Saponins

Terpenes and sterols are complex molecules synthesized by equally complex biosynthetic pathways. Recent progress in using the tools of genetics, molecular genetics and genetic engineering to dissect triterpene metabolism in the cytosol, and terpene metabolism in the ...

The occurrence of the two new cis-fused A/B rings furostanol saponins (25S)-26-O-β-Dglucopyranosyl-5β-furostan-1β,3β,22α,26-tetraol-1-O-β-D-glucopyranoside and (25S)-26-Oβ-D-glucopyranosyl-5β-furostan-1β,2β,3β,5β,22α,26-hexaol and the known compounds

All rights reserved EUROPEAN JOURNAL OF MASS SPECTROMETRY Desmodium adscendens (DA) (Sw) D.C. var. Adscendens (Papilionaceae) is a medicinal herb commonly used in African traditional medicine. It is reported to be used for asthma, to aid parturition, to treat dysmenorrhoea and to improve lactation. It is known to have hepato-protective properties and is employed to manage several other conditions, including fever, pain and epilepsy. It is a typical example of a single plant being used for many apparently unrelated diseases. 1 Many studies have reported that Desmodium adscendens activates calciumdependent potassium channels, 2 inhibits NADPH-dependent

Aims To characterize the natural history of methamphetamine withdrawal during the first 3 weeks of abstinence. Design Cross-sectional study with comparison group. Setting A substance use treatment facility in Chiang Mai Province, Thailand. Participants The sample comprised 21 in-patients undergoing treatment for methamphetamine dependence. Nine age-and sex-matched non-dependent individuals provided comparison data. Measurements Instruments including: the Amphetamine Withdrawal Questionnaire, a modified version of the Cocaine Selective Severity Assessment, Clinical Global Impression scale and the St Mary's Hospital Sleep Questionnaire were completed daily for the first 3 weeks of abstinence. Findings Methamphetamine withdrawal severity declined from a high initial peak within 24 hours of the last use of amphetamines reducing to near control levels by the end of the first week of abstinence (the acute phase). The acute phase of amphetamine withdrawal was characterized by increased sleeping and eating, a cluster of depression-related symptoms and less severely, anxiety and craving-related symptoms. Following the acute withdrawal phase most withdrawal symptoms remained stable and at low levels for the remaining 2 weeks of abstinence. Conclusions This study has provided evidence of a methamphetamine withdrawal syndrome that can be categorized into two phases, the acute phase lasting 7-10 days during which overall symptom severity declined in a linear pattern from a high initial peak, and a subacute phase lasting at least a further 2 weeks.

The methanolic extract from the leaves of the Vietnamese medicinal plant Maesa balansae showed potent in vitro and in vivo activity against the tropical protozoal parasite Leishmania infantum. Bioassay-guided purification of the extract led to the identification of six triterpenoid saponins, maesabalides I-VI (1-6), each having a strong and specific anti-leishmanial activity. Maesabalide III (3) and IV (4) were the most potent with IC 50 values against intracellular amastigotes of about 7 and 14 ng/mL. In comparison, the IC 50 value of sodium stibogluconate, the reference drug for treatment of leishmaniasis, is only 5.6 µg/mL. No cytotoxicity was present on a human fibroblast (MRC-5) cell line (CC 50 > 32µg/mL). In vivo evaluation in the BALB/C mouse model demonstrated that >90% reduction of liver amastigote burdens was obtained 1 week after a single subcutaneous dose at 0.2-0.4 mg/kg was administered. Several chemical derivatives of maesabalides I-VI were prepared in order to study the structure-activity relationship.

Effects of principal saponins, chakasaponins I-III, from the flower buds of Camellia sinensis cultivated in Fujian province, China on plasma triglyceride (TG) and glucose levels in olive oil or sucrose-loaded mice were examined. Chakasaponins I-III at 50 and 100 mg/kg significantly inhibited increases in plasma TG and glucose levels. Furthermore, they prevented gastric emptying, suggesting that the former inhibitory effect is partly dependent on the inhibition of gastric emptying. In addition, the chemical structure of a new acylated oleanane-type triterpene oligoglycoside, chakasaponin IV, was elucidated on the basis of chemical and physicochemical evidence.

AaSmcr.-By means of activity-directed chromatographic fractionation using the 12-0tetradecanoylphorbol acetate (TPA)-induced edema test, two saikosaponins were isolated from the MeOH extract of Hetermotpba trgoliata leaves. They were identified as 16P,23-dihydroxy-13,28-epoxyolean-l l-en-3P-yl-[P-D-glucopyranosyl )1-[P-D-glucopyranosyl (1+3)f-f!-D-fucopyranoside E l f and 16P,23,28-trihydroxy-l la-methoxyolean-12-en-3f!-yl-[~-Dglucopyranosyl (1+2)]-[P-~glucopyranosyl (1+3)f-P-D-fucopyranoside 121. Compound 1

Two types of Barbarea vulgaris var. arcuata, the G-type and the P-type, differed in resistance to larvae of the diamondback moth (DBM) Plutella xylostella. Rosette plants of the G-type were fully resistant to the DBM when grown in a greenhouse or collected in the summer season, but leaves collected during the late fall were less resistant, as previously found for flea beetle resistance. The P-type was always susceptible. Extracts of resistant leaflets inhibited larval growth in a bioassay, and a growth-inhibiting fraction was isolated by activity-guided fractionation. A triterpenoid saponin (1) was isolated from this fraction and identified as 3-O-β-cellobiosyloleanolic acid from spectroscopic data and analysis of hydrolysis products. The decrease in resistance of the Gtype in the fall was correlated with a decrease in the level of 1, from 0.6-0.9 to <0.2 µmol/g dry wt. Compound 1 was not detected in the susceptible P-type. We conclude that 1 is correlated with the variable resistance of B. vulgaris foliage to the DBM.

Bacopa monnieri is an outstanding nervine tonic used for raising the mental performance. It helps in concentration, comprehension, recall and alertness, Brahmi is particularly beneficial as it aids in categorizing information in brain and its subsequent expression. Bacopa is also called as a natural antioxidant which may give details its neuroprotective role seen in the memory centers of the brain. Epilepsy is neuronal disorder characterized by learning, cognitive and memory impairments. The present review summarizes information concerning botany, chemistry and beneficial effect of Bacopa monnieri on epilepsy associated behavioral deficits.

The hemolytic activity of the dinoflagellate Cochlodinium polykrikoides from Bahía de La Paz, Gulf of California was investigated as part of the ichthyotoxic mechanism of this microalga. Two different kinds of erythrocytes, fish and human, were tested for the hemolytic assay. Since fatty acids have been associated with hemolytic activity in C. polykrikoides, the composition of fatty acids of this dinoflagellate was also analyzed. The concentration of C. polykrikoides causing 50% hemolysis (HE 50 ) was 4.88 and 5.27 Â 10 6 cells L À1 , for fish and human erythrocytes, respectively. According to the standard curve of saponin, an equivalence between the hemolytic activity of saponin and the dinoflagellate concentration was found with 1 lg saponin mL À1 equivalent to 1 Â 10 6 cells L À1 of C. polykrikoides. The polyunsaturated fatty acids: hexadecaenoic (16:0), docosahexaenoic (22:6 n3) and octadecapentaenoic (18:5 n3) were found in an abundance of $62% of total fatty acids.

Eccentric muscle contraction causes fibre injury associated with disruption of the myofibrillar cytoskeleton. The medicinal plant Panax ginseng C.A. Meyer, known for its therapeutic properties, was studied to explore its protective Ž . effects after eccentric contraction. A crude extract and a standardised extract G115 of different saponin compositions were tested as to their efficacy in reducing lipid peroxidation, inflammation and release of myocellular proteins after the Ž . realisation of an eccentric contraction protocol on a rat treadmill. Plasma creatine kinase CK levels were significantly reduced by approximately 25% after ingestion of both extracts of ginseng. Both extracts reduced lipid peroxidation by approximately 15% as measured by malondialdehyde levels. ␤-Glucuronidase concentrations and glucose-6-phosphate Ž . dehydrogenase G6PDH levels, which can be considered markers of inflammation, were also significantly reduced. The values of ␤-glucuronidase were increased from 35.9" 1.5 to 128.4" 8.1 in vastus and to 131.1" 12.1 U g y1 in rectus, the protection due to ginseng administration being approximately 40% in both muscles. Both extracts appeared to be equally effective in reducing injuries and inflammation caused by eccentric muscle contractions. ᮊ

Analysis of mitochondrial function is central to the study of intracellular energy metabolism, mechanisms of cell death and pathophysiology of a variety of human diseases, including myopathies, neurodegenerative diseases and cancer. However, important properties of mitochondria differ in vivo and in vitro. Here, we describe a protocol for the analysis of functional mitochondria in situ, without the isolation of organelles, in selectively permeabilized cells or muscle fibers using digitonin or saponin. A specially designed substrate/inhibitor titration approach allows the step-by-step analysis of several mitochondrial complexes. This protocol allows the detailed characterization of functional mitochondria in their normal intracellular position and assembly, preserving essential interactions with other organelles. As only a small amount of tissue is required for analysis, the protocol can be used in diagnostic settings in clinical studies. The permeabilization procedure and specific titration analysis can be completed in 2 h.

Fagonia indica is a small spiny shrub of great ethnopharmacological importance in folk medicine. The aqueous decoction of aerial parts is a popular remedy against various skin lesions, including cancer. We used a biological activity-guided fractionation approach to isolate the most potent fraction of the crude extract on three cancer cell lines: MCF-7 oestrogen-dependent breast cancer, MDA-MB-468 oestrogen-independent breast cancer, and Caco-2 colon cancer cells. A series of chromatographic and spectroscopic procedures were utilised on the EtOAc fraction, which resulted in the isolation of a new steroidal saponin glycoside. The cytotoxic activity of the saponin glycoside was determined in cancer cells using the MTT and neutral red uptake assays. After 24 h treatment, the observed IC 50 values of the saponin glycoside were 12.5 lM on MDA-MB-468 and Caco-2 cells, but 100 lM on MCF-7 cells. Several lines of evidence: PARP cleavage, caspase-3 cleavage, DNA ladder assays, and reversal of growth inhibition with the pan-caspase inhibitor Z-VAD-fmk, suggested stimulation of apoptosis in MDA-MB-468 and Caco-2 cells, but not in MCF-7 cells, which do not express caspase-3. The haemolytic activity of the saponin glycoside was confirmed in sheep red blood cells, with cell lysis observed at >100 lM, suggesting that, at this concentration, the saponin glycoside caused necrosis through cell lysis in MCF-7 cells. Using the DNA ladder assay, the saponin glycoside (12.5 lM) was not toxic to HUVEC (human umbilical vein endothelial cells) or U937 cells, indicating some selectivity between malignant and normal cells. We conclude that the steroidal saponin glycoside isolated from F. indica is able to induce apoptosis or necrosis in cancer cells depending on the cell type.

Medicinal plants constitute an important source of potential therapeutic agents for diabetes. The purpose of present study is to investigate the effect of root extract of Rosa rugosa Thunb. on inhibition of sucrase related to diabetes mellitus (DM). Bioassay-guided fractionation of the methanol extract led to the identification of 13 triterpenoid saponins (1-13). Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D, 2D NMR, and MS. The n-butanol fraction showed potent rat intestinal sucrase inhibitory activity with value of 87.62 ± 5.84 % inhibition compared to the positive control acarbose (50.96 ± 2.97 % inhibition at 0.02 mM). Subsequently, compounds 11-13 (1.0 mM) exhibited significant sucrase inhibitory activity, with inhibition percentage values of 41.17 ± 3.52, 46.80 ± 4.00, and 39.39 ± 4.19 %, respectively. Whereas, compounds 2-6, 8, and 10 showed moderate sucrase inhibitory activity (ranging from 13.26 ± 7.00 to 32.08 ± 6.04 % inhibition) at a same concentration. The data provide a starting point for creating new sucrase inhibitors, which may be useful for the development of effective therapies for the treatment of DM.

The aim of the study was to prepare cationic ISCOMs using cationic derivatives of the saponin Quil A. The polyamines ethylenediamine, spermidine and spermine were conjugated with the glucuronic acid moiety of Quil A. The aqueous solubility of the derivatives increased with decreasing pH, and the pK a values were between 6 and 7. The CMCs of the ionised derivatives were around 0.5-1.0 mg/mL. Using the method of hydration of freeze-dried monophase systems, the interaction of each of the Quil A derivatives with phosphatidylcholine and cholesterol, at a mass ratio of 4:4:2 and a pH of 3 and 7.4, was investigated. A few ISCOM-like structures were present in the systems prepared at pH 7.4, hence the ternary system of Quil A spermine derivative, phosphatidylcholine and cholesterol was further investigated at pH 7.4 using a variety of mass ratios. A relatively high number of cationic ISCOM-like structures were observed at the mass ratio of 6:2:2. These ISCOM-like structures were less homogeneous and more irregular in shape than ISCOMs prepared from unmodified Quil A. Colloidal particles with positive zeta potential were produced and may find application in the delivery of nucleic acids or anionic proteins.

Astragalus memebranaceus is used as immunomodulating agent in treating immunodeficiency diseases and to alleviate the adverse effects of chemotherapeutic drugs. In recent years, it has been proposed that Astragalus may possess antitumorigenic potential in certain cancer cell types. In this study, the anti-carcinogenic effects of Astragalus saponin extract were investigated in HT-29 human colon cancer cells and tumor xenograft. Our findings have shown that Astragalus saponins (AST) inhibit cell proliferation through accumulation in S phase and G2/M arrest, with concomitant suppression of p21 expression and inhibition of cyclin-dependent kinase activity. Besides, AST promotes apoptosis in HT-29 cells through caspase-3 activation and poly(ADP-ribose) polymerase (PARP) cleavage, which is indicated by DNA fragmentation and nuclear chromatin condensation. Nevertheless, we also demonstrate the anti-tumorigenic effects of AST in vivo, of which the reduction of tumor volume as well as pro-apoptotic and anti-proliferative effects in HT-29 nude mice xenograft are comparable to that produced by the conventional chemotherapeutic drug 5-fluorouracil (5-FU). In addition, the side effects (body weight drop and mortality) associated with the drug combo 5-FU and oxaliplatin are not induced by AST. These results indicate that AST could be an effective chemotherapeutic agent in colon cancer treatment, which might also be used as an adjuvant in combination with other orthodox chemotherapeutic drugs to reduce the side effects of the latter compounds.

Avicins are a class of natural saponins with selective pro-apoptotic activity in cancer cells. In this work, we studied the inXuence of avicins on metabolic state of rat liver mitochondria. Avicin-treated mitochondria underwent a signiWcant decrease in oxygen consumption rate that was completely restored by addition of exogenous cytochrome c. On the other hand, avicins increased the rotenone-insensitive oxidation of external NADH in the presence of exogenous cytochrome c, long before high amplitude swelling of mitochondria was observed. The increase in external NADH oxidation was cyclosporin A-insensitive. Avicin G signiWcantly accelerated hydroperoxideinduced oxidation of mitochondrial endogenous NAD(P)H, the drop of the inner membrane potential and the high amplitude swelling of mitochondria. The obtained data might explain selective induction of apoptosis in tumor cells by avicins. Based on other studies showing that tumor cells generate hydroperoxides with a very high rate, avicins could provide a new strategy of anticancer therapy by sensitizing cells with high levels of reactive oxygen species to apoptosis.

Aim of the study: Saponins from Helicteres isora have previously been shown to exert antidiabetic effects. The present study explored the underlying mechanisms in C2C12 skeletal muscle cells. Materials and methods: C2C12 cells were incubated with saponins and sapogenin followed by Western blotting and immunofluorescence analysis. Results: Western blotting revealed that incubation with saponins (100 g/ml) and sapogenin (100 g/ml) induced the phosphorylation of the phosphatidylinositol-3-kinase (PI3K) as well as of the downstream targets protein kinase B/Akt (at Ser473) and glycogen synthase kinase GSK-3␣/␤ (at Ser21/9) in a timedependent manner. In contrast, no phosphorylation of the AMP-sensitive kinase AMPK (at Thr172) was observed. Within 48 h saponins/sapogenin treatment further increased the protein abundance of the insulin-sensitive glucose transporter Glut4. Confocal microscopy confirmed that saponins/sapogenin treatment stimulated Akt phosphorylation and revealed that the treatment was followed by translocation of Glut4 into the cell membrane of C2C12 muscle cells. Conclusions: Saponins and sapogenin activate the PI3K/Akt pathway thus leading to phosphorylation and inactivation of GSK-3␣/␤ with subsequent stimulation of glycogen synthesis as well as increase of Glut4-dependent glucose transport across the cell membrane.

Plasma membrane permeabilization by saponin and anticancer avicins was studied using light dispersion measurements, since high correlation between light dispersion changes and hemolysis has been demonstrated. Nevertheless, we observed that rat red blood cell swelling in moderately hypotonic media was accompanied by up to 20% decrease of light dispersion, when hemolysis was not yet detectable. Avicin G and avicin D were significantly more efficient than saponin in inducing cytotoxicity in PC3 human prostate cancer cells. We found that the preincubation of avicins with the plasma membrane, but not with the cytosolic fraction of previously lysed red blood cells, completely protected fresh cells against permeabilization. The data suggest that the plasma membrane can tightly bind the avicins, but not the saponin. Using the "osmotic protection" method with 100 mOsm PEGs of increasing molecular weight in isotonic media, the size of the pores generated by avicin G and avicin D in the plasma membrane was estimated to be higher than the hydrodynamic radius of PEG-8000. The obtained results indicate that the anticancer activity of avicin G and avicin D could be related, at least partially, to their high ability to permeabilize biological membranes. These data might represent interest for possible applications of these anticancer drugs in vivo.

Bioassay-directed fractionation of the dried roots of Asparagus cochinchinensis led to the isolation of a new spirostanol saponin, asparacoside (1), two new C-27 spirosteroids, asparacosins A (2) and B (3), a new acetylenic derivative, 3′′-methoxyasparenydiol (4), and a new polyphenol, 3′-hydroxy-4′-methoxy-4′dehydroxynyasol (6), as well as five known phenolic compounds, asparenydiol (5), nyasol (7), 3′′methoxynyasol (8), 1,3-bis-di-p-hydroxyphenyl-4-penten-1-one (9), and trans-coniferyl alcohol (10). Compounds 1, 6, and 8 demonstrated moderate cytotoxicities in a panel comprised of KB, Col-2, LNCaP, Lu-1, and HUVEC cells, with IC 50 values ranging from 4 to 12 µg/mL. The structures were determined by spectroscopic and chemical methods.

Macrostemonoside A, a newly found compound, is derived from Allium macrostemon Bung. However, investigation into its nature is lacking. In this study, the effects of macrostemonoside A on hyperglycemia, hyperlipidemia, visceral fat accumulation, and related enzyme activities in high-fat diet-fed C57BL/6 mice are examined. The results showed that mice fed with a high-fat diet had a significant increase in fasting blood glucose, liver glycogen, serum total cholesterol, and visceral fat accumulation, but were mildly or moderately inhibited by macrostemonoside A at a dose of 4 mg/kg/d after 30 days of treatment. This hypoglycemic effect might be associated with the potential increase in insulin sensitivity and visfatin expression, although it needs further validation in future studies. Its anti-obesity effect might be associated with elevated total lipase activity in visceral adipose cells. The up-regulation in the expression of peroxisome proliferators-activated receptor gamma 2 might be responsible for the increased lipase activity in visceral adipose cells. Furthermore, we supposed that its action mechanisms might promote energy metabolism in muscles. Macrostemonoside A, with its steroid-like structure, has no significant cortisone-like side effects on the immune system but has potential cardiovascular protective effects. These results suggested that a potential compound to treat hyperglycemia, hyperlipidemia, and visceral obesity could be developed. However, its underlying mechanisms need further investigation in future studies.

The biodegradability of water-extracted saponins of berries from the Endod plant, Phytolacca dodecandra L&#x27;Herit, was evaluated under OECD standardized conditions. Persistence of the saponins was evaluated by determination of saponin concentrations in water over a 30-day period, using a quantitative HPLC method and a semiquantitative hemolytic assay, which is considered a potential field method. The two methods were compared. Bioassays

Concentrated agave sap (CAS) has gained popularity as an unrefined sweetener. It is obtained by boiling "aguamiel" that contains phytochemicals with diverse bioactivities. Saponins have been the most widely studied agave phytochemicals due to their cancer antiproliferative effect but their concentration may vary due to maturity of the agave plant and collection site. In this study, 18 CAS samples produced in different states of Mexico were analyzed using multivariate methods to determine which physicochemical or phytochemical parameters were responsible for variation. Additionally, extracts with different saponin profiles were tested to determine possible correlations with antiproliferative activity. Total soluble solids, pH, and water activity were similar to those reported for other agave sweeteners. Antioxidant capacity of samples was correlated to browning index. Eleven steroidal saponins were found in CAS samples and they were the main source of variability. Magueyoside B, a kammogenin tetraglycoside, was the most abundant saponin in all samples. With respect to bioactivity, multivariate analysis indicated that magueyoside B and a gentrogenin tetraglycoside were compounds strongly related with bioactivity. CAS from Hidalgo, Puebla, and Veracruz had higher concentration of magueyoside B than from the other kamogenin tetraglycoside found in the samples from other Mexican states. These results could be used as a first approach to characterize and standardize CAS to validate the potential health benefits derived from its consumption.

Great interest in herbal medicine as a potential source of phytopharmaceuticals has created the need to review common factors responsible for major diseases and body disorders. This review shows one such common factor in inflammation and the role herbal medicine can play. Traditional medicinal herbal remedies in the southern African region have long been used to treat various pain-or inflammation-related symptoms. Although the precise mechanisms of action of many herbal drugs have yet to be determined, some of them have been shown to exert anti-inflammatory and/or antioxidant effects in a variety of cells in the human and animal bodies. There is increasing evidence to indicate that both peripheral and central nervous system cells play a prominent role in the chronic inflammatory responses in the body system and anti-inflammatory herbal medicine and its constituents are being proved to be a potent protector against various pro-inflammatory mediators in diseases and disorders. These mediators have therefore been suspected of being the functional basis of diseases and disorders. The structural diversity of these medicinal herbs makes them a valuable source of novel lead compounds against the therapeutic molecular targets, cytokines and mediators, that have been newly discovered by the platforms of genomics, proteomics, metabolomics and highthroughput technologies. This article reviews the basic mechanisms of inflammation and the potential of 123 southern African plant species to be effective as chronic inflammatory disease preventive agents. With one third of these species there are no indications of the chemical composition, indicating possible subjects for further research.

The thermochemical pretreatment by saponification of two kinds of fatty slaughterhouse waste -aeroflotation fats and flesh fats from animal carcasses -was studied in order to improve the waste's anaerobic degradation. The effect of an easily biodegradable compound, ethanol, on raw waste biodegradation was also examined. The aims of the study were to enhance the methanisation of fatty waste and also to show a link between biodegradability and bio-availability. The anaerobic digestion of raw waste, saponified waste and waste with a co-substrate was carried out in batch mode under mesophilic and thermophilic conditions.

Background: Carpobrotus edulis (Mesembryanthemaceae), also known as igcukuma in Xhosa language is a medicinal plant used by the traditional healers to treat common infections in HIV/AIDS patients. Based on this information, we researched on the plant phytoconstituents, as well as its inhibitory effect using aqueous and three different organic solvent extracts in order to justify its therapeutic usage. Methods: Antioxidant activity of the extracts were investigated spectrophotometrically against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) diammonium salt, hydrogen peroxide (H 2 O 2 ), nitric oxide (NO), and ferric reducing power, Total phenols, flavonoids, flavonols, proanthocyanidins, tannins, alkaloids and saponins were also determined using the standard methods.

From the leaves and roots of Polyscias fruticosa, eight new oleanolic acid saponins named polysciosides A to H were isolated together with three known saponins. The structures of the saponins were established by means of spectral data, particularly NMR, which included COSY, HSQC, HMBC, HOHAHA and ROESY techniques.

new triterpenoid saponin, bacoside A,, a constituent of bacosides, the saponin mixture of Bacopa monniera, was isolated and characterized. Its structure was established as 3-/i-[O-/l-D-glucopyranosyl(l-+3)-O-[a-Larabinofuranosy(1 +2)]-0-/?-D-glucopyranosyl)oxy] jujubogenin by chemical and spectral analyses. The cis-isomer of ebelin lactone was also obtained as one of the artefacts of the aglycone and its structure revised.

Ethnopharmacological relevance: Quillaja saponaria bark contains a high percentage of triterpene saponins and has been used for centuries as a cleansing and analgesic agent in Chilean folk medicine. Aim of the study: The topical and systemic analgesic effects of a commercial partially purified saponin extract, 3␤,16␣-dihydroxy-23-oxoolean-12-en-28-oic acid (quillaic acid), methyl 3␤,16␣-dihydroxy-23oxoolean-12-en-28-oate and methyl 4-nor-3,16-dioxoolean-12-en-28-oate. Materials and methods: The samples were assessed in mice using the topical tail-flick and i.p. hot-plate tests, respectively. Results: All the samples showed activity in both analgesic tests in a dose-dependent manner. The most active against tail flick test was commercial partially purified saponin extract (EC50 27.9 mg%, w/v) and more than the ibuprofen sodium. On hot-plate test, methyl 4-nor-3, 16-dioxoolean-12-en-28-oate was the most active (ED50 12.2 mg/kg) and more than the ibuprofen sodium.

The developments during 2002-2005 in the methods used for saponin analyses in plant material are presented. There were number of papers published on isolation and identification of new saponins by chromatographic techniques. Some new developments can be found in separation techniques or solid and mobiles phases used. Separation of individual saponins is still complicated and time consuming. This is due to the fact that in most of the plant species saponins occur as a multi-component mixture of compounds of very similar polarities. Thus, to isolate single compound for structure elucidation or biological activity testing, a combination of different chromatographic techniques has to be used, e.g. first separation of the mixture to simpler sub-fractions on reversed phase C18 has to be followed by further purification on normal phase Silica gel column. Especially difficult is determination of saponins in plant material as these compounds do not posses chromophores and their profiles cannot be registered in UV. Most HPLC methods apply not only specific registration at 200-210 nm, but these methods are not applicable for determination of many saponins in plant material at levels lower than 200-300 mg/kg. Some new or improved techniques for quantification of saponins in plant material were published in reviewed period. These include further progress in the application of evaporative light scattering detection (ELSD) for saponin profiling and quantification, which is also not only specific but also more sensitive in comparison to 200-210 nm detection. Some progress in development of new applications for liquid chromatography-electrospray mass spectrometry (LC/ESI/MS) for saponin determination has also been done. This method gives highest sensitivity and on line identification of separated saponins and should be recommended for specialized analyses of extracts and pharmaceutical formulas like the validation of a new assay. From non-chromatographic techniques for saponin determination, a sensitive and compound specific ELISA tests for some saponins were developed.

This study was conducted to evaluate the effect of adding Yucca Schidigera powder (Y.P) at levels of 50,100,150 and 200 mg/kg of rabbit diets as feed additive on growth performance, carcass traits, blood parameters and economical efficiency. A total of 60 growing male rabbits, 6 weeks of age, were divided into 5 dietary treatments of 12 rabbits each in three replicates (5×3×4).The diets were formulated to be iso-nitrogenous (18.02% Crude protein) and iso-energetic (2752 kcal DE/kg diet ).The experiment was terminated when rabbits were 14 weeks of age. Weight gain, feed intake, and feed conversion were calculated. At the end of the experiment, some blood plasma constituents and carcass characteristics were measured. Results showed that addition of Yucca Schidigera powder (Y.P) at level of 100 mg/kg of rabbits diet, significantly improved the final body weight, body weight gain, feed conversion and globulin level, red blood cells, white blood cells counts, packed cell volume in the blood plasma. Also, decreased abdominal fat and proved to be more economical than the other treatments and the control group. assuming control treatment = 100%.

Results from the in vitro antiamoebic activity of some Congolese plant extracts used as antidiarrhoeic in traditional medicine indicated that of 45 plant extracts tested, 35 (77.78%) exhibited an antiamoebic activity and 10 (22.22%) were inactive. The highest activity (MICB 100 vg/ml) was obtained with extracts from root bark of Paropsia brazzeana, Cryptolepis sanguinolenta, Alchornea cordifolia, Hensia pulchella, Maprounea africana, Rauwolfia obscura and Voacanga africana, leaves and stem bark of Psidium guaja6a, stem bark of Dialum englerianum, Harungana madagascariensis and Mangifera indica, mature seeds of Carica papaya, and leaves of Morinda morindoides and Tithonia di6ersifolia. Metronidazole used as reference product showed a more pronounced activity than that of all plant extracts tested.

Pure analytical standards for the major saponins present in processed soy products, the group B saponins (soyasaponins I, II, III and IV), were isolated in mg quantities by a combination of processing, precipitation! re-solubilisation, TLC and preparative HPLC. These standards were determined to be pure by LC-ESIIMS analvsis and NMR. The standards were used to perfect a facile analytical HPLC method using spectrometric dete~tion to determine the percent composition of the group B soyasaponins in various products from processing of soybean.

Saponins, amphiphiles of natural origin with numerous biological activities, are widely used in the cosmetic and pharmaceutical industry. Some saponins exhibit relatively selective cytotoxic effects on cancer cells but the tendency of saponins to induce hemolysis limits their anticancer potential. This review focused on the effects of saponin activity on membranes and consequent implications for red blood and cancer cells. This activity seems to be strongly related to the amphiphilic character of saponins that gives them the ability to self-aggregate and interact with membrane components such as cholesterol and phospholipids. Membrane interactions of saponins with artificial membrane models, red blood and cancer cells are reviewed with respect to their molecular structures. The review considered the mechanisms of these membrane interactions and their consequences including the modulation of membrane dynamics, interaction with membrane rafts, and membrane lysis. We summarized current...

Kidney beans (Phaseolus vulgaris L.), are common legumes, consumed worldwide. The delicacy of kidney beans is highly appreciable but, at the same time, their toxicity has raised an alarming concern. Kidney bean toxicity may be divided into two subcategories: toxicity caused by its lectins, saponins, phytates, and protease inhibitors or allergenicity induced by its allergenic proteins. The purpose of this review is to unravel the facts behind the different aspects of toxicity and allergenicity induced by kidney beans and try to fill the gaps that exist currently.

A novel HPLC-UV method has been developed for the fingerprint analysis of the steroidal saponins in the rhizomes of three Ruscus species (Ruscus aculeatus, Ruscus hypoglossum and Ruscus colchicus). Saponins were identified by HPLC-ESI-MS. During the study a new major saponin was detected in the rhizomes of R. hypoglossum and R. colchicus. The structure of the new compound was defined as 1-O-wa-L-rhamnopyranosyl-(1™2)-6-Oacetyl-b-D-galactopyranosylx-1b,3b,22j,26-tetrahydroxy-furost-5(6)-en-26-O-b-D-glucopyranoside (8) by spectral analysis. ᮊ

From the leaves of Viburnum tinus L. (Adoxaceae) two acylated iridoid glucosides (viburtinoside A and B), a coumarin diglucoside scopoletin 7-O-b-D-sophoroside and a natural occurred dinicotinic acid ester 2,6-di-C-methyl-nicotinic acid 3,5-diethyl ester were isolated. In addition to these, 10 known compounds were isolated, namely two bidesmosidic saponins, a hexamethoxy-flavone and five flavonol glycosides, as well as suspensolide A and oleanolic acid were isolated for the first time in this genus and species, respectively. The structures were determined mainly by spectroscopic methods (UV, IR, ESI-MS, 1 H-, 13 C NMR and DEPT). Toxicity of the investigated extract was determined (LD 50 = 500 mg/kg). CCl 4 -induced hepatotoxicity has been evaluated in terms of the determination of alanine aminotransferase (ALT), aspartate aminotransferase (AST), lipid peroxide and nitric oxide levels in serum and compared using adult male rats weighing 150-180 g. Their highly elevated levels were significantly reduced by treatment with the investigated aqueous methanol extract in dose-dependant manner.

A new steroidal saponin named diurnoside I has been isolated from a methanolic extract of fresh leaves of Cestrum diurnum and the structure, (25 R)-5~t-spir~stan-3 fl-y~-4-~-~ [ 2-~-(~-D-g~uc~pyran~sy~)-~-D-g~uc~pyran~sy~]-3-O-[fl-D-xylopyranosyl]-fl-D-glucopyranosyl}-fl-D-galactopyranoside, was determined by modern NMR techniques and chemical reactions.

We isolated a new saponin named codonoposide (1) from the roots of Codonopsis lanceolata (Campanulaceae) and characterized it as 3-O-[beta-D-xylopyranosyl(1-3)-beta-D-glucuronopyranosyl]-3beta,16alpha-dihydroxyolean-28-oic acid 28-O-[beta-D-xylopyranosyl (1-3)-alpha-L-rhamnopyranosyl (1-2)-alpha-L-arabinopyranosyl] ester by chemical, physicochemical, and 2DNMR techniques. Complete hydrolysis of 1 produced a sapogenin (1a), and the partial hydrolysis and further isolation afforded two prosapogenins (1b, 1c). The structures of 1a, 1b, and 1c were found to be 3beta,16alpha-dihydroxyolean-28-oic acid (echinocystic acid, 1a), 3-O-beta-D-glucuronopyranoside of 1a, and 3-O-beta-D-xylopyranosyl (1-3)-beta-D-glucuronopyranoside of 1a, respectively, on the basis of spectroscopic data. On MTT assay, 1a showed marginal cytotoxic activity whereas 1b exhibited more cytotoxicity than 1a. However, the bisdesmosylsaponin 1 exhibited no cytotoxicity (IC(50)&gt;0.3 mM against tested cell lines). This ...

Elaeagnus angustifolia was analyzed for determination of metals, phytoconstituents, bactericidal, fungicidal and insecticidal effects and to explore its chemical and biological potential. The root, branches, leaves, stem bark and root bark parts of E. angustifolia were found to contain iron, lead, copper, cadmium, zinc, chromium, nickel and cobalt in different concentrations. Crude extract of Elaeagnus angustifolia (Ea.Cr) was tested positive for the presence of alkaloids, flavonoids, saponins and tannins. Ea.Cr and its fractions, n-hexane (Ea.Hex), ethyl acetate (Ea.EtAc) and aqueous (Ea.Aq) showed bactericidal activity against Escherichia coli and Staphylococcus aureus, while against Pseudomonas aeruginosa only Ea.Hex and Ea.EtAc were effective. When tested for antifungal effect, Ea.Cr exhibited fungicidal action against Aspergillus fumagatus, Ea.EtAc and Ea.Aq against Aspergillus flavis and Ea.EtAc against Aspergillus niger. Ea.Hex was active against all three fungal strains. The chloroform fraction (Ea.CHCl 3 ) was found inactive against the used microbes. Ea.Cr, Ea.Hex, Ea.CHCl 3 , Ea.EtAc and Ea.Aq caused mortality of Tribolium castaneum and Ephestia cautella insects observed after 24 and 48 h of treatment. These data indicate that E. angustifolia exhibits different heavy metals and compound groups. Methanolic extract of E. angustifolia and its various fractions possess antibacterial, antifungal and insecticidal activities, which elucidate medicinal application of the plant.

Analysis of saponins by thin layer chromatography (TLC) is reported. The solvent system was n-butanol:water:acetic acid (84:14:7). Detection of saponins on the TLC plates after development and air-drying was done by immersion in a suspension of sheep erythrocytes, followed by washing off the excess blood on the plate surface. Saponins appeared as white spots against a pink background. The protocol provided specific detection of saponins in the saponins enriched extracts from Aesculus indica (Wall. ex Camb.) Hook.f., Lonicera japonica Thunb., Silene inflata Sm., Sapindus mukorossi Gaertn., Chlorophytum borivilianum Santapau & Fernandes, Asparagus adscendens Roxb., Asparagus racemosus Willd., Agave americana L., Camellia sinensis [L.] O. Kuntze. The protocol is convenient, inexpensive, does not require any corrosive chemicals and provides specific detection of saponins.

Quantitative thin layer chromatography was used to estimate the saponin content of 20 common food plants and also of foods prepared from some of them. The food plants found to be richest in saponins weie chickpeas (Cicer arietinum), soya beans (Cl-vcine max), lucerne (alfalfa) sprouts (Medicago sutivu) and varieties of Phuseolus vulgaris (navy beans, haricot beans, kidney beans). Saponins were not destroyed by processing or cooking. They were present in falafels (prepared from chickpeas), canned baked beans, canned broad beans and protein isolate from faba beans. However, the saponin content of a fermented soya bean product (tempe) was only half that of whole soya beans. Guar meal (Cyamopsis tetragonolobiw) contains saponins but only a trace could be detected in samples of guar gum.