Cosmeceutical Containing Herbs - Fact, Fiction and Future

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Cosmeceuticals Containing Herbs: Fact, Fiction, and Future

CARL THORNFELDT, MD, FAAD

Private practice, CT Derm, PC, Fruitland, Idaho; Oregon Health Sciences University, Portland, Oregon; EpiSciences,
Inc., Boise, Idaho

BACKGROUND. Modern medicine is rooted in ethnobotanical tra- METHOD . English-language medical journal and symposium
ditions using indigenous flora to treat symptoms of human dis- searches.
eases or to improve specific aspects of the body condition. Herbal RESULTS. The most important botanicals pertaining to dermato-
medicine is now used by over half of the American population. logic uses, such as cosmeceuticals, include teas, soy, pomegran-
Yet the American medical community generally lacks knowledge ate, date, grape seed, Pycnogenol, horse chestnut, German
of the function, metabolism, interaction, adverse reactions, and chamomile, curcumin, comfrey, allantoin, and aloe. All are doc-
preparation of herbal products. umented to treat dermatologic conditions. Only green and black
OBJECTIVE. Because over 60 botanicals are marketed in cosme- tea, soy, pomegranate, and date have published clinical trials for
ceutical formulations, dermatologists need to obtain working the treatment of parameters of extrinsic aging.
knowledge of the major botanicals. The preparation, traditional CONCLUSIONS. Preparation of botanical-based cosmeceuticals is
uses, mechanisms of action, human clinical data, adverse reac- complex. Very few of these products are supported by evidence-
tions, and interactions all impact herbal efficacy and are dis- based science.
cussed below.

CARL THORNFELDT, MD, FAAD, HAS INDICATED NO SIGNIFICANT INTEREST WITH COMMERCIAL
SUPPORTERS.

THE FOUNDATION of modern pharmacologic medicine must have a working knowledge of botanicals to provide
is rooted in ethnobotanical traditions using indigenous optimal medical care.
flora. Over 200 indigenous medicinals were listed in the Several botanical treatments for cutaneous diseases
first U.S. Pharmacopeia in 1820, including podophyllin have stood the test of time for their effectiveness, as docu-
resin, white willow bark, wintergreen, and juniper tar, mented by modern scientific evidence. Podophyllotoxin is
which are still used today.1 a prescription purified podophyllin resin, a galenic extract
Botanicals used for medicinal, flavoring, or fragrances of mayapple (Podophyllum peltatum). Capsaicin is a non-
are known as herbs.1,2 The guiding principle of herbal prescription therapy for pruritis and pain extracted from
medicine is that the naturally occurring mixture of active cayenne peppers (Capsicum species). Henna (Lawsonia
compounds in plants is more effective and safer than indi- inermis) is a hair dye used by people sensitized to other
vidual molecules and manufactured combinations of syn- commercial coloring agents.4
thetic molecules. The natural composition is the commin-
uted, powdered, or galenic extracts of the whole or specific
Scientific Issues
anatomic parts of the plant. Botanical medicinals are
focused more on the treatment of signs and symptoms of Herbal medicine plays a vital role in current American
disease, while improving the total “body condition,” than health care by (1) providing alternatives to prescription
the etiology. medications, (2) enhancing the therapeutic effects of other
Botanical sales in 2002 in the United States exceeded prescriptives, (3) protecting against adverse reactions to
$4.3 billion and grew by one-third over only 6 years. allopathic therapy, and (4) providing treatment for dis-
Echinacea was the largest selling botanical in 2002, with eases for which there is no current prescription therapy or
sales of nearly $190 million. Botanical product growth has only poorly effective or high-risk therapy. Herbal and
flourished to now consume 25% of all health- and other alternative medical strategies are used by over half of
lifestyle-related dollars.3 Now over 60 different botanicals the population, especially by those suffering from chronic
are formulated into cosmeceuticals. Thus, dermatologists diseases, such as psoriasis; those with less hope for a cure,
such as human immunodeficiency virus (HIV); and those
with terminal diseases.5,6 Extensive public use of comple-
Address correspondence and reprint requests to: Carl Thornfeldt, mentary and alternative medicine resulted in the National
MD, FAAD, CT Derm, PC. 811 NW 12th Street, Fruitland, ID Institutes of Health establishing the Office of Alternative
83619, or e-mail [email protected]. Medicine in 1995.1

© 2005 by the American Society for Dermatologic Surgery, Inc. • Published by BC Decker Inc
ISSN: 1076–0512 • Dermatol Surg 2005;31:873–880.
874 THORNFELDT: COSMECEUTICALS CONTAINING HERBS Dermatol Surg 31:7 Part 2:July 2005

Unfortunately, two major myths taint herbal medicine. distillates that can be easily added to a cosmetic formula-
Most patients believe the myth that there are no side tion. However, this processing may destroy or adversely
effects because herbal medicine uses “natural substances.” modify some of the physiologically active molecules. The
In fact, experienced Chinese practitioners are concerned results are oil, wax, juice, tincture, decoction, tea, infu-
about the well-known side effects of hepatotoxicity and sion, and/or powders, which are then formulated into top-
contact dermatitis with oral and topical Chinese herbal ical applications, including solutions, gels, lotions, creams,
medicinals and preparations, respectively.7 ointments, and pastes. Some of these preparations are fur-
Many allopathic physicians believe the myth that ther applied as fomentation, a compress, or a poultice.2 See
double-blinded, placebo-controlled studies do not exist the glossary in Table 1. 9
for traditional medicines. Yet there are many such studies The concentration of the herb, its extract, and the active
conducted throughout Asia and India, including studies molecules affects therapeutic activity. Usually in cosme-
investigating the mechanisms of action of the medicinal ceuticals, the medicinal botanicals are added in very small,
botanicals.7 subtherapeutic amounts for the marketing story. Few
Chinese medicine herbs must be used cautiously herbs, unlike most synthetic pharmaceuticals, are required
because in Taiwan, 40% were adulterated with cortico- only in a very low concentration to provide the desired
steroids, nonsteroidal anti-inflammatory drugs, and/or effect because their high potency is so high. Herbal efficacy
central nervous system medicines. Over 50% of the Chi- is first challenged by the stratum corneum permeability
nese herbal medicines have two or more of these synthet- barrier. Delivery across the mucocutaneous surface is dif-
ics.8 ficult owing to the botanical’s multiple active compounds
The understanding of the function, metabolism, and with different solubility, polarity, and therapeutic concen-
interaction of these medicinal botanicals is often lacking. tration, as well as the reactivity of different mucocuta-
The specific scientific issues include documenting (1) com- neous targets.
plete characterization of the multiple active compounds in These complex biologic science and formulation issues
each plant source; (2) the activity and synergistic or addi- indicate that the only validation of herbal activity in a
tive interaction of each of these compounds and their cosmeceutical formulation is a human clinical trial con-
metabolites; (3) interaction of these active components ducted by a reputable third-party researcher. Without such
with food, nutrients, nutritional supplements, and other studies, health care providers and the public are being
medicines; and (4) how the potential toxicity of specific asked to trust in products based on “voodoo” science.
compounds is reduced.2 For example, ricin, a bioterrorist
weapon, and azelaic acid, a nontoxic prescription derma-
tologic medicine, are both extracted from the castor bean.
Table 1. Glossary

Preparation of Herbs Antiphlogistic: preventing and/or relieving inflammation


Astringent: arrests secretions, contracts tissue, and controls
Botanicals must undergo a significant amount of chemical bleeding
processing prior to incorporation into a cosmeceutical, Comminuted: whole plant or portion broken into multiple
and this processing greatly affects the biologic activity of pieces
the botanical. The most important factor for the biologic Decoction: liquid extract produced by simmering the plant
activity of an herb to be incorporated into a cosmeceutical part in water for over 20 min
product is the source of the plant material because each Elixir: sweetened alcohol extract
plant part may contain hundreds of different individual Essential oil: concentrated oil from the whole plant, usually
chemicals and molecules. Growing conditions, including volatile and fragrant
soil composition, amount of available water, climate vari- Fomentation: liquid extract–soaked cloth
Galenic: crude plant remedies
ations, plant stress, and harvesting conditions, such as
Herb: botanical used for medicine, flavoring, or fragrance
time from harvest to transport, care of plant materials dur-
Infusion: liquid extracts combined in hot water
ing shipping, storage conditions prior to manufacture, and Mucilage: botanicals that swell with exposure to water for
preparation of the herb and final product, as well as mix- soothing application
ing with other herbs, are other factors that may substan- Poultice: liquid extract combined with powdered herb applied
tially alter solubility, stability, biologic availability, phar- directly to lesions while mass is moist
macokinetics, pharmacologic activity, and toxicity. Rubefacient: substance that causes cutaneous erythema by
Galenic extracts are made from leaves, roots, fruits, counterirritant effects
berries, stems, twigs, barks, and flowers by crushing, Tea: dried whole or parts of plant simmered in hot water,
grinding, comminuting, boiling, distilling, pressing, dry- usually 5–10 min
ing, or exposing them to solvents. Usually, the plant mate- Tincture: alcoholic solution of whole or portion of plant or
extract
rial is heated or processed to obtain essential oils or other
Dermatol Surg 31:7 Part 2:July 2005 THORNFELDT: COSMECEUTICALS CONTAINING HERBS 875

Regulation Even simple plants contain multiple reactive and inter-


active compounds, but natural medicine advocates and the
Medicinal botanicals used in cosmeceuticals are consid-
media frequently do not warn the public of the impor-
ered food additives or dietary supplements by the US Food
tance of interactions between different herbs and between
and Drug Administration (FDA), which declared them as
herbal and prescription medicines. Moreover, 70% of
safe. The herbs are allowed to be marketed to consumers
patients fail to disclose their use of herbal products pre-
directly without obtaining drug status or being restricted
operatively.13 Interactions with medical consequences
by FDA’s over-the-counter monograph requirements.
probably are underreported. There are many herb-food,
Thus, no standards of herbal potency, concentration in the
herb-drug, and herb-herb interactions, as shown in
marketed product, safety, or efficacy studies exist.
Table 3. 4
The regulatory authority for herbs in Germany is the
“Commission E.” It is the best consensus of experts for Table 2. Adverse Cutaneous Reactions
weighing the quality of clinical evidence and systemic and
topical safety to identify reasonably effective uses of over Anaphylaxis
German chamomile (Matricaria recutita) and horse
300 botanicals.
chestnut (Aesculus hippocastanum)
For those herbs or indications not considered by Com-
Blistering (immunoglobulin A linear dermatosis)
mission E, one of the most complete herbal compendiums Tea tree (Melaleuca alternifolia)
is the PDR for Herbal Medicines.4 This publication com- Carcinogenic
pleted an exhaustive literature review conducted by the Aloe vera (Aloe barbadensis) and comfrey (Symphytum
respected PhytoPharm US Institute of Phytopharmaceuti- officinale)
cals for approximately 400 more herbs with regard to their Cutaneous, nonspecific
use and adverse reactions. Tea tree
Death
Safety Comfrey
Dermatitis
A news magazine in 2001 revealed that over 2,900 adverse German chamomile, horse chestnut, and tea tree
events requiring medical care were attributed to herbs dur- Dermatitis, allergic contact
ing the previous year. In addition, 104 deaths were attrib- German chamomile and tea tree
uted primarily to ephedra, St. John’s wort, ginkgo, and Edematous
ginseng.10 In 2003, the FDA removed ephedra and ma Aloe vera
huang (Ephedra sinica) from the market owing to 155 Erythematous
Horse chestnut
deaths directly attributed to it.11
Erythema multiforme
The most common adverse cutaneous reactions to Tea tree
herbal products include allergic and/or irritant contact Fasciculation
dermatitis. Cross-sensitivity to the most sensitizing botan- Horse chestnut
icals is not uncommon. For example, 12 of 106 dermatitis Hypesthesia
patients had a positive patch test to tea tree oil (TTO), and Tea tree
all of these patients had positive reactions to 1 or more of Mucositis/stomatitis
12 other natural compounds, including lavender (Lavan- Horse chestnut
dula angustifolia).12 Severe cutaneous reactions include Pruritis
angioedema/urticaria, exfoliative erythroderma, linear Horse chestnut
immunoglobulin A bullous dermatosis, lupus erythemato-
sus, malignancies, pemphigus, Stevens-Johnson syndrome, Table 3. Herb-Drug Interactions
Sweet’s syndrome, ulcerative stomatitis, and vasculitis.4
Aloe
Ten herbs used to treat dermatologic conditions have
Antiarrhythmics (aloe-induced hypokalemia may affect
induced fatal reactions, including aristolochia (Aris-
cardiac rhythm), digitalis glycosides (increases effect),
tolochia species), arnica (Arnica montana), cayenne (Cap- corticosteroids, thiazide diuretics, and licorice (increased
sicum annuum), comfrey (Symphytum officinale), henna potassium loss)
(Lawsonia inermis), kava kava (Piper methysticum), German chamomile
mistletoe (Phoradendron species), rue (Ruta species), Alcohol or benzodiazepines (may increase sedative effect),
senna (Cassia species), and yohimbine (Pausinystalia warfarin (may be additive)
yohimbe). Other severe reactions include anaphylaxis, Green tea
coma, rhabdomyolysis, and shock. Herbs known to pose Alkaline drugs (decreased absorption)
dermatologic surgery dangers include St. John’s wort, Horse chestnut
ginkgo, ginseng, garlic, echinacea, kava, and valerian.13 Anticoagulant drugs (may be additive with anticoagulant
drugs)
See the adverse reactions listed in Table 2.
876 THORNFELDT: COSMECEUTICALS CONTAINING HERBS Dermatol Surg 31:7 Part 2:July 2005

The medicinal botanicals of proven and potential der- John’s wort, tea tree, and oolong tea. Borage, evening
matologic significance are listed in Table 4.4 Multiple primrose, gotu kola, grape seed, black tea, PYC, and Chi-
herbs are effective for several different indications. Herbal nese herbal mixtures have been documented to treat der-
medicines may be divided into several groups. Clinically matologic conditions when administered orally. The
validated ones have published human-controlled clinical botanicals discussed include teas, soy, pomegranate, date,
trials. These herbs are among the most commonly used by grape seed, PYC, horse chestnut, tea tree, German
the public and alternative medicine practitioners and chamomile, curcurmin, comfrey, allantoin, and aloe vera.
would be expected to be the most commonly used in cos-
meceuticals. Photoaging clinical trials have been published
only on green and black tea, soy, pomegranate, and date. Specific Herbs
Those botanicals with published human studies for der- Allantoin and Comfrey (Symphytum officinale)
matologic conditions using topical formulations include
allantoin and comfrey, aloe, anise, bitter orange, black Comfrey is approved by the German Commission E to
nightshade, black seed, camptotheca, curcumin, German treat blunt injuries owing to the activity of triterpene
chamomile, grape seed, horse chestnut, lemon balm, neem, saponins, tannins, and silicic acid, as well as allantoin.4
olive oil, onion, Oregon grape, Pycnogenol (PYC), St. Allantoin has been extracted from the comfrey root and
leaves but is now commercially manufactured. Allantoin is
Table 4. Herbal Indications an antiphlogistic, antioxidant, and soothing keratolytic
that has an antitrichomonal effect and induces cell prolif-
Acne eration. It is listed in the FDA over-the-counter mono-
German chamomile (Matricaria recutita) and tea tree graph as a safe and effective skin protectant at 0.1 to
(Melaleuca alternifolia) 2.0%.14 Allantoin and/or comfrey–based products are
Bites used to treat wounds, ulcers, burns, dermatitis, psoriasis,
Tea tree impetigo, and acne. When formulated with surfactant and
Bruises
benzalkonium chloride, it is an effective hand sanitizer and
Comfrey (Symphytum officinale), horse chestnut (Aesculus
hippocastanum), and turmeric (Curcuma longa)
onychomycosis therapy.15
Burns Comfrey contains hepatotoxic pyrriolizidine alkaloids,
Tea tree which have resulted in deaths with oral consumption. It is
Carcinoma, squamous cell prevention of carcinogenic and contraindicated in pregnancy and lacta-
Green tea tion.4
Furunculosis/abscess Allantoin formulated with onion (Allium cepa) extract
German chamomile in a proprietary topical formulation improved the signs
Hemorrhoids and symptoms of scars and keloids.16 No photoaging clin-
Horse chestnut ical trials using topical allantoin and/or comfrey have been
Infections, fungal published.
Aloe (Aloe barbadensis, A. capensis, A. vera)
Infections, bacterial and mixed organisms/cellulitis/erysipelas
Tea tree Aloe (Aloe barbadensis, A. capensis, A. vera)
Inflammation
German chamomile, horse chesnut, and Aloe is used in Asian medicine for therapy of fungal and
turmeric other infections, infestations, tumors, and other skin dis-
Leprosy eases. The aloe substance released from comminuted leaves
Turmeric contains mucopolysaccharides; glucomannan, including
Mucocutaneous pain beta mannan; allantoin; anthracenes, such as aloin and
Comfrey
emodin; alkylchromone, including aletinic acid and choline
Mucocutaneous pruritus
Turmeric
salicylate; flavonoids; amino acids; hydroxyquinine glyco-
Stomatitis sides; carboxypeptidases; and minerals.4,17 The hydroxyan-
German chamomile, tea tree, and turmeric thraquinone emodin inhibits neuroectodermal tumors,
Ulcers, skin/decubitus, leg, vascular such as Merkel cell carcinoma.18 Acetylated mannans and
Tea tree lectins appear to have immunomodulatory effects. Aloe is
Venous insufficiency/varicosities/venous stasis antibacterial to Staphylococcus aureus, Helicobacter
Horse chestnut pylori, and dermatophyte fungus.19 It is viricidal to herpes
Wound care simplex and varicella zoster and is clinically effective in
Date palm (Phoenix dactylifera), German chamomile, and treating genital herpes. This herb inhibits thromboxane
turmeric vasoconstriction. Aloe inhibits photoimmunosuppression
Dermatol Surg 31:7 Part 2:July 2005 THORNFELDT: COSMECEUTICALS CONTAINING HERBS 877

of ultraviolet B (UVB) and inhibits cyclooxygenase for anti- German Chamomile


inflammatory effects. It also increases collagen biosynthe-
Matricaria recutita functions as an antiallergic, antimicro-
sis and degradation in granulation tissue. The antineopla-
bial, anti-inflammatory, antioxidant analgesic and was
sia effect is improved with melatonin and ascorbic acid.20
approved by the German Commission E for inflammatory
Aloe vera applied topically is accepted therapy for radia-
mucocutaneous diseases and wound and burn therapy.
tion and stasis dermatitis and ulcers, frostbite, burns, fun-
The major components of German chamomile include the
gal and bacterial infections, cold sores, pruritis, pain, pso-
primary anti-inflammatory agents: alpha-bisabolol,
riasis, and contact irritant dermatitis. The latter two were
chamazulene, levomenol, and matricine. Other active
documented in blinded studies.21–23
compounds include bisaboloxides; farnesenes; choline;
No photoaging clinical studies using topical aloe vera
glycosides; flavonoids, such as apigenin and rutin; tannins;
have been published, despite its use as one of the two most
hydroxycoumarins, such as umbelliferone; mucilages; sac-
common extracts in skin care formulations. The health
charides; fatty acids; and salicylates.23,27
risks of aloe are cutaneous eruptions and mutagenicity.4,18
Chamazulene inhibits leukotriene B4 synthesis via inhi-
It is contraindicted in pregnancy and lactation.4,23
bition of lipoxygenase and cyclooxygenase, lipid peroxi-
dation, leukocyte infiltration, and histamine release. Lev-
Curcumin Derived from Turmeric (Curcuma omenol is an anti-inflammatory hydrating agent that
domestica) diminishes the signs of photodamage and reduces pruritis.
Apigenin inhibits adhesion molecules. Bisabolol promotes
This herb is used in Asian medicine for cutaneous inflam-
granulation tissue.23,27
mation, pruritis, wounds, and ulcers. Its active compounds
Clinical studies showed that topical chamomile cream
include volatile oils, such as tumerone; curcuminoids; and
was superior to 0.5% hydrocortisone in treating dermati-
heptanoids. Tumerone, the volatile oil, provides the
tis and sunburn and statistically significantly decreased the
unique aroma. This extract provides the yellow color and
wound area and healing time.2 This herb is administered as
much of the flavor for curry in foods.4 These molecules
an oil for infusion, tea, ointment, gel, wash, gargle, or cap-
provide antioxidant, antitumor, antimicrobial, antifertility,
sule.4
and anti-inflammatory effects. They also repel insects.
Chamomile is a member of the Compositae family and
Curcumin may color cosmeceuticals claiming to be free of
has a significant risk of contact sensitization, conjunctivi-
artificial ingredients. Tetrahydrocurcumin, a hydrogenated
tis, angioedema, and anaphylaxis. It also has an additive
form of curcumin, is only off-white in color. It is also
anticoagulant effect to warfarin.4
added to cosmeceuticals to protect the formulation and
impact the skin. This antioxidant appears to be superior to
tocopherol.
Grape Seed (Vitis vinifera)/PYC/OPCs
Five human studies have found curcumin to be safe and
have found definite anti-inflammatory effects. It inhibits The pharmacologic activity of grape seed extract, along
lipoxygenase, cyclooxygenase, leukotrienes, thrombox- with French maritime pinebark (Pinus pinaster) extract,
ane, prostaglandins, nitric oxide, tumor necrosis factor, primarily resides in the potent antioxidant proantho-
and interleukin-12. Curcumin has been documented to cyanidins. These are the two richest natural sources and
inhibit collagenase, elastase, and hyaluronidase.24 the most commercially viable. Other rich natural sources
Clinical studies demonstrating the effects on parameters include green and black tea, red wine, red apple, red cab-
of photoaging are lacking, but when combined with bage, black currant, sangre de drago, bilberry, blackberry,
another herb, curcumin effectively treated scabies.25 blueberry, strawberry, black cherry, cranberry, peanut
skins, almonds, cocoa, parsley, onions, legumes,
hawthorn, and witch hazel bark.4,23 The standardized
Date Palm (Phoenix dactylifera)
pinebark extract is patent-protected PYC, which has been
This food stuff is an Asian medicine therapy for inflamed the generic term for proanthocyanidins. These polypheno-
wounds. The active compounds include 50% sugars, such lic bioflavonoids are also known as procyanidins, pro-
as saccharose; 10% fatty oils; oligomeric proanthocyani- cyandiol oligomers, leukoanthocyanidins, condensed tan-
dins (OPC); piperidine derivatives, including pipecolic acid; nins, and OPCs.28,29 OPCs consist of dimers of catechins
and phytohormones. It has no reported health hazards.4 and oligomers of epicatechin and catechin and their gallic
A placebo-controlled trial with 5% date versus placebo acid esters. These compounds are scavengers of both reac-
in 10 patients was applied to the eyelid area twice daily for tive oxygen and nitrogen species.23,28 Grape seed also
5 weeks. A statistically significant reduction in wrinkle includes other therapeutic compounds, including
surface (27.6%) and wrinkle depth was achieved. Six of flavonoids, such as kaempferol and quercetin glucosides;
the participants said that visual improvement occurred.26 stilbenes, such as resveratrol and viniferins; fruit acids;
878 THORNFELDT: COSMECEUTICALS CONTAINING HERBS Dermatol Surg 31:7 Part 2:July 2005

tocopherols; essential fatty acids; and phenylacrylic acids, The health risks of horse chestnut include hepatotoxic-
such as caffeoyl and feruloylsuccinic acid. Resveratrol is a ity, renal toxicity, urticaria, anaphylaxis, and mucocuta-
potent antioxidant that inhibits angiogenesis and carcino- neous irritant dermatitis. It may also interact with salicy-
genesis, is antiviral against herpes, and has phytoestrogen lates and warfarin. This herb is administered as a tea, a
activity.23 PYC also contains monomeric epicatechin and tincture for infusion, a gel, or an ointment.4
catechin.4,28,30
Grape seed applied topically improved cutaneous pho-
Pomegranate (Punica granatum)
toprotection to UVB, inhibits histamine synthesis, pro-
motes wound healing, reduces apoptosis induced by This herb was used in ancient Egypt for inflammation of
chemotherapy, reduces vascular engorgement, is cytotoxic the skin, mucosa, and joints. Punica granatum may con-
to adenocarcinoma, and inhibits Streptococcus. Grape tain a more potent antioxidant mixture than grape seed
seed protects deoxyribonucleic acid (DNA) against oxida- extract, PYC, red wine, or green tea. The major con-
tion more effectively than vitamins C and E and stabilizes stituents are tannins (25–28%), including punicalagin;
collagen and elastin by inhibiting matrix metallopro- polyphenols, such as ellagic acid; ascorbic acid; niacin;
teinases. It treats chronic venous insufficiency (CVI) and potassium; and piperidine alkaloids.4,23 Pomegranate func-
postoperative edema in clinical studies. All of these func- tions as an astringent that also inhibits NF-B.37 It has
tions of grape seed strongly suggest that it should improve documented antimicrobial activity for gram-negative bac-
photoaged skin and protect against further damage. Grape teria, Saccharomyces fungus, parasites, and viruses.38
seed has been used for centuries in Asia to treat a variety There are no health hazards reported with pomegran-
of cutaneous conditions.4,23,28–30 ate. It is administered as a decoction.4 Topical and oral
PYC increases nitric oxide levels, stimulates T- and B-cell administration of this herb induced photoprotection to
function, and inhibits nuclear receptor transcription factors UVB in a human clinical trial.39
nuclear factor B (NF-B) and activating protein (AP)-1
and the adhesion molecule intercellular adhesion molecule
Soy (Glycine soja)
1, as well as interferon-. It recycles vitamins C and E.23,30
Topically applied PYC reduces sunburn, immunosup- This antioxidant, antiproliferative, antiangiogenic extract
pression, and tumor formation by ultraviolet light while is used to treat hyperhidrosis in Asian medicine.23 Epi-
raising the minimal erythema dose in mice.31,32 PYC demiologic studies indicating much lower malignancy and
administered orally reduced the area of severity of cardiac disease rates in people eating a diet high in soy
melasma within 30 days and the signs and symptoms of resulted in thorough investigations revealing multiple
CVI by 60 days.33,34 medicinal uses. The major components of soy are phos-
A topical formulation consisting of grape seed, jojoba, pholipids (45–60%), such as phosphatidyl choline, and
lavender, rosemary, and thyme was used to treat alopecia essential fatty oils (30–35%). The minor components
areata. After 7 months of daily use, statistically significant include the most active compounds, such as isoflavones,
improvement in hair regrowth occurred (44% vs 15% for saponins, essential amino acids, phytosterols, calcium,
placebo).35 It has been used in antiaging creams for several potassium, iron, and the proteases soybean trypsin
years.23 No controlled clinical studies evaluating these inhibitor and Bowman-Birk inhibitor. The most potent
herbs for treatment of photoaging have been published. isoflavones are the phytoestrogens genistein and
daidzein.4,23,40 Topical estrogens have been shown to
increase skin thickness and promote collagen synthesis;
Horse Chestnut (Aesculus hippocastanum)
thus, soy phytoestrogen stimulation of human fibroblast
This herb is approved by the German Commission E for collagen synthesis is expected. Genistein is the most potent
CVI therapy. In homeopathy, horse chestnut treats hemor- antioxidant; it inhibits lipid peroxidation and chemical-
rhoids. The mechanisms of action include inhibition of elas- and UVB-induced carcinogenesis. The two protease
tase and hyaluronase, decreasing capillary permeability, inhibitors lighten pigmented lesions and reduce unwanted
inhibiting leukocyte activation, and inducing vasoncontric- facial and body hair in human clinical trials.40
tion. The active compounds in the seeds of this herb contain Soy products have rarely caused dermatitis and pruritis,
50% polysaccharides and oligosaccharides, other triterpene as well as asthma and gastrointestinal symptoms.4,23
saponins including aescin, the most active component, fatty
oils, and flavonoids, including quercetin and OPCs.4,23,36
Tea Tree (Melaleuca alternifolia)
Leg circumference, heaviness, and pain were statisti-
cally significantly reduced in multiple CVI trials with oral This essential oil has become one of the most commonly
therapy. Topically applied horse chestnut reduced the used nonprescription remedies for mucocutaneous disor-
symptoms of CVI in one trial and hemorrhoids in ders. TTO’s active compounds include terpinenes, such as
another.36 Photoaging clinical studies are lacking. cineole. The monoterpene terpinen is the major sensitizing
Dermatol Surg 31:7 Part 2:July 2005 THORNFELDT: COSMECEUTICALS CONTAINING HERBS 879

compound in TTO and has become one of the most com- pressed both type I and IV allergic reactions in the skin.47,48
mon contact allergens. The terpene alcohols, such as ter- Oral oolong tea effectively treated atopic dermatitis.49
pinin-4-ol, are the major constituents, comprising 40% of A recent double-blinded trial of 51 patients treated for
TTO. They reduce histamine-induced edema and wheal 12 weeks with topical green tea extract containing 5.5 to
volume in type I hypersensitivity reactions. TTO does not 8.5% EGCG did not reduce the number of actinic ker-
have antioxidant activity, nor does it suppress neutrophil atoses on forearms compared with placebo.50
superoxide.4 Its wide antimicrobial spectrum includes Pro- The major adverse reactions are gastrointestinal upset,
pionobacterium acnes, Escherichia coli, S. aureus, herpes constipation, irritability, and, very rarely, hepatotoxicity,
simplex, Candida albicans, Trichophyton dermatophytes, delirium, and seizures. Caution should be used during
and Sarcoptes scabiei.41,42 pregnancy and lactation with excessive consumption
Multiple double-blinded clinical trials have docu- (more than four cups per day).23
mented that TTO effectively treats acne and fungal or
yeast infections. TTO failed to effectively treat atopic der-
Summary
matitis and CVI.4,23,42
TTO is cytolytic to epithelial cells and fibroblasts, so it Although there is a sharp increase in the use of botanicals
should not be used for burns. Photodamaged TTO is a in cosmeceuticals, there is a paucity of human clinical
stronger sensitizer and has induced erythema multiforme studies and often a lack of sound scientific rationale. Proof
with topical application. Thus, the use of TTO in cosme- that the cosmeceutical formulation has any objective effec-
ceuticals for sun-exposed tissue is not scientifically sound.42 tiveness is also usually lacking. The most significant
human cosmeceutical data have been generated with for-
mulations containing green and black tea, soy, pomegran-
Teas: Black, Green, Oolong, and White (Camellia
ate, date, and a grape seed–based mixture. Cosmeceutical
sinensis)
formulations with the highest risk of reactions contain tea
All true teas are derived from Camellia sinensis. Black tea tree oil, comfrey, and German chamomile.
is the most processed (fermented), with white tea recently
supplanting green tea as the least processed; oolong is par-
Acknowledgments
tially fermented. Green tea contains 8 to 12% polyphenols
and 2 to 4% caffeine. White tea is a more potent antioxi- I greatly appreciate the assistance of Sheena Beavers,
dant and is more effective than green tea in inhibiting bac- David Talford, PA-C, Charity Burkheimer, and Elisha
terial dysplastic mutations.4,23,43 Green tea decreases Andrews with the manuscript.
melanoma cells in tissue culture and squamous cell carci-
noma cell formation with topical and oral administration
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Commentary Ground-up leaves and twigs are not appealing in a skin cream.
The botanical must be processed such that it is a white powder
Botanicals are of great interest to the dermatologist and the con- that can be easily stirred into a moisturizer formulation. It must
sumer. From a dermatologic standpoint, topical botanicals are a be white because few consumers want to put a gray-pink cream
source of contact dermatitis, whereas oral botanicals can inter- on their face. It must be a powder because these are the easiest to
fere with blood clotting and create postsurgical complications. disperse. The powder must be very fine because a gritty mois-
From a consumer standpoint, the idea of topical and oral natu- turizer is not acceptable to most consumers. So what does this
ral products inducing improvement in the growth and function- mean? This means that everything from rosemary to lavender to
ing of the skin, hair, and nails is enormously appealing. Dr. aloe to chamomile to jojoba to soy must be distilled down to a
Thornfeldt has taken a systematic evaluative approach to the fine white powder. What happens when all botanical ingredients
cataloging of those botanicals of dermatologic significance. His are transformed into a fine white powder? Perhaps one might say
knowledge should help the dermatologist in obtaining a better that they now are not truly botanicals but chemical extracts of
understanding of the source and effect of plant derivatives. one sort or another derived from a plant source. It is possible that
It is noteworthy, however, to remember that most botanical our natural botanicals have now become unnatural chemicals!
extracts are just extracts. What does this imply? This means that
they are just one fraction of a plant-derived material that has ZOE DIANA DRAELOS, MD
been processed to meet the needs of the cosmetic formulator. High Point, NC

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