experienced improved weight gain, and higher lymphocyte and eosinophil counts compared to the placebo group.11
Dosage Ranges
1. Benign Prostatic Hyperplasia - 20 mg beta-sitosterol, three times per day or 65 mg beta-sitosterol, twice per
day.4,5,7,8
2. Cholesterol Lowering - 500 mg to 10,000 mg per day of beta-sitosterol.2,3
3. Autoimmune Diseases - 1 capsule sterinol, three times daily on an empty stomach.12 (i.e., Moducare)
4. HIV and Tuberculosis Infection - 2 capsules of sterinol, three times a day for one week, and 1 capsule, three times
a day for maintenance13 (i.e., Moducare). Other infectious diseases may also be aided with sterinol
supplementation.13
Adverse Side Effects and Toxicity
Oral Beta-sitosterol is very non-toxic as demonstrated by various studies. Other than occasional mild constipation or
diarrhea at very high doses, beta-sitosterol is not associated with any significant side effects. 9
Drug-Nutrient Interactions
There are no well-known drug-nutrient interactions with beta-sitosterol.14
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Meschino Health Comprehensive Guide to Herbs
Pregnancy and Lactation
During pregnancy and lactation, the only supplements that are considered safe include standard prenatal
vitamin and mineral supplements. All other supplements or dose alterations may pose a threat to the
developing fetus and there is generally insufficient evidence at this time to determine an absolute level of
safety for most dietary supplements other than a prenatal supplement. Any supplementation practices
beyond a prenatal supplement should involve the cooperation of the attending physician (e.g., magnesium
and the treatment of preeclampsia.)
References: Pregnancy and Lactation
1. Encyclopedia of Nutritional Supplements. Murray M. Prima Publishing 1998.
2. Reavley NM. The New Encyclopedia of Vitamins, Minerals, Supplements, and Herbs. Evans and
Company Inc. 1998.
3. The Healing Power of Herbs (2nd edition). Murray M. Prima Publishing 1995.
4. Boon H and Smith M. Health Care Professional Training Program in Complementary Medicine.
Institute of Applied Complementary Medicine Inc. 1997.
1. Awad, AB, et.al., Phytosterols as Anticancer Dietary Components: Evidence and Mechanism of Action, J Nutr 2000;130:2127-30.
2. Lees, AM, et.al., Plant Sterols as Cholesterol-lowering Agents: Clinical Trials in Patients with Hypercholesterolemia and Studies of Sterol
Balance, Atheroscles 1997;28:325-38.
3. Pelletier, X, et.al., A Diet Moderately Enriched in Phytosterols Lowers Plasma Cholesterol Concentrations in Normocholesterolemic
Humans, Ann Nurt. Metab 1995;39:291-5.
4. Berger, RR, et.al., Randomised, Placebo-controlled, Double-blind Clinical Trial of Beta-sitosterol in Patients with Benign Prostatic
Hyperplasia, Lancet 1995;345:1429-532.
5. Klippel, KF, et.al., A Multicentric, Placebo-controlled Double-blind Clinical Trial of Beta-sitosterol for the Treatment of Benign Prostatic
Hyperplasia, Br J Urol, 1997;80:427-432.
6. Bouic, PJ, et.al., Plant Sterols and Sterolins: A Review of Their Immune-modulating Properties, Altern Med Rev 1999;3:170-7.
7. Berger, R, et.al., Treatment of Symptomatic Benign Prostatic Hyperplasia with Beta-sitosterol, an 18-month Follow-up, Br J Urol
2000;85(7):842-6.
8. Wilt, TJ, et.al., Beta-sitosterol for the Treatment of Benign Prostatic Hyperplasia: A Systematic Review, BR J Urol Int. 1999;83(9):976-83.
9. Pegel, KH, The Importance of Sitosterol and Sitosterolin in Human and Animal Nutrition, South African J Sci. 1997;93:263-8.
10. Bouic, P, Immunomodulation in HIV/AIDS: The Typerberg:/Stellenbosch University Experience, Bouic, P AIDS Bulletin, 1997;6:18-20.
11. Donald, PR, et.al., A Randomized, Placebo-controlled Trial of the Efficacy of Beta-sitosterol and its Glucoside as Adjuvants in the
Treatment of Pulmonary Tuberculosis, Int J Tuberc Lung Dis. 1999;1(5):518-22.
12. Vanderhaeghe, L and Bouic P, The Immune System Cure, Prentice-Hall Canada Inc, 1999:125-55.
13. Vanderhaeghe, L and Bouic P, The Immune System Cure, Prentice-Hall Canada Inc, 1999:175-96.
14. Healthnotes Online, Healthnotes 2000, Inc.
Ostland RE,(Jr), et al. Sitostanol administration in lecithin micelles potently reduces cholesterol absorption in humans.
Am J Clin Nutr. 1999; 70: 826-831.
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Meschino Health Comprehensive Guide to Herbs
Bilberry (Vaccinium Myrtilus)
General Features
Bilberry extract is well recognized for its ability to support collagen tissue (especially in blood vessel supporting
connective tissues) and provides antioxidant protection to the macula of the eye. As such, it is recommended for
certain eye conditions, such as macular degeneration, diabetic retinopathy, and in cases of capillary fragility. During
World War II British fighter pilots taking Bilberry reported an improved ability to adjust to glare and an increase in their
visual acuity and nighttime vision.21,22,23
Active Ingredients
Research has focused primarily upon the anthocyanosides, which are flavonoid compounds, unique to Bilberry extract.
They are formed by an anthocyanidin backbone bound to one of three sugars (arabinose, glucose or galactose).
The concentration of anthocyanosides in the fresh fruit is only 0.1 to 0.25 percent, whereas concentrated extracts of
Bilberry taken as supplements yield an anthocyanidin content of 25 percent.1,2,3,21,22
Mechanism of Action
1. Collagen
Stabilizing action – Bilberry preserves collagen and related ground substance by increasing the cross-linking of
collagen fibers, acting as a free radical scavenger, inhibiting enzymatic cleavage of collagen by enzymes secreted
by leukocytes during inflammation, reducing the release of histamine, serine proteases, prostaglandins and
leukotrienes and by promoting the synthesis of glycosaminoglycans (see glucosamine in this document) and
collagen by chondrocytes.4,5,6,7
2. Anti-aggregation of platelets
Like many other flavonoids anthocyanosides heve been shown to decrease platelet aggregation in experimental
studies.8,9,10
3. Antioxidant
The anthocyanodins derived from Bilberry also demonstrate very potent antioxidant properties.4
Clinical Applications
1. Macular Degeneration of the Eye
Macular degeneration is the most common cause of blindness in individuals over the age of 55 (see also Lutein and
Zeazanthin in this document) in North America. Bilberry anthocyanidins appear to be able to help defend against
and manage macular degeneration and other eye conditions via several biological actions. The first is that these
unique flavonoids have been shown to improve the delivery of oxygen and blood to the eye. The second is that
they provide antioxidant protection against ultra-violet light induced free radical damage (from sunlight) to the
macula of the eye, which has been shown to contribute to the development and progression of macular
degeneration. Third, anthocyanidins from Bilberry have been shown to stabilize the blood vessel wall of small
blood vessels in the macular region of the eye, helping to prevent leaking of blood (micro-hemorrhaging) into the
macular region as often occurs in diabetic retinopathy and the wet form of macular degeneration. Like the
antioxidant carotenoids lutein and zeazanthin, Bilberry anthocyanosides are known to concentrate in the macula of
the eye, where they have the opportunity to quench ultra-violet light induced free radicals.21,22
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Meschino Health Comprehensive Guide to Herbs
In one study, 31 patients with various retinopathies (20 diabetic, 5 retinitis pigmentosa, 4 macular degeneration,
hemorrhagic retinopathy) were treated with Bilberry extract.
There was a tendency toward reduced permeability and hemorrhage observed in all patients, especially in those
with diabetic retinopathy.18
2. Cataract
In the study by Bravetti G. (1989), Bilberry extract, plus vitamin E stopped progression of cataract formation in 97
percent of 50 patients with senile cortical cataracts. This effect is thought to be due to its powerful antioxidant
properties, protecting the lens of the eye from oxidation and regenerating its collagen fibers.17
3. Night Vision
Bilberry anthocyanosides have an affinity for the pigmented epithelium or visual purple of the retina, which is the
portion of the retina responsible for night vision (rhodopson pigment formed from vitamin A on the rods).
The Royal Air Force pilots reported improved night vision during World War II with the use of Bilberry extract (also,
quicker adjustment to darkness and faster recovery from glare). Even individuals with retinitis pigmentosa and
hemeralopia (day blindness) have realized impressive improvement with Bilberry extract
supplementation.11,12,13,14,15,16,17,18
4. Varicose Veins and Capillary Fragility
Via its effects on collagen and connective tissues, which include increased synthesis of glycosaminoglycans
(cement substance between fibers), reduced permeability and impaired prostaglandin synthesis, Bilberry has been
used in clinical trials with capillary fragility problems. In one study, 47 patients with varicose veins treated with
Bilberry extract (480 mg per day) witnessed significant improvement with edema, heaviness feeling, parethesia,
pain and skin dystrophy.19,20 ( see also Horse chestnut and Grape seed extract in this document).
Dosage and Standardized Grade
For most eye conditions and capillary fragility conditions, the following recommendations can be considered:
80 to 160 mgs of Bilberry extract, (standardized to 25 percent anthocyanidin content), three times per day.
Adverse Side Effects, Toxicity and Contraindications
Bilberry extract has been shown to be very non toxic and has not produced any significant side effects is studies to
date. There are no well known health conditions that preclude the use of Bilberry extract.21,22
Drug-Nutrient Interactions
Anticoagulant Medications (e.g. warfarin, coumadin, aspirin) – as Bilberry extract has been shown in experimental
studies to reduce the clotting action of blood platelets, it may potentiate the action of other anticoagulant drugs. In
these cases, prothrombin time (INR) should be monitored closely to guard against a possible bleeding disorder,
although no human reports of such an occurrence have yet been reported.24
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Meschino Health Comprehensive Guide to Herbs
Pregnancy and Lactation
During pregnancy and lactation, the only supplements that are considered safe include standard prenatal
vitamin and mineral supplements. All other supplements or dose alterations may pose a threat to the
developing fetus and there is generally insufficient evidence at this time to determine an absolute level of
safety for most dietary supplements other than a prenatal supplement. Any supplementation practices
beyond a prenatal supplement should involve the cooperation of the attending physician (e.g., magnesium
and the treatment of preeclampsia.)
References: Pregnancy and Lactation
1. Encyclopedia of Nutritional Supplements. Murray M. Prima Publishing 1998.
2. Reavley NM. The New Encyclopedia of Vitamins, Minerals, Supplements, and Herbs. Evans and
Company Inc. 1998.
3. The Healing Power of Herbs (2nd edition). Murray M. Prima Publishing 1995.
4. Boon H and Smith M. Health Care Professional Training Program in Complementary Medicine.
Institute of Applied Complementary Medicine Inc. 1997.
1. Kuhnau J, The flavonoids, A Class of Semi-essential Food Components: Their Role in Human Nutrition, World Rev Nutr Diet
1976;24:117-91.
2. Gabor M, Pharmacologic Effects of Flavonoids on Blood Vessels, Angiologica 1972;9:355-74.
3. Havsteen B, Flavonoids, A Class of Natural Products of High Pharmacological Potency, Biochem Pharmacol 1983;32:1141-8.
4. Monboisse JC, et. al. Non-enzymatic Degradation of Acid Soluble Calf Skin Collagen by Superoxide Ion: Protective Effect of Flavonoids,
Biochem Pharmacol 1983;32:53-8.
5. Monboisse JC, Braquet P, Borel JP. Oxygen-free Radicals as Mediators of Collagen Breakage. Agents Actions 1984;15:49-50.
6. Rao CN, Rai VH, And Steinman B, Influence of Bioflavonoids on the Collagen Metabolism in Rats with Adjuvant Induced Arthritis. Ital J
Biochem 1981;30:54-62.
7. Ronziere MC, et. al., Influence of Some Flavonoids on Reticulation of Collagen Fibrils in Vitro. Biochem Pharmacol 1981;30:771-6.
8. Middleton E, The Flavonoids, Trends Pharm Sci 1984;5:335-8.
9. Amella M, et. al., Inhibition of Mass Cell Histamine Release by Flavonoids and Bioflavonoids. Planta Medica 1985;51:16-20. Jonadet M,
et. al., Anthocyanosides Extracted from Vitis Vinifera, Vaccinium Myrtillus and Pinus Maritimus, I. Elastese-inhibiting Activities in Vitro, II.
Compared Angioprotective Activities in Vivo, J Pharm Belg 1983;38:41-6.
10. Detre A, et. al., Studies on Vascular Permeability in Hypertension: Action of Anthocyanosides. Clin Physiol Biochem 1986;4:143-9.
11. Jayle GE and Aubert L, Action des Glucosides D’Anthocyanes sur la Vision Scotopique et Mesopique du Sujet Normal Therapie
1964;19:171-85.
12. Terrasse J and Moinade S, Premiers Resultats Obtenus Avec un Nouveau Facteur Vitaminique P “les Anthocyanosides” Extraits du
Vaccinium Myrtillus, Presse Med 1964;72:397-400.
13. Sala D, Rolando M, Rossi PL and Pissarello L, Effects of Anthocyanosides on Visual Performances at Low Illumination. Minerva Oftalmol
21, 283-285, 1979. Gloria E and Peria A, Effect of Anthocyanosides on the Absolute Visual Threshold, Ann Ottalmol Clin Ocul
1966;92:595-607.
14. Junemann G, On the Effect of Anthocyanosides on Hemeralopia Following Quinine Poisoning. Klin Monatsbl Augenheilkd 1967;151:891-
6.
15. Caselli L, Clinical and Electroretinographic Study on Activity of Anthocyanosides. Arch Med Int 1985;37:29-35.
16. Wegman R, Maeda K, Troche P, and Bastide P. Effects of Anthocyanosides on Photoreceptors, Cytoenzymatic Aspects. Ann Histochim
1969;14:237-56.
17. Bravetti G, Preventive Medical Treatment of Senile Cataract with Vitamin E and Anthocyanosides: Clinical Evaluation. Ann Ottalmol Clin
Ocul 1989;115:109.
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Meschino Health Comprehensive Guide to Herbs
18. Scharrer A and Ober M, Anthocyanosides in the Treatment of Retinopathies. Klin Monatbsl Augenheilkd 1981;178:386-9.
19. Mian E, et.al., Anthocyanosides and the Walls of Microvessels, Further Aspects of the Mechanism in the Action of their Protective Effect
in Syndromes due to Abnormal Capillary Fragility. Minerva Med 1977;68:3565-81.
20. Ghiringhelli G, Gregoratti F, and Marastoni F, Capillarotropic Activity of the Anthocyanosides in High Doses in Phlebopathis Stasis. Min
Cardioangiol 1978;26:255-76.
21. Murray MT, The Healing Power of Herbs (2nd edition), Prima Publishing, 1995.
22. Dietary Supplement Information Bureau. www.content.intramedicine.com: Bilberry
23. Jayle GE, et al. Study concerning the action of athocyanoside extracts of Vaccinium myrtillus on night vision. Ann Occul Paris. 1965; 198
(6): 556-62.
24. Moranzonni P, et al. Vaccinium myrtillus. Fitoterapia. 1996; vol LXVII (1): 3-29
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Meschino Health Comprehensive Guide to Herbs
Black Cohosh (cimicifuga racemosa)
Black Cohosh is an upright perennial plant, which contains active constituents shown to be of importance in the
management of menopause and various female reproductive conditions, especially PMS. Black Cohosh commercial
stocks come from the United States and Canada, although it is especially popular in Germany. Historically, it has been
used for its medicinal properties by peoples of the First Nations.1
Principle Active Constituents
Terpenoids (triterpene glycosides, which are saponins), Formononetin.1
Black Cohosh triterpenes have been shown to mimic the effects of estriol, the weakest endogenous estrogen formed in
the body.2
Clinical Application and Mechanism of Action
1. Menopause
A number of studies (double-blind, placebo-controlled and open trials) involving postmenopausal women have
demonstrated that Black Cohosh supplementation can: reduce hot flashes and other menopausal symptoms
(insomnia, profuse sweating, dizziness, headache, heart palpitation, tinnitus, nervousness/irritability, anxiety,
depressive moods).
Black Cohosh has also been shown to maintain integrity of the vaginal lining (mucosa) in postmenopausal women,
preserving sexual function and preventing atrophy and dryness of these tissues that often accompanies
menopause.3,4,5,6,7,8
Black Cohosh triterpenes appear to account for these therapeutic effects as these active constituents are known to
exert a weak, but significant estrogenic effect, that has been shown to be sufficient to compensate for the 90%
decline in estrogen production that occurs in the menopausal years of a women’s life. A very high percentage of
women in these studies reported significant benefits from the use of Black Cohosh extract in controlling their
menopausal symptoms and improvement was on par or better than the relief afforded by estrogen or hormone
replacement therapy.3,4,5,6,7,8
N.B. These effects of Black Cohosh were evident in head to head trials against hormone replacement therapy,
diazepam and in patients where hormone replacement therapy was contraindicated, or refused.
2. Premenstrual Syndrome
Several published trials revealed that Black Cohosh is highly effective in reducing the symptoms of PMS.9,10 Some
reports suggest that PMS is caused or aggravated by a high estrogen to progesterone ratio in affected women. It
has been proposed that Black Cohosh triterpenes act as phytoestrogens, competing with the body’s more powerful
estrogens, for binding to estrogen receptors on reproductive tissues. In this capacity Black Cohosh triterpenes can
reduce the stimulation of the body’s more powerful estrogens (estradiol, estrone), toning down (down-regulating)
their influence upon the breast, uterus and other tissues. In turn, this reduces the estrogen over-stimulation that
may be a factor in the promotion of PMS. Another aspect of PMS management involves the fact that Black Cohosh
triterpenes have also been shown to be a precursor (building block) for the body’s synthesis of progesterone. It
appears that some women display corpus luteum failure, in that the ovaries secrete insufficient amounts of
progesterone during the second half of the menstrual cycle. This can aggravate the high estrogen to progesterone
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Meschino Health Comprehensive Guide to Herbs
ratio described above. Thus, the use of Black Cohosh extract is proposed to provide relief of PMS in as much as
its triterpene constituents can block the over-stimulation effect of the body’s more powerful estrogens and enable
the body to increase its production of natural progesterone. Further, Black Cohosh triterpenes have also been
shown to be anti-spasmodic, helping to reduce abdominal and uterine cramping associated with PMS. No other
natural agent has been shown to provide all three of these biological actions, which appear to be of significance in
the management of PMS.13,18
Other Female Conditions
Preliminary trials suggest that Black Cohosh may provide benefit in other gynaecological complaints such as
amenorrhea (both primary and secondary) dysmenorrhea, polymenorrhea, uterine fibroids, and fibrocystic breast
disease.9,10,11
Breast Cancer and Other Safety Concerns
The BGA, the German equivalent to the FDA in the United States and HPB in Canada, includes no contraindications or
limitations of use for black cohosh. To date its effects on established breast tumor cell line has shown no stimulatory
effects but rather inhibitory effects of cancer cell replication.12
From our current understanding, Black Cohosh offers an appropriate natural alternative to hormone replacement
therapy for menopause (unless osteoporosis is well established), especially where hormone replacement therapy is
contraindicated (i.e., women with a history of estrogen-dependent cancer, unexplained uterine bleeding, liver and
gallbladder disease, pancreatitis, endometriosis, uterine fibroids or fibrocystic breast disease.13
The phytoestrogens contained in black cohosh, exhibit a relative binding affinity for estrogen receptors that is only
1/100 as strong as 17-beta-estradiol (the body’s most potent estrogen).14
Black Cohosh phytoestrogens do not stimulate growth of endometrial cells therefore, concurrent progesterone
replacement is not required to reduce risk of endometrial cancer (with estrogen replacement therapy, progesterone is
used to block the stimulatory effects of estrogen on endometrial overgrowth and the known cancer risk associated with
this effect). As such, Black Cohosh may be beneficial as a treatment for endometriosis.14
Commission E, a German regulatory agency, considers Black Cohosh useful in the management of premenstrual
syndrome, dysmenorrhea and nervous conditions associated with menopause.15 In 1997, over ten million monthly
units of a popular German Black Cohosh product (Remifemin) were sold in Germany, the United States, and
Australia.13
Dosage and Standardized Grade
Black Cohosh extract standardized to 2.5% triterpenes is the clinical extract used in most studies (often calculated as
27 – deoxyacteine).
Menopause and PMS - the dosage for PMS and Menopause ranges from 40 mg, twice per day, to two 40 mg capsules
or caplets (80 mg), twice per day, for a daily total intake ranging from 80 – 160 mg of Black Cohosh extract,
standardized to 2.5% triterpenes.16
Adverse Side Effects, Toxicity and Contra-Indications
De