmonella and Staphylococcus bacteria. the antiseptic tonic
properties of thyme make it a useful tonic for the immune system in
chronic, especially fungal, infections as well as an effective remedy for
chest infections such as bronchitis, whooping cough, and pleurisy.
Therapeutic properties of thyme oil:
• antirheumatic, antiseptic, antispasmodic, bactericidal, bechic,
carminative, diuretic, expectorant, insecticide, stimulant, tonic and
vermifuge
• Industrial :
• Industrial The essential oil of thyme is used to preserve processed meat
and butter, and in making chewing gum, ice cream, candy, and the liqueur
Benedictine. Thymol is active ingredient in mouthwashes (Listerine)
• COSMETIC :
• COSMETIC it is used for skin problems such as oily skin, sciatica, acne,
dermatitis, eczema and insect bites
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7. VOLATILE OILS NOTES BY BILAL MALIK
DEFINITION:
Rosemary consists of dried Stems, leaves and flowers of Rosmarinus
officinalis (also known as Rosmarinus coronarium) of the Labiatae
Most sources interpret the Latin name as rosmarinus“ dew of the sea”.
GEOGRAPHICAL SOURCES:
Native to the Mediterranean regions, southern Europe, South Africa, India and
Pakistan
MACROSCOPICAL FEATURES:
Stem
Rosemary is an evergreen, shrubby herb that grows to a height of 1 to 2 m, with
a unique aromatic odour and a camphoraceous undertone. The erect stems are
divided into numerous long, slender branches that have ash-coloured and scaly
bark.
Leaves
The branches bear opposite, leathery thick leaves which are lustrous,
linear, dark green above and grey somewhat wooly below.
Flower
The flowers are small and pale blue to deep blue. Much of the volatile essential
oils reside in their calyces.
Rosmary Constituents:
Hydroxy-cinnamic acid [antioxidant in various oxidative stress induced
disorders]
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7. VOLATILE OILS NOTES BY BILAL MALIK
Rosmanol
Epi-rosmanol
Rosmarinic acid
Carnosic acid
Carnosol
α and β amyrin
Ursolic acid
Oleanolic acid
Rosemary Oil:
• Rosemary oil is extracted from the fresh flowering tops by steam
distillation. It yields 1.0 - 2.0 %.
Description:
Rosemary oil is colorless to pale yellow
It has a powerful aromatic refreshing herbal smell,
It is clear in color
and watery in viscosity
Rosemary Oil – CONSTITUENTS:
• It contains 0.8-6 % of Esters and 8-20 % of alcohols. The main chemical
components of rosemary oil are:
• α –pinene [induced apoptosis in cancer cells]
• Borneol [alleviates mechanical hyperalgesia in models of chronic
inflammatory and neuropathic pain in mice]
• β -pinene
• Camphor
• Bornyl acetate
• Camphene [induces intrinsic apoptosis in melanoma cells and displays
antitumor activity in vivo].
• 1,8-cineole [1,8-cineole acts as a P450 inhibitor-like compound,
improving the toxicity of other xenobiotics]
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7. VOLATILE OILS NOTES BY BILAL MALIK
• limonene.
• https://www.youtube.com/watch?v=uuIxH0bS0Hw
ROSEMARY OIL USES:
COSMETIC
Rosemary acts on the hair follicles by stimulating growth and acts against
dandruff.
It is used in preparations for acne and dermatitis.
Rosemary is also one of the ingredients used in the preparation of eau de
cologne.
It is added to liniments as a fragrant stimulant.
ROSEMARY OIL USES:
PHARMACEUTICAL AND THERAPEUTIC
Rosemary oil has a pronounced action on the brain as it clears the mind
and aids the memory. It is an external stimulant and a relaxant for
nervousness, muscle spasms, headaches, migraines, neuralgia, mental
fatigue and nervous exhaustion.
The antiseptic action of rosemary oil is especially suitable for intestinal
infections and diarrhoea, and it also eases colitis, dyspepsia, flatulence,
hepatic disorders and jaundice.
On the respiratory system rosemary oil is effective for asthma,
bronchitis and whooping cough. It may ease congestion, puffiness and
swelling and also may improve acne, dermatitis and eczema.
Diuretic
Its stimulating action may benefit scalp disorders and encourage hair
growth.
Rosemary has been used as a folk remedy against rheumatism, and
treating of wounds.
It has been used in the treatment of cancer and as a tonic to the kidneys.
FOOD AND FLAVOURING
223
7. VOLATILE OILS NOTES BY BILAL MALIK
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7. VOLATILE OILS NOTES BY BILAL MALIK
The cultivation of the drug is done by sowing the fruits. It needs sandy loam
soil, devoid of gravels, with slightly acidic nature.
It is a cold weather crop and is grown during rabi season. Its sowing is done in
October and the crop is harvested in March/April.
The umbels are collected after full maturity, dried thoroughly and shaken to
separate the fruits.
Fruits removed and then packed into the bags are sieved, excess of foreign
organic matter is removed and then packed into the bags.
MACROSCOPICAL FEATURES:
The fruits are yellowish or pale brown with narrow wings.
Odour and Taste: Aromatic and characteristic
Size: The fruits are about 4 mm in length, 2 to 3 mm in width and 1 mm in
thickness.
Shape: Broadly ovate, strongly compressed dorsally. The fruits are found in the
form of mericarps usually separated and free from pedicel.
Each mericarp is yellow in colour, lateral rides of mericarp are extended as
wings.
ANETHUM- DILL OIL:
Extraction
• Dill oil is extracted by steam distillation, mainly from the seeds, or the
whole herb, fresh or partly dried.
Oil properties
• Dill oil has a grass-like smell and colorless or pale yellow liquid with a
watery viscosity.
ACTIVE CONSTITUENTS:
Volatile oil (2.4 – 4.0%):
The chief constituent of the volatile oil is aromatic liquid, known as carvone (43
to 63%).
It also contains:
Dihydrocarvone,
D-limonene,
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7. VOLATILE OILS NOTES BY BILAL MALIK
ii) Garlic:
DEFINITION: consist of dried ripe bulb of Allium sativum Linn. Family:
Liliaceae
{The name is of Anglo-Saxon origin, being derived from gar (a spear) and lac
(a plant), in reference to the shape of its leaves}
GEOGRAPHICAL SOURCES
Garlic occurs in central Asia, southern Europe and USA. It is widely cultivated
in India and Pakistan.
Cultivation:
• Divide the bulbs into their component 'cloves' - each bulb will divide into
eight or fifteen cloves and with a dibber put in the cloves separately,
about 2 inches deep and about 6 inches apart, leaving about 1 foot
between the rows.
• When planted early in the spring, in February or March, the bulbs should
be ready for lifting in August, when the leaves will be beginning to witer.
• Should the summer have been wet and cold, they may probably not be
ready till nearly the middle of September.
Morphology:
• Garlic is a bulbous perennial herb, closely related to the onion.
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7. VOLATILE OILS NOTES BY BILAL MALIK
• It has a tall, erect flowering stem that reaches 2-3 feet in height.
• The plant has pink or purple flowers that bloom in mid to late summer.
• It is a perennial herb having bulbs (the only part eaten) that is of a
compound nature, consisting of numerous (8-15) bulblets, known
technically as 'cloves,' grouped together between the membraneous scales
and enclosed within a whitish skin, which holds them as in a sac.
• Outer surface of each clove is convex while the inner one is concave.
• The flowers are placed at the end of a stalk rising direct from the bulb and
are whitish, grouped together in a globular head, with an enclosing kind
of leaf or spathae, and among them are small bulbils.
• Odour: When crushed gives odour that is because of allicin.
Constituents:
• The potentially active chemical constituents reported are
• Sulfur compounds: aliin, allicin, ajoene, allylpropyl disulfide, diallyl
trisulfide, sallylcysteine, vinyldithiines, S-allylmercaptocystein, and
others
• Enzymes: allinase, peroxidases, myrosinase, and others
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7. VOLATILE OILS NOTES BY BILAL MALIK
228
8)RESINS NOTES BY BILAL MALIK
Resins:
Introduction:
• Resins are amorphous solid or semisolid substances that are invariably
water insoluble but mostly soluble in alcohol or other organic solvents.
• Physically they are found to be hard, translucent or transparent and
fusible i.e., upon heating they first get softened and ultimately melt.
• Chemically, they are complex mixtures of allied substances, such as:
resin acids, resin alcohols (resinols), resino-tannols, resin esters and
gluco-resins.
• Thus, Resins as amorphous products having an inherent complex
chemical entity.
• Resins are normally produced either in schizogenous ducts or in cavities
and are regarded as the end products of metabolism.
• They are electrically non-conductive and combustible in nature.
Oleoresins:
• Oleoresins are homogenous mixtures of resins and volatile oils.
• These are the vegetative (asexual) secretions obtained as natural products
and composed of resin dissolved in essential oils.
Distribution of Resins in Plants:
• The resins and resinous substances are more or less extensively
distributed throughout the entire plant kingdom, specifically the
Spermatophyta i.e., the seed plants.
• Notably, their presence is almost rare and practically negligible in the
Pteridophyta i.e., the ferns and their allies.
• However, the resins have not been reported in the Thallophyta i.e., the
sea-weeds, fungi etc.
• These findings and observations lead to the fact the resins are the overall
and net result of metabolism in the higher plants,
• since the majority of them belong to the phyllum Angiosperum i.e., seed-
enclosed flowering plants, and Gymnosperm i.e., naked-seed non-
flowering plants.
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8)RESINS NOTES BY BILAL MALIK
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8)RESINS NOTES BY BILAL MALIK
5. On being heated in the air i.e., in the presence of oxygen, resins usually
burn readily with a smoky flame by virtue of the presence of a large
number of C-atoms in their structure.
6. On being heated in a closed container i.e., in the absence of oxygen,
they undergo decomposition and very often give rise to empyreumatic
products i.e., products chiefly comprising of hydrocarbons.
7. Resins are bad conductors of electricity, but when rubbed usually
become negatively charged.
8. They are practically insoluble in water, but frequently soluble in
ethanol, volatile oils, fixed oils, chloral hydrate and non-polar organic
solvents e.g., benzene, n-hexane and petroleum ether.
Chemical Properties of Resins:
1. Resins, in general, are enriched with carbon, deprived of nitrogen and
contain a few oxygen in their respective molecules.
2. Majority of them undergo slow atmospheric oxidation.
3. Resins are found to be a mixture of numerous compounds rather than a
single pure chemical entity.
4. Their chemical properties are exclusively based upon the functional
groups present in these substances.
5. Consequently, the resins are broadly divided into resin alcohols, resin
acids, resin esters, glycosidal resins and resenes (i.e., inert neutral
compounds).
6. It is also believed that resins are nothing but oxidative products of
terpenes.
7. They may also be regarded as the end-products of destructive
metabolism.
8. The acidic resins when treated with alkaline solutions they yield soaps
(or resin-soaps).
Preparation of Resins:
No general method has either been suggested or proposed for the
preparation of resins. In fact, there are two categories of resinous
products, namely:
(a) Natural Resins
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8)RESINS NOTES BY BILAL MALIK
a) Natural Resins:
These resins usually formed as the exudates from various plants obtained
either normally or as a result of pathogenic conditions.
These are also obtained by causing deep incisions or cuts in the trunk of
the plant.
They may also be procured by hammering and scorching, such as:
balsam of Peru.
Prepared Resins:
The resins obtained are by different methods:
(i) The crude drug containing resins is powdered and extracted with
ethanol several times till complete exhaustion takes place.
The combined alcoholic extract is either, evaporated on a electric water-
bath slowly or poured slowly into cold distilled water.
The precipitated resin is collected, washed with cold water and dried
carefully under shade or in a vacuum desiccator,
Examples: Podophyllum; Scammony and Jalap.
(ii) In the case of alco-resins, organic solvents with lower boiling points
are normally employed e.g., solvent ether (bp 37°C), acetone (bp 56.5°C)
for their extraction.
(iii) In the instance of gum-resins, the resin is extracted with 95% (v/v)
ethanol.
• https://www.youtube.com/watch?v=PXOLSuB79yE
Chemical Composition of Resins:
The constituents of resins may be classified as
(i) Resin Acids
e.g. Colophony and Copaiba.
(ii) Resin Esters and their Decomposition Products
e.g. Asafoetida, Benzoin, Balsam of Peru and Tolu.
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8)RESINS NOTES BY BILAL MALIK
(iii) Resenes
e.g. Mastic, Myrrh, Olibanum.
Classification of Resins:
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8)RESINS NOTES BY BILAL MALIK
Colophony:
Synonym: Rosin
Biological Source:
It is the residue left after distilling off the volatile oil from the oleoresin
obtained from Pinus palustris and other species of Pinus belonging to family
Pinaceae.
Generally, it is offered as wood rosin obtained from exudate from incisions
in the living tree , P. palustris and finally from tall oil rosin.
It is chiefly produced in the USA.
https://www.youtube.com/watch?v=Nu-FEad49P8
Characteristic Features:
Fuses gradually at 100°C and at a higher temperature it burns with a
smoky flame, while leaving not more than 0.1% of ash as a residue.
The alcoholic solution of colophony turns into milky-white on addition
of water.
It is a pale yellow to amber, translucent fragments, brittle fracture at
ordinary temperature.
https://www.youtube.com/watch?v=qTAJNmTV-_E
It has turpentine-like odour and taste.
Its acid number is not less than 150.
It is almost insoluble in water, but freely soluble in ethanol, benzene,
ether, glacial acetic acid and oils.
Chemical Tests
1. Dissolve 0.1 g of powdered colophony resin in 10 ml of acetic
anhydride, add one drop of sulphuric acid and shake well. The
appearance of a purple colour which rapidly changes to violet colour.
Chemical Constituents:
1. Colophony contains 90% resin acids known as abietic acid. The
remaining 10% as resene-an inert substance and esters of fatty acids.
2. It also contains a mixture of dihydroabietic acid and dehydroabietic
acid.
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8)RESINS NOTES BY BILAL MALIK
Podophyllum:
• Synonyms: Podophyllum resin, May apple, Mandrakes Root, Indian
apple, Vegetable calomel.
• Biological Sources:
Podophyllum is the dried rhizomes and roots of Podophyllum peltatum.
• Family: Berberidaceae
Preparation:
• Extract powdered podophyllum (1kg) by means of slow percolation until
it is almost exhausted of its resin content, using ethanol as the
menstruum.
• Carefully concentrate the percolate by evaporation until the residue
attains the consistency of a thin syrup.
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• Pour the resulting syrupy liquid with constant stirring into 1 L of distilled
water containing 10 ml of concentrated HCl and previously cooled to a
temperature less than 10°C.
• Allow the precipitate to settle down completely, decant the clean
supernatant liquid and wash the precipitate with cold distilled water
slowly, dry the resin and powder it.
Characteristic Features:
• It is a light brown to greenish-yellow powder, or small, yellowish, bulky,
fragile lumps usually becoming darker in shade on exposure to either heat
or light.
• It has a characteristic faint odour and a bitter acrid taste.
• It is freely soluble in ethanol, it is also soluble in dilute alkaline solution.
Chemical Constituents:
• Podophyllum contains 3.5 to 6% of resin. The most important ones
present in the podophyllum resin are podophyllotoxin (20% in American
Podophyllum) and almost up to 40% in Indian Podophyllum.
• Besides, it also contains α-peltatin (10%) and β-peltatin (5%).
• The resin also comprise of the closely related dimethylpodophyllotoxin
and its glycoside; and dehydropodophyllotoxin, as well as quercetin-a
tetra-hydroxy flavonol.
Uses:
• 1. Peltatin has shown antiviral activity
• 2. It is used as a slow-acting purgative.
• 3. Podophyllotoxin possesses anti-tumour properties and may be used in
the treatment of cancer.
• 4. It is invariably prescribed with other purgatives, henbane or belladonna
to prevent griping in infants.
Cannabis:
Synonyms:
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(–)-Δ9-trans-tetra-hydrocannabinol
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Chemical Constituents:
• Besides, the resin contains several active constituents, such as:
cannabinol, cannin, cannabol, tetrahydrocannabinol, cannabigerol,
cannabichromene and Δ8-tetrahydrocannabinol.
• It also contains choline, volatile oil and trigonelline.
• Indian Hemp seeds contain 20% of fixed oil.
Uses
• It has been used as a sedative in equine [relating to or affecting horses
or other members of the horse family]colic.
Uses of Cannabis
• 1.Used to reduce nausea and vomiting during chemotherapy
• 2. To improve appetite in people with HIV/AIDS, and to treat chronic
pain and muscle spasms.
• 3.Its use for other medical applications, however, is insufficient for
conclusions about safety or efficacy
• Common side effects include dizziness, feeling tired, vomiting, and
hallucinations
Turpentine:
• Synonym: Gum turpentine
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Myrrh:
• Synonyms:
Gum Myrrh, Myrrha.
• Biological Source:
Myrrh is an oleo-gum-resin obtained from the stem and branches of
Commiphora obyssinica or from other species of Commiphora
belonging to family Burseraceae.
https://www.youtube.com/watch?v=u9fQdXOnB7Y
https://www.youtube.com/watch?v=EFFUNRSxjVw
Preparation:
• The plants usually exude yellow coloured resin after proper incisions are
made in the bark of a tree.
It gradually hardens and becomes dark or reddish-brown in appearance.
The mass is collected by the native tribals of Somalia for trading.
Characteristic Features:
• Myrrh normally occurs either in the form of isolated irregular, rounded
tears of 2.5 cm in diameter or as masses duly formed by the
agglomeration of these tears.
• The tears are dull, rough and reddish-brown in appearance.
• It has a strong aromatic odour and possesses an acrid, bitter taste.
Chemical Constituents:
Myrrh contains volatile oil (7-17%), resin (20-25%), gum (57-61%), and
bitter principle (3 to 4%).
The resin is found to consist of a mixture of α-, β-, and γ-commiphoric acids
(resin acids).
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Uses:
• 1. It is used chiefly in perfumes and incense.
• 2. It is frequently employed as an antiseptic and stimulant.
• 3. Myrrh acts as an astringent to the mucous membrane and hence it find
its application in oral hygiene formulations, such as: gargles, mouth-
washes.
• 4. It is also used as a carminative.
• Chemopreventive effects of myrrh (Commiphora molmol) in
hepatocarcinogenic rats.
• In vitro cytotoxic and anti-inflammatory effects of myrrh oil
• It inhibit Oxidative stress and immunotoxic effects of lead.
• Resin is widely used in Asia as a cholesterol-lowering agent based on
Indian Ayurvedic medicine
Asafoetida:
• Synonyms
Asafetida; Asant; Devil's dung; Food of the Gods; Gum Asafoetida.
• Biological Sources
Asafoetida the oleo-gum-resin is obtained as an exudation of the
decapitated rhizome on roots of Ferula assafoetida ; Ferula foetida and some
other species of Ferula, belonging to the nature order Umbelliferae.
Preparation:
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Balsams:
• Balsams are the resinous mixtures that essentially contain large quantum
of benzoic acid, cinnamic acid or both, or esters of these organic aromatic
acids.
• Naturally occurring balsams
Storax
Peruvain Balsam
Tolu Balsam
Benzoin
https://www.youtube.com/watch?v=ZeZkE3337CM
Storax:
Synonyms
Styrax; Sweet oriental gum; Levant Storax
Biological Source
Storax is the balsam obtained from the trunk of Liquid amber orientalis
belonging to the natural order Hamamelidaceae.
Preparation
The storax is a pathological product formed as a result of injury
caused to the plant. It generally, exudes into the natural cavities between the
bark and the wood. The crude storax, thus collected from these cavities in
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Peruvian Balsam:
Synonyms: Balsam Peru; Black balsam; China oil;
Biological Source:
Balsam Peru is obtained from Toluifer pereiare belonging to family
Leguminosae.
Preparation:
Peruvian Balsam is a pathological product and is obtained usually by
inflicting injury to the trees. * It is prepared by beating the stems of the trees
with mallet.
*After a week the injured areas of the stem are scorched so as to separate the
bark from the stem and after a similar duration the bark is peeled off
completely.
* The desired balsam starts exuding freely from all the exposed surfaces, which
are then covered carefully with cloth to absorb the exuding balsam.
* The cloth that are completely soaked with the balsam is then removed and
boiled with water in a large vessel slowly.
* The balsam gets separated and settles at the bottom of the vessel. The
supernatant layer of water is removed by decantation and the residual balsam is
dried and packed in the containers.
Characteristic Features:
• It is a dark brown, viscid liquid having a pleasant aromatic odour.
• It has a peculiar warm bitter taste and persistent aftertaste which
resembles like vanilla.
• The Balsam Peru is transparent in thin films. It does not harden on being
exposed to atmosphere. It is brittle when cold.
• It is almost insoluble in water and petroleum ether but soluble in ethanol,
chloroform and glacial acetic acid.
Chemical Constituents:
Peruvian balsam contains
• Free benzoic and cinnamic acids (12-15%)
• Benzyl (40%)
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Uses:
1. It is a local protectant and rubefacient.
2. It also serves as a parasiticide in certain skin disorder.
3. It is used as an antiseptic and is applied externally either as ointment alone or
in alcoholic solution.
4. It acts as an astringent to treat hemorrhoids.
1. Peru Balsam is used as miticide, to aid in healing of indolent wounds, as
scabicide and parasiticide, in skin catarrh, diarrhoea, ulcer therapy, as local
protectant, and rubefacient.
2. It is an antiseptic and vulnerary and as a stimulating expectorant.
It is also employed in perfumery and some
chocolate flavourings, also in making of odours.
Peruvian Balsam is topically used as an antiseptic to
treat burns, frostbites, cracks, erythema, pruritus, ulcers,
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and wounds. Its suppositories are used to cure pain, pruritus, piles, and other
anal disorders. It is an ingredient in
cosmetic and hygiene products (soups, creams, lotions,
detergents) and in fixative. It can cause contact dermatitis
in some people
Tolu Balsam:
Synonyms
Thomas balsam; Opobalsam; Resin Tolu.
Biological Source
Tolu Balsam is a balsam obtained from toluifera balsamum belonging to
family Leguminosae.
It is also obtained from myroxylon balsamum
Family: Fabaceae.
Preparation:
• Tolu Balsam is considered to be a pathological product produced in the
new wood formed as a result of inflicted injury. For its preparation, it is
an usual practice to make ‘V’ shaped incisions deep into the body of the
main trunk.
• The exudate thus produced is collected in cups held strategically just at
the base of each incisions. Balsam of Tolu is collected from these cups,
mixed and packed in air-tight sealed tins.
Characteristic Features:
• It is a yellowish-brown or brown semifluid or nearly solid resinous mass.
• It has a characteristic aromatic vanilla-like odour and slightly pungent
taste.
• It is usually brittle when cold.
• It is found to be transparent in thin layers, and shows numerous crystals
of cinnamic acid.
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Benzoin:
Synonyms: Bitter almond-oil camphor.
Biological Source:
Benzoin in the balsamic resin obtained from styrax benzoin and styrax
paralleloneurus , generally known in trade as Sumatra Benzoin belong to the
family Styraceae
Preparation:
• Benzoin is also a pathological product that is obtained by incising a deep-
cut in the bark. It has been observed that after a span of about eight
weeks, the exudating balsamic resin tends to become less sticky in nature
and firm enough to collect. The entire exudate is usually collected in two
stages:
• Stage 1: First tapping-yields almond tears, and
• Stage 2: Second tapping-yields a more fluid material.
Characteristic Features:
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Tannins
• The name ‘tannin’ is derived from the French ‘tanin’ (tanning substance)
and is used for a range of natural polyphenols. Tannins are complex
organic, non-nitrogenous plant products, which generally have astringent
properties.
• The term ‘tannin’ was first used in 1796 to denote substances which
have the ability to combine with animal hides to convert them into
leather which is known as tanning of the hide.
• According to this, tannins are substances which are detected by a tanning
test due to its absorption on standard hide powder. The test is known as
Goldbeater’s skin test.
• The conversion of raw animal hides into leather has traditionally been
carried out with plant-derived tannins.
• Many different cultures have developed the process of tanning. The
compounds that bind to the plant proteins are called (by definition)
tannins.
How tanning works
• Animal skins are made up of protein called collagen (among other
things). This protein is readily degraded by bacteria and fungi.
• When tannins bond to the collagen, the cross-linked fibers are no longer
susceptible to attack.
• The tannin must effectively crosslink the protein, but must also have
desirable color properties and meet many other requirements.
CHARACTERISTICS OF TANNINS:
• 1. Tannins are colloidal solutions with water.
• 2. Non crystalline substance.
• 3. Soluble in water (exception of some high molecular weight
structures), alcohol, dilute alkali, and glycerin.
• 4. Sparingly soluble in ethyl acetate.
• 5. Insoluble in organic solvents, except acetone.
• 6. Molecular weight ranging from 500 to >20,000.
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The tannin compounds can be divided into two major groups on the basis of
Goldbeater’s skin test.
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BIOSYNTHESIS OF TANNINS:
• Tannins belong to the phenolics class of secondary metabolites. All
phenolic compounds; either primary or secondary are in one way or
another formed through shikirnic acid pathway (phenylpropanoid
pathway). Hydrolysable tannins and condensed tannins (Pro-
anthocyanidins) are the two main categories of tannins that impact animal
nutrition.
Common tannins are formed as follows
Gallic acid is derived from quinic acid.
Ellagotannins are formed from hexahydroxydiphenic acid esters by the
oxidative coupling of neighbouring gallic acid units attached to a D-
glucose core.
Further oxidative coupling forms the hydrolysable tannin polymers.
Proanthocyanidin (PA) biosynthetic precursors are the leucocyanidins
(flavan-3,4-diol and flavan-4-ol) which on autoxidation, in the absence of
heat, form anthocyanidin and 3-deoxyanthocianidin, which, in turn,
polymerize to form PAs
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KINO (pterocarpus):
• Biological Source
• It consists of dried juice obtained by making vertical incisions to the stem
bark of the plant Pterocarpus marsupium Linn., belonging to family
Leguminosae.
• Geographical Distribution
It is found in various parts of the world.
Chemical Constituents:
• Kino contains about 70–80% of kinotannic acid, kino-red, k-pyrocatechin
(catechol), resin and gallic acid.
• Kinotannic acid is glucosidal tannin, whereas kino-red is anhydride of
kinoin.
• Kinoin is an insoluble phlobaphene and is produced by the action of
oxydase enzyme. It is darker in colour than kinotannic acid.
• Chemical Tests
1. When the solution of drug is treated with ferrous sulphate, green colour is
produced.
• 2. With alkali (like potassium hydroxide) violet colour is produced.
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Uses:
• Kino is used as powerful astringent and also in the treatment of diarrhoea
and dysentery, passive haemorrhage, toothache, and in diabetes.
• It is used in dyeing, tanning, and printing.
• The aqueous infusion of the wood is considered to be of much use in
diabetes.
• The alcoholic, as well as, aqueous extracts of heartwood are known to
possess hypoglycaemic action.
• The bark exhibited hypotensive properties in pharmacological trials.
• Bark also showed antiviral effects.
Catechu:
Gambir or pale catechu of the BP 1989' BP (Vetelinary), 2000 is a dried,
aqueous extract prepared from the leaves and young twigs of a climbing
shrub,
• Botanical source: Uncaria gambier
• Family: Rubiaceae
• Geographical Source
• The tree is cultivated in tropical India, Sri Lanka, Malay States, South
China, Philippine Islands and parts of East Africa (including Zanzibar
and Tanzania).
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Chemical Constituents:
Pale catechu contain from about 7 to 30% of pseudotannin catechin and
22 to 55% of a phlobatannin catechutannic acid. Both of the about
component constitute over 60% of the drug.
It also contains catechu red, gambier fluorescin and quercetin.
It contains indole alkaloid up to 0.05%, which includes gambir-tannin and
its derivatives. Gambirtannin gives a strong fluorescence under UV light.
Catechin forms white, needle like crystals, which dissolves in alcohol and
hot water. Catechutannic acid gives green colour with ferric chloride
Uses
• Pale catechu is medicinally used as local astringent.
• In diarrhoea, it is used as general astringent. It is largely used in various
countries of east for chewing with betel leaf.
• Gambirine is reported to be hypotensive; d-catechu constricts blood
vessels.
• Catechins protect the liver from infection.
• Large proportion of gambier is used in dyeing and tanning industries. It is
used for tanning of animal hides to convert it to leather.
Nutgall:
• Synonyms (Nutgalls, blue galls, Turkish galls)
• Biological source
• Nutgall consists of the pathological outgrowth obtained from the young
twigs of the dyers oak, Quercus infectoria
• Olivier, belonging to family Fagaceae.
• Outgrowth is caused by the puncture of ovums of insect Cynipstinctoria
or Adleria gallaetinctoriae Olivier Family Cynipidae
Geographical Source
Oak galls are obtained principally from Turkey. Dyers
oak is found in Turkey, Syria, Iran, Cyprus, and Greece.
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Chemical Constituents:
• Nutgalls contains about 50–70% tannin mainly gallotannic acid which is
official tannic acid.
• It also consists of 2–4% gallic acid, ellagic acid, sitosterol, methyl
belulate and methyl oleanolate which are methyl esters of betulic and
oleanolic acid. Recently few more compounds such as roburic acid, and
syringic acids have been reported from galls. It contains abundant starch.
• Syringic acids exhibited hepato-protective, antibacterial effects,
antidiabetic effects, antiglycating properties,
• Syringic acids induced motor dysfunction, dopaminergic markers
expression and neuro-inflammation in mice
• Tannic acid of commerce is a hydrolysable tannin which yields gallic
acid and glucose. The molecule of tannic acid may contain the gallic acid
up to pentagalloyl glucose. It is isolated by fermentation and subsequent
extraction of galls with water-saturated ether.
Uses:
• Nutgall is the major source of tannic acid, which is largely used in
tanning and dyeing industry and for the manufacture of ink.
• It is used medicinally as a local astringent in ointments and suppositories.
• Antibacterial effect of Quercus infectoria is reported
• No cytotoxic effect
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Krameria:
Botanical origin: Krameria triandra
• Family : Krameriaceae.
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Myrobalan:
• The common name myrobalan can refer to several unrelated fruit-
bearing plant species:
• Cherry plum, myrobalan plum (Prunus cerasifera)
• Amla, Amalaki, emblic myrobalans (Phyllanthus emblica)
• Bibhitaki, Belliric myrobalans (Terminalia bellirica)
• Haritaki, Chebulic myrobalans (Terminalia chebula)
• Arjuna, Arjun myrobalans (Terminalia arjuna)
• Myrobalan extracts (at least from Terminalia chebula) are used
for tanning
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Cosmeceuticals
• Cosmeceuticals are cosmetic products with biologically active
ingredients having medical or drug‐like benefits.
Moisturizing Agents:
Stratum corneum is the primary barrier of the skin whose one of main
purpose is to keep inside in & outside out. This barrier is rich in
cholesterol, free fatty acids, and ceramides.
Water from the stratum corneum gets evaporated very quickly leading to
dehydration. This dehydration of skin can be averted by using
moisturizers which provide flexibility to the skin.
Moisturizers by hydrating the skin, make the stratum corneum softer &
can even alter physiology of skin.
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Sunscreen Agents:
• Use of sunscreen agents and limiting the exposure to sun prevents early
wrinkling and skin cancer.
• Sunscreen agents are used to prevent sunburns.
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• Chemical sunscreen agents protect the skin from the sun by absorbing the
ultraviolet (UV) and visible sun rays, while physical sunscreen agents
reflect, scatter, or block the rays.
• Chemical sunscreens mainly based on para‐amino benzoic acid, its
derivatives, cinnamates, various salicylates etc. are frequently employed
as sun blocking agents.
• Direct physical blockers include metal containing compounds such as
iron, zinc, titanium, and bismuth.
Vitamins:
• Exposure to the UV radiations accelerates the aging effect of the skin.
• Damage is initiated by the generation of reactive oxygen species (free
radicals). It is a progressive process whose consequences are damage to
DNA.
• The topical treatment of acne vulgaris with vitamin A, is very well
supported by evidence.
• Vitamin B3, commonly known as nicotinamide is available in
cosmeceutical products and can be used as a complementary agent for
some types of acne, as well as aging skin.
Vitamin A:
• The human epidermis contains significant amounts of vitamin A (alltrans‐
retinol). It has been observed that both UVB and UVA can damage the
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• L‐ascorbic acid is the active form of vitamin‐C, which was first used as
cosmeceutical creams.
• Previous formulations ( L‐ascorbic acid) were very unstable due to the
oxidation of the vitamin exposed to air. So to overcome this problem,
esterified derivatives of L‐ascorbic acid in topical formulations have been
used to improve stability.
• The most commonly used derivatives are ascorbyl‐ 6‐palmitate and
magnesium ascorbyl phosphate.
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Nutraceuticals
“bio-actiVe products presented as 'dietary supplements' or similar”
Introduction:
• Nutraceuticals, a term first coined by Stephen DeFelice in 1989.
• These are natural plant products that are not only the source of nutrient-
rich foods, but also have therapeutic effects with virtually no adverse
reactions.
• Because of their beneficial effects on the prevention and treatment
of several diseases, major biotechnology companies and academia have
ventured into the screening and large-scale production of the next-
generation pharmaceuticals from plants
• Nutraceuticals may be defined as—‘any substance that may belong to a
plant, food or an essential component of food providing definitive
medicinal usefulness and health promotion as well as physiological
benefits, and ultimately minimise the possible risk of the prevailing
chronic disease significantly.
• Products of which one would have heard rarely some l0 or 20 years
ago are now objects of daily discussion. The lack of licensing of
these products is a point of major concern
• One of the significant outcomes of such a search is the identification of a
medicinal plant, Echinacea purpurea, as a rich source of nutraceuticals.
The plant extract has been reported to prevent viral infection and reduce
tumor progression.
• In addition, daily use of the extract is known to significantly abate
leukemia as well as extend the life span of both leukemic and aging mice.
• Functional Food may be defined as—“the food usually prepared by the
aid of ‘scientific intelligence’ using definite knowledge about its
anticipated merit/usefulness.”In this manner, the functional food
essentially caters to the body with the necessary quantum of vital
carbohydrates, fats, proteins and vitamins, etc, required for its normal as
well as healthy survival.
• Examples: Vegetables, rice, wheat, fruits, pulses, fish, eggs, poultry
products, beef, meat etc
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12)TUMOUR INHIBITORS FROM PLANTS BY BILAL MALIK
Natural anticancer:
• Natural products have played a major beneficial role in cancer
chemotherapy for over 50 years, both in terms of providing
established drugs and new lead compounds for synthetic optimization,
and in furnishing substances for probing cellular and molecular
mechanisms of action relevant to cancer inhibition.
• Out of 175 small-molecule anticancer drugs introduced into therapy over
an approximately 70-year period, about 49% were either obtained from
organisms directly or were derived from natural products .
Catharanthus roseus:
• Vinblastine is isolated from the dried entire plant of Catharanthus roseus
Linn (Apocynaceae).
• It is indigenous to Madagascar but is now widely distributed
throughout warm regions and is much cultivated as an ornamental; it
grows profusely in southern Florida. Commercial supplies of the
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12)TUMOUR INHIBITORS FROM PLANTS BY BILAL MALIK
drug are obtained from both wild and cultivated plants produced in
various locations, including Africa, India, Thailand, Taiwan, eastern
Europe, Spain, USA and Australia.
Constituents:
• About 150 alkaloids have now been isolated from C. Roseus .Of
particular interest is a group of about 20 bisindole alkaloids which
contains those having antineoplastic activity, including vincristine and
vinblastine
• vincristine is obtained in about 0.0002% yield from the crude drug.
Uses:
• Uses. vinblastine is used mainly for the treatment of generalized
Hodgkin's disease, and non-hodgkin's lymphomas. Vincristine is
used principally in the treatment of acute lymphocytic leukaemia in
children.
• It has other applications for lymphomas, small cell lung cancer,
cervical and breast cancers.
• The semi-synthetic vindesine is also used in the treatment of acute
lymphoid leukaemia in children. vincristine has a superior antitumour
activity compared to vinblastine, but is more neurotoxic.
• Vinorelbine is a newer, orally active, semi-synthetic
anhydroderivative of 8‘-norvinblastine with a broader anticancer
activity and lower neurotoxic side-effects than the other
Catharanrthus alkaloids.
Podophyllum peltatum:
• Synonyms: Podophyllum, American Mandrake, May-apple root.
• Geographical Source
Podophyllum peltatum is indigenous to Eastern part of the United States and
Canada. It grows wildly in Virginia, North Carolina, Kentucky, Indiana, and
Tennessee
Chemical Constituents:
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Rifampicin:
• Rifampicin, also known as rifampin, is an antibiotic used to treat several
types of bacterial infections. This
includes tuberculosis, leprosy(Leprosy is an infectious disease that
causes severe, disfiguring skin sores and nerve damage in the arms and
legs).
• Rifampicin was discovered in 1965, marketed in Italy in 1968, and
approved in the United States in 1971.
• It is on the World Health Organization's List of Essential Medicines, the
most effective and safe medicines needed in a health system.
Angiogenesis:
• Tumor growth beyond a certain prevascular size depends on the
production of new capillaries from preexisting vessels.
• This complex process, called angiogenesis, involves enzymatic and
signal transduction cascades that affect extracellular matrix
degradation, fibrinolysis, hemodynamic control of oxygenation,
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Antitumor effects:
• Rifampicin, exerts potent inhibitory effects on hepatic tumors when
administered orally at low doses. The in vitro effects of rifampicin to
rapidly downregulate angiogenesis- and mitogenesis-related genes in
cultured endothelial cells are reminiscent of endostatin, one of the most
well-studied angiogenesis inhibitors.
• However, rifampicin at the expected hepatobiliary concentrations after
low oral doses showed more complete antiproliferative effects on
endothelial cells, which make rifampicin favorable as an adjunct
anticancer regimen.
{ Vascular endothelial growth factor (VEGF), is a signal protein produced by cells that
stimulates vasculogenesis and angiogenesis. It is part of the system that restores the oxygen
supply to tissues when blood circulation is inadequate such as in hypoxic conditions. VEGF's
normal function is to create new blood vessels. When VEGF is overexpressed, it can
contribute to disease. Solid cancers cannot grow beyond a limited size without an adequate
blood supply; cancers that can express VEGF are able to grow and metastasize. It also has
inhibitory effect on VEGF.}
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Macrolides as antitumor:
• The macrolides are a class of natural products that consist of a
large macrocyclic lactone ring to which one or more deoxy sugars may be
attached.
• The lactone rings are usually 14-, 15-, or 16-membered. Macrolides
belong to the polyketide class of natural products. Some macrolides
have antibiotic or antifungal activity and are used as pharmaceutical
drugs.
• Azithromycin
• Clarithromycin
• Erythromycin
Bryostatins are a group of macrolide lactones first isolated in the 1960s from
extracts of a species of bryozoan, Bugula neritina.
The structure of bryostatin 1 was determined in 1982. To date, 20 different
bryostatins have been isolated; further, certain analogs of bryostatin have been
referred to as "bryologs". Bryostatins are potent modulators of protein kinase C.
They are currently under investigation as
Anti-cancer agents,
Anti-aids/Hiv agents and
a memory-enhancing agent.
{ Hodgkin disease (Hodgkin lymphoma) is a type of lymphoma, a cancer that starts in white
blood cells called lymphocytes. Lymphocytes are part of the immune system.
https://www.youtube.com/watch?v=FcvqEsLb23s}
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• {Non-Hodgkin lymphoma (NHL) is a group of blood cancers that includes all types
of lymphoma except Hodgkin's lymphomas
• https://en.wikipedia.org/wiki/Protein_kinase_C}
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Clinical Pharmacognosy
Introduction:
Natural medicines have been used to enhance human health since
time immemorial and the success of modern medical science largely
depends on drugs originally obtained from natural resources.
Medical science has exploited plants, animals, microorganisms and
minerals as the potential sources of drugs to prevent and cure
human health problems.
Even today, the traditional medicinal practices and natural remedies
are equally relevant in modern pharmaceutical practices worldwide.
In the modern pharmacy, about 50% of drugs and drug substances
are derived from natural products.
Clinical pharmacy requires optimum use of medications, therapeutic
knowledge, counseling, clinical experience, therapeutic drug monitoring
and disease good diagnosis.
Clinical pharmacists should monitor patient outcomes according to the
patient’s situation and the probable risks associated with therapy.
Recognition of therapeutic systems and patient records are principles of
this field.
Clinical pharmacists should prepare a nice atmosphere and consultation
area and have a good communication skill as well as should know the
patient’s quality of life that can be obtained via interview of patients
While clinical pharmacy significantly progressed, a gap between this
science and herbal and traditional medicines fields is evident. As the use
of herbals increased in the recent years, new kinds of demands are raised.
There are several potential problems associated with herbal remedies like
lacking of systematic reviews and evidence-based data about their
efficacies.
One of the reasons behind increase in use of herbal medicines is the belief
that they have lower toxicities but the fact is that herbal medicines may
cause unwanted effects, allergic or toxic reactions
Herbs can even cause drug-drug, drug-food and herb-drug interactions if
not properly used specially in use of OTC drugs.
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Clinical pharmacognosy should deal with above problems and find the
best solutions for them. Although this term has been used in a workshop
in the United States entitled, “Clinical Pharmacognosy: Contribution of
pharmacognosy to clinical trials of botanicals and dietary supplements”,
which took place at the American Society of Pharmacognosy meeting in
Portland, Maine, on July 2007 and in a Japanese journal on March 2011,
there has not been any comprehensive definition yet
The revival of herbal medicine in the world creates a demand for studies
in the field of pharmacognosy, traditional medicine and some related
fields.
From a practical perspective this includes quality control (identity, purity,
consistency), efficacy (therapeutic indications, clinical studies,
pharmacological investigations), documentation and safety (adverse
reactions, drug interactions, contraindications, precautions and toxicities).
There are huge capacities of research topics in the herbal and traditional
medicine fields which this new discipline can design and perform them
clinically. This new borderline discipline may extend the scope of clinical
aspects of pharmacognosy and play a progressive role in the safe, rational
and efficient use of traditional and herbal medicine
Clinical pharmacognosy is a bridge between clinical research and
botanicals knowledge providing clinical and pharmaceutical researchers,
physicians and other healthcare professionals with the key information
they need to assist the progress of herbal and traditional medicines.
Clinical pharmacognosist should ask the patients about the herbal drugs
or other supplements they have had taken before and about the history of
possible allergic reactions.
He should also evaluate the patient recovery process after using each kind
of synthetic, herbal or traditional drugs and should focus on resolving a
wide range of challenging problems
It seems that in the third millennium, we need education of clinical
pharmacognosists for providing more details regarding different aspects
of clinical applications of natural health products. In order to use rational
herbal and traditional medicines and adding standard clinical values to
them, establishing and spreading of clinical pharmacognosy feature may
help to improve health to all.
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Mechanism:
Increase the force of systolic contraction
Shorten length of systole
As a result
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b) Convallaria majalis :
Family:
Liliaceae
Part Used:
Rhizomes/roots or aerial parts
Constituents:
The principal glycoside is convalla-toxin, which on hydrolysis gives
strophanthidin and rhamnose.
Uses:
Cardio-active (same as digitalis).
Convallatoxin, a Dual Inducer of Autophagy and Apoptosis, Inhibits
Angiogenesis In Vitro and In Vivo exerts cytotoxic effects on a number of
cancer and normal cell lines and induces apoptosis by increasing caspase-
3 and poly ADP ribose polymerase (PARP) cleavage.
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c) Urginea indica:
Synonym: Sea onian, Indian squill, scilla
Family: Liliaceae
CHEMICAL CONSTITUENTS
Glucoscillaren A
Enzyme scillarenase
Mucilage
Calcium oxalate
PHARMACOLOGICAL ACTIVITY
Uses:
The squill has shown to have cardiac effects similar to digoxin, including
positive inotropic and negative chronotropic effects.
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The aglycones in squill are poorly absorbed from the GI tract and are
therefore less potent than digitalis cardiac glycosides. Additional
cardiovascular properties include reducing left ventricular diastolic
pressure and reducing pathologically elevated venous pressure.
a. food flavoring
b. medicine
Garlic Bulb:
The bulb of Allium sativum is the only part of the plant eaten
The cloves are grouped together between the membranous scales and
enclosed within a whitish skin, which holds them as in a sac
History:
In China, garlic tea has long been recommended for fever, headache, and
cholera.
In Japan, garlic is used as remedy for the common cold with headache,
fever and sort throat.
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Common Uses:
Antiseptic
Antimicrobial activities
Insect repellent
Anticancer effects
Vaginal Infections
Antioxidant effects
High cholesterol
Hypertension
Medical Uses:
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DosageBulb—3g
e) PUNICA GRANATUM:
Pomegranate:
Family:
Punicaceae
Cultivation:
Plant:
10 cm in diameter
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Constituents:
Fruit
◦ Antioxidants
Polyphenols
Tannins (Ellagitannins)
Anthocyanins
◦ Piperidine alkaloids
Historic Uses:
pregnancy
strengthen teeth.
Traditional Uses:
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Modern Uses:
◦ Antiathersceloris
◦ Prevent cancers
◦ Hypertension
◦ Diabetes
◦ Anthelmintic
◦ Antidiarrheal
◦ Dried Flowers
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• Unani Peepal.
Constituents:
Aerial roots are given to women, also used in prescriptions, for inducing
conception.
The fruits contain 4.9% protein having the essential amino acids,
isoleucine and phenyl-alanine.
Medicinal Uses
Bark
The crude bark extract of the plant also showed protection in acute
animal models of convulsions, which was found to be due to GABA
aminotransferase inhibitory activity of its bioactive metabolites
Laxative
Its leaf extract was studied in acute animal models of convulsion, but was
found to be ineffective
Fruits
Roots
The crude root extract and fractions were studied for anticonvulsant activity
only saponins has shown significant effect.
Effects on Respiratory:
The alcoholic bark extract at 300, 375, 450 mg/kg;i.p. and 75 mg/kg;i.v.
doses inhibited the acetylcholine and histamine. The extract exhibited
more pronounced effect against asthma induced by acetylcholine as
compared to histamine, suggesting strong involvement of
parasympatholytic and weak antihistaminic mechanisms.
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Leaves of the plant In guinea pigs at a dose of 150 and 300 mg/kg
significantly delay the onset tine of histamine and acetylcholine induced
pre-convulsive dyspnea.
Potent Mast cell stabilizing effect was observed and was comparable to
ketotifen at 20 µg/ml of
Further details?????????
Pharmacokinetic profile??????
The long history of traditional use, with no reports of any serious side
effect suggests that F. religiosa can be considered as safe.
In acute toxicity studies carried out on male Swiss albino mice, the
methanolic fruit extract of F. religiosa was found to be safe at 10 times of
its effective doses (up to 1000 mg/kg; i.p.).
• Family Acanthaceae.
• Unani Arusaa
Constituents:
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Actions/Uses:
The chief quinazoline alkaloid vasicine is reported in all parts of the plant.
Which have the following properties
• Bronchodilator,
• Respiratory stimulant,
• Hypotensive,
• Cardiac depressant,
• Uterotonic
• Abortifacient
• Expectorant
• Antispasmodic
• Febrifuge
• Antifungal activity
Dosage
• Leaf—10–20 ml juice.
• Root—3–6 g powder.
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Constituents
Aloe gel also slows or inhibits the synthesis of thromboxane, which may
accelerate the healing of burns.
Uses:
Toxicity reports
Aloe vera extract also caused hyperplasia of the large intestine in male
and female mice and hyperplasia of the mesenteric lymph node in male
mice and hyperplasia of the stomach in female mice
Aloe barbadensis extracted with water and given to pregnant albino rats
on gestational days (GDs) 0 through 9 was an abortifacient and produced
skeletal abnormalities.
Aloin (an anthraquinone) did not produce tumors when included in the
feed of mice for 20 weeks,
Other animal data also suggest that components of Aloe inhibit tumor
growth and improve survival.
Diarrhea was the only adverse effect of note with the use of Aloe-derived
ingredients to treat asthma, ischemic heart disease, diabetes, ulcers, skin
disease, and cancer.
The Cosmetic Ingredient Review Expert Panel advised the industry that
the total polychlorobiphenyl (PCB)/pesticide contamination of any plant-
derived cosmetic ingredient should be limited to not more than 40 ppm,
with not more than 10 ppm for any specific residue and that limits were
appropriate for the following impurities: arsenic (3 mg/kg maximum),
heavy metals (20 mg/kg maximum), and lead (5 mg/kg maximum).
Contraindications:
Dosage:
Constituents:
Uses:
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Contraindications:
Dosage:
• Root—1–3 g powder.
Constituents:
Uses:
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• English _ Lemon.
• Unani _ Utraj
Constituents:
Uses:
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Dosage:
• Fruit—6–12 g
(Juice—5– 10 ml).
e) Balsamodendron mukul:
• Synonym _ Commiphora mukul,
C. wightii (Arn.).
• Family _ Burseraceae.
• Habitat _India
Constituents:
Uses:
Dosage : Oleo-gum-resin—2–4 g
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Musculo-skeletal disorders :
Musculoskeletal Disorders or MSDs are injuries and disorders that affect
the human body’s movement or musculoskeletal system (i.e. muscles,
tendons, ligaments, nerves, discs, blood vessels, etc.).
Constituents
. The seeds are reported to contain a fatty oil rich in unsaturated fats,
mainly linoleic acid (50-60%), oleic acid (20%), eicodadienoic acid
(3%) and dihomolinoleic acid (10%)
The extracts have used to treat nervous system diseases such as memory
impairment, epilepsy, neurotoxicity, as antispasmodic, analgesic effects
on experimental animals.
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The methanol extract modifies amino acid levels in the rat brain regions
and thus could be helpful in some neurodegenerative diseases which is
related to amino acid level imbalances in the central nervous system.
Other uses:
• diuretic,
• antihypertensive,
• anti-diabetic,
• immune-modulatory,
• antimicrobial,
• anthelmintic,
• bronchodilator,
• antiinflammatory,
• anti-tussive,
• gastroprotective,
• hepato-protective,
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• Cholesterol decreasing
• Renalprotective and
Anti-oxidant properties
Traditional Uses:
• Stimulant,
• Carminative,
• Diuretic,
• Puerperal fever.
• Common cold,
• Cough
• Bronchospasm.
• Sexual diseases,
• Diarrhea
• Skin disorders
• English: Fenugreek.
Constituents:
• Flavonoids (vitexin)
• Glycosides
• Esters
• Luteolin
• mucilage (galactomannan)
Uses:
• Loss of appetite,
• Flatulence,
• Dyspepsia,
• Colic;
• Diarrhoea,
• Dysentery;
• Galactagogue
• Secretolytic,
• Antiseptic
• Demulcent
• Hypoglycaemic,
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• Diabetes mellitus,
• Hypercholesterolaemia.
• Anti-inflammatory,
• Antispasmodic,
• Skeletal muscular disorders
• Expectorant,
• Circulatory stimulant,
• Diaphoretic,
• Irritable bowel
• Diarrhea,
• Colds and influenza
• Migraine and cluster headache.
• Dyspepsia,
• Loss of appetite,
• Tympanitis,
• Anaemia,
• Cough
• Dyspnoea
• Constipation,
• Colic,
• Edema
• Throat infections
• Motion sickness
• Vomiting of Pregnancy, post-Operative Antiemetic
• Anorexia,
• Bronchitis
• Rheumatic complaints
• Suppress gastric contractions and secretions
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Dosage:
Dried leaf—1–3 g powder; 10–20 g for decoction.
stembark—2–4 g powder decoction for external use.
Leaf juice—10–20 ml; oil—5–10 drops.
Bark decoction—50–100 ml
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The aqueous alcoholic extract of the bark contains bergenin, gallic acid
and ethyl gallate.
The fruit contains anthocyanins and yielded citric, malic and gallic acids.
Gallic acid and tannins account for astringency of the fruit. Malic acid is
the major acid of fruit; a small quantity of oxalic acid is reported to be
present. Glucose and fructose are principal sugars in the ripe fruit;
sucrose was not detected.
The seeds contain tannin, ellagic acid, gallic acid, beta-sitosterol,
essential oil, myricyl alcohol is present.
The stem bark yielded friedelan- -alpha-ol, kaempferol, quercetin,
betasitosterol and its glycoside, kaempferol- -O-glucoside, gallic acid,
friedelin and betulinic acid. It contained eugenin and epi-friedelanol.
tannins were reported.
The leaves contain aliphatic alcohols, sitosterols, betulinic acid and
crategolic (maslinic) acid.
The flowers contain triterpenic acids—oleanolic acid and crategolic acid.
The oleanolic acid is a strong protector against adriamycin-induced lipid
peroxidation in liver and heart microsomes.
Phenols, including methylxanthoxylin and, -dihydroxy- -
methoxyacetophene have been isolated from the plant (also from the
seed).
Seeds in normal and alloxanized rabbits exhibited hypoglycaemic
activity. The chloroform fraction of seed extract exhibited potent anti-
inflammatory action. Water extract exhibited antibacterial properties.
Action Fruit—stomachic, carminative, diuretic.
Bark and seed—anti-diarrhoeal. Seed—hypo-glycaemic.
Leaf—antibacterial, anti-dysenteric.
Key application: Bark—in nonspecific acute diarrhoea and in topical
therapy for mild inflammation of the oral-pharyngeal mucosa; externally
in mild, superficial inflammation of the skin. The seed has been included
among unapproved herbs by German Commission E, as the blood sugar-
lowering effect could not be established by several researchers.
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a)Nux Vomica:
Synonyms:
Poison Nut, Dog Button, Quaker Button
Description:
S. nux-vomica is a medium-sized tree with a short thick trunk.
The leaves are about 4 inches long and 3 inches wide.
The flowers are small with a pale green colour with a funnel shape.
The fruit are about the size of a large apple with a smooth and hard shell
which when ripened is a mild shade orange colour.
The flesh of the fruit is soft and white with a jelly-like pulp containing
five seeds covered with a soft woolly substance.
The seeds are removed from the fruit when ripe.
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b)DATURA:
Jimson Weed
Syn : Jimson weed, Thorn Apple, Mad Apple
History:
The name “Jimson” comes from the word “Jamestown.” Early colonists
were known to have found the weed growing in abundance in Jamestown.
Dating and analysis of remains show 4000 years of use.
Was used as an aphrodisiac in the Middle Ages.
Very toxic and can cause hallucinations
Description:
Grows to about 1.5m tall.
Annual shrub that grows mainly in the summer months (July – October).
Requires sunlight to grow.
Prefers neutral or basic, dry soils.
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Preparations:
Leaves are rolled into cigarettes for asthma treatment
Seeds can be crushed and used in drinks or teas
Flowers can be boiled
Leaf extracts or seeds can be made into pill form
Constituents:
Atropine
Scopolamine (main cause of hallucinations)
Hyoscyamine
Other tropanes
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Scopolamine:
Central nervous system depressant
Antimuscarinic effects similar to atropine
Commonly used to prevent motion sickness
Blocks short-term memory
Also used as a gastrointestinal and urinary antispasmodic
Hyoscyamine:
Has similar, but more potent, antimuscarinic effects as atropine and
scopolamine
Used as an adjunct in treatments of peptic ulcer disease and Zollinger-
Ellison syndrome
Antidote to cholerinesterase inhibitors
Contraindications:
Due to the dangerous effects of datura, its use is not recommended, but is
still used in many areas.
The accumulation of acetylcholine leads to persistent stimulation of
nicotinic receptors, possibly altering fetal development.
Adverse Effects:
All parts of Datura are toxic
Overdosing on Jimson weed will lead to:
Visual hallucinations
Disorientation
Speech incomprehension
Dilated pupils
Can be fatal
Delirium, agitation and seizures
Scopolamine is known to be the main cause of hallucinations
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The seeds yield a fatty oil containing palmitic, stearic, oleic, linoleic and
linolenic acids.
Actions
Opium is obsolete as a drug. Narcotic, sedative, hypnotic, analgesic,
sudorific (promote sweating), anodyne (releive pain), antispasmodic,
hypoglycemic and antitumor.
Poppy seed—nutritive, demulcent, emollient, spasmolytic, against
constipation, also used in catarrh of the bladder.
Poppy seed oil is also free from narcotic properties.
Used against diarrhoea, dysentery and scalds (burns).
e)Atropa . belladonna:
Synonym A. acuminata
Family Solanaceae
Habitat Kashmir
English Indian Belladonna, Indian Atropa.
Unani Luffaah, Luffaah-Barri, Yabaruj, Shaabiraj.
The herb contains tropane (tropine) or alkaloids including hyoscamine
and atropine; flavonoids; coumarins; volatile bases (nicotine).
Tropane alkaloids inhibit the parasympathetic nervous system, which
controls involuntary bodily activities; reduces saliva, gastric, intestinal
and bronchial secretions, and also the activity of urinary tubules.
Tropane alkaloids also increase the heart rate and dilate the pupils. These
alkaloids are used as an additive to compound formulations for
bronchitis, asthma, whooping cough, gastrointestinal hypermotility,
dysmenorrhoea, nocturnal enuresis and fatigue syndrome.
Atropine provides relief in parkinsonism and dystonia (neurological
movement disorders).
The root is most poisonous,
Actions
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anti-inflammatory,
diuretic
Relieves bloating,
nausea,
settles stomach
stimulates appetite
Amenorrhoea
Enuresis
Dyspepsia
flatulence.
catarrh of the upper respiratory tract.
Dosage:fruit. 3-6 g pwd
Contraindications: Pregnancy
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USES:
Olea-gum-resin: stimulates the intestinal and respiratory tracts and the
nervous system bark.
Used for simple digestive problems such as bloating, indigestion,
constipation; for congested mucus, bronchitis, whooping cough, also for
neurological affections, epilepsy, cramps and convulsions, In dyspepsia,
chronic gastritis, irritable colon; as spasmolytic.
Contraindications: bleeding disorders, pregnancy, infectious or inflammatory
GI diseases
Dosage: oleo gum-resin—125–500 mg.
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diarrhoea,
stimulant,
diuretic,
antibacterial,
emmenagogue,
galactagogue,
hypotensive
Dosage
Fruit—1–3 g pwd.
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Uses:
Stomachic,
antimicrobial
diarrhoea,
colitis,
dysentery
enteric infections,
digestive,
astringent,
spasmolytic,
hypoglycaemic.
Roots in dysuria;
Stem bark in diabetes and lipid disorders.
Dosage
Pulp of unripe/ half ripe fruit—3 g Pwd
Roots—6 g Pwd.
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Kernel contains fixed oil about 45% and amygdalin and benzoic acid
among others.
The crude extract of the fruit was found effective in controlling centrally
induced emesis in dogs. The action was comparable to that of
Metoclopramide (Maxolon) and chlorpromazine (Largactil).
Uses:
Fruit
laxative
Nutritive
Improves haemoglobin levels in iron deficiency
Promotes excretion of excess calcium by the kidneys
An adjuvant for atherosclerosis and arthritis
Root
Astringent
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b) Picrorhiza kurroa:
Family: Scrophulariaceae
Habitat: Kashmir
English: Picrorhiza
Unani: Kutki
Part Used: Roots, Rhizome
Uses:
Stomachic
Antidiarrhoeal
Hepatoprotective (in Jaundice)
Used in hepatitis
Chronic dysentery, Amoebiasis.
Intermittent fever, Dyspnea and Skin Diseases.
Family: Scrophulariaceae
Habitat: Kashmir
English: Picrorhiza
Unani: Kutki
Part Used: Roots, Rhizome
Uses:
Stomachic
Antidiarrhoeal
Hepatoprotective (in Jaundice)
Used in hepatitis
Chronic dysentery, Amoebiasis.
Intermittent fever, Dyspnea and Skin Diseases.
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c)Nigella sativaLinn. :
• Family: Ranunculaceae.
• Habitat: Cultivated in India and Pakistan.
• English: Black Cumin, Small Fennel.
• Unani: Kalonji, Kamaazaruus.
• Part used: Seeds
Constituents:
• The essential oil contains nigellone, 2-methyl-4-isopropyl-p-quinone,
carvone, d-limonene, cymene, fatty acids including palmitic, myristic,
stearic, oleic, linoleic, linolenic and Beta-sitosterol. Nigellone inhibits the
release of histamine.
• The extracts have antispasmodic, CNS depressant and analgesic effects
on experimental animals.
Uses:
• Skeletal muscular prob.
• stimulant,
• carminative,
• diuretic,
• lactiferous,
• emmenagogue (stimulate uterine)
• puerperal fever.
• common cold,
• cough
• bronchospasm.
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e) Claviceps purpurea:
• Family Hypocreaceae.
• Habitat A fungous parasite on a number of grasses particularly in rye,
cultivated in the Nilgiris and at Chakrohi farm in Jammu.
• English Ergot of Rye. Fungus of Rye.
• Unani Argot.
• The fungus gave indole alkaloids. The ergometrine or ergonovine group
includes ergometrine and ergometrinine. The ergotamine group includes
ergotamine and ergotaminine. The ergotoxine group includes
ergocristine, ergocristinine, ergocryptine, ergocryptinine, ergocornine and
ergocorninine.
• The fungus also contains histamine, tyramine and other amines, sterols
and acetylcholine.
• Ergotamine is used to relieve migrainous headaches as it is a
vasoconstrictor and has anti-serotonin activity.
• Ergometrine is used after childbirth and for post-partum haemorrhage, as
it is a powerful uterine stimulant, particularly of the puerperal uterus.
(Both the constituents are used under medical supervision).
• Ergocornine significantly inhibited the development of induced
mammary tumours in rats. The derivatives of ergot alkaloids are known
to have suppressing effect on human breast cancer in initial stages. This
activity is linked to prolactin inhibitory action.
• The extract is toxic at 1.0–3.9 g, ergot alkaloids at 1 g in adults, 12 mg in
infants. (Francis Brinker).
USES/ACTION:
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Uses/Action
• Nutmeg—carminative, spasmolytic, antiemetic; used in flatulency,
diarrhoea, nausea and vomiting; topically anti-inflammatory.
• stimulant carminative, Narcotic in high doses, used in rheumatism,
chronic bowel complaints and asthma. When roasted, both nutmeg and
mace are used for diarrhea, colic, flatulence, antispasmodic, inhibit
prostaglandin synthesis and used in dyspepsia.
• Fruit in spermatorrhoea.
Dosage dried seed—0.5–1 g pwd
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14. CLINICAL USE OF HERBS & HERBAL MEDICINE BY BILAL MALIK
a)Cucumis melo:
Synonym: C. utilissimus Roxb
Family: Cucurbitaceae
Habitate: Cultivated in India, Pak, Afghanistan
English: Snake Cucumber
Unani: Kakari
Part used: seeds
Uses: Cooling,
diuretic (in painful micturation)
Dysurea,
lithiasis
Dosage: seeds 3-6 g.
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Blood purifier,
c)Zea mays:
Family: Gramineae, Poaceae
Habitat: South america, India, Pak,
Kashmir
English: Maize, Corn
Unani: Makka, Zurraa Makka
Constituents:
Saponins,
alantoin,
sterols (beta-sisterol and stigmasterol),
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14. CLINICAL USE OF HERBS & HERBAL MEDICINE BY BILAL MALIK
alkaloids hordenine,
polyphenols,
mucilage,
potassium,
vit-C,
Vit-K,
Cryptoxanthin,
anthocyanins,
plant acids,
tannin
USES:
diuretic,
urinary demulcent,
antilithic,
cystitis,
urethritis,
prostatitis,
irritation of UT,
nephritis,
uncontrollable bladder,
bed-wetting.
Antiviral
antitumor
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14. CLINICAL USE OF HERBS & HERBAL MEDICINE BY BILAL MALIK
Habitat: India
English: Land-Caltrops, Puncture Vine
Unani: Khaar-e-Kkasak Khurd
Part used: Fruit, leaves and seeds
Constituents:
Sapogenins
diosgenin,
gitogenin,
chlorogenin,
ruscogenin,
D-spirosta-diene,
Flavonoids—rutin,
quercetin,
kaempferol,
kaempferol
glucoside,
rutinoside,
tribuloside
alkaloids
(harmane and harmine)
Harmol
Uses:
diuretic,
demulcent,
anti-inflammatory,
anabolic,
spasmolytic,
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muscle relaxant,
hypotensive,
hypoglycaemic,
strangury,
urolithiasis,
crystallurea,
urinary discharge,
pruritis,
sexual inadequacy,
support medicine of cough and asthma.
haemostatic.
stomachic,
cardiotonic
for treating angina pectoris
hypotensive,
hypolipidaemic,
hypoglycaemic.
Dosage:
Fruit— 3-6 g powder
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