23. Schrader E, Meier B, Brattstrom A. Hypericum treatment of mild-moderate depression in a placebo-controlled study: a prospective,
double-blind, randomized, placebo-controlled, multicentre study. Hum Psychopharmacol 1998;13:163-9
24. Müller WE, Rolli M, Schäfer C, Hafner U. Effects of hypericum extract (LI 160) in biochemical models of antidepressant activity.
Pharmacopsychiatry 1997;30(suppl):102–7
25. Kalb R, Trautmann-Sponsel RD, Kieser M. Efficacy and tolerability of hypericum extract WS 5572 versus placebo in mildly to moderately
depressed patients. A randomized double-blind multicenter clinical trial. Pharmacopsychiatry 2001;34:96-103
26. Hansgen KD, Vesper J. Antidepressant efficacy of a high-dose hypericum extract [translated from German]. MMW Munch Med
Wochenschr 1996;138:29-33
27. Shelton RC, Keller MB, Gelenberg A, et al. Effectiveness of St. John’s wort in major depression: a randomized controlled trial. JAMA
2001;285:1978-86
28. Hypericum Depression Trial Study Group. Effect of Hypericum perforatum (St. John’s wort) in major depressive disorder: a randomized
controlled trial. JAMA 2002;287:1807-14
29. Schrader E. Equivalence of St John’s wort extract (Ze 117) and fluoxetine: a randomized, controlled study in mild-moderate depression.
Int Clin Psychopharmacol 2000;15:61-8
30. Harrer G, Schmidt U, Kuhn U, et al. Comparison of equivalence between the St. John’s wort extract LoHyp-57 and fluoxetine.
Arzneimittelforschung 1999;49:289-96
31. Brenner R, Azbel V, Madhusoodanan S, et al. Comparison of an extract of hypericum (L1 160) and sertraline in the treatment of
depression: a double-blind, randomized pilot study. Clin Ther 2000;22:411-9
32. Philipp M, Kohnen R, Hiller KO. Hypericum extract versus imipramine or placebo in patients with moderate depression: randomized
multcentre study of treatment for eight weeks. BMJ 1999;319:1534-9
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33. Martinez B, Kasper S, Ruhrmann S, et al. hypericum in the treatment of seasonal affective disorders. J Geriatr Psychiatr Neurol
1994;7(suppl 1):S29-33
34. Muller WEG, et al. Effects of Hypericum Extract on the Expression of Serotonin Receptors. J Geriatric Psychiatry and Neurology.
1994;7:S63-S64
35. Rayburn WF, Gonzalez CL, Christensen HD, et al. Effect of prenatally administered hypericum (St John’s wort) on growth and physical
maturation of mouse offspring. Am J Obstet Gynecol 2001;184:191-5
36. Woelk H, Burkard G, Grunwald J. Benefits and risks of the hypericum extract LI 160: Drug monitoring study with 3,250 patients. J Geriatr
Psychiatr neurol 1994;7(suppl 1):S34-8
37. Hubner WD, Arnoldt KH. St John’s wort: a one year treatment study [in German; English abstract]. Z Phytother 2000;21:306-10
38. Schulz V, Hansel R, Tyler VE. Rational Thytotherapy: A Physicians’ Guide to Herbal Medicine. 3rd ed. Berlin, Germany: Springer-Verlag
1998:p56
39. De Smet PA, Nolen WA. St. John’s wort as an anti-depressant. BMJ 1996;3:241-2
40. Suzuki O, Katsumata Y, Oya M, et al. Inhibition of monoamine oxidase by hypericin. Planta Med 1984;50:272-4
41. Bladt S, Wagner H. Inhibition of MAO by fractions and constitutents of hypericum extract. J Geriatr Psychiatr Neurol 1994;7(suppl 1):S57-
9
42. Thiede HM, Walper A. Inhibition of MAO and COMT by hypericum extracts and hypericin. J Geriatr Psychiatr Neurol 1994;7(suppl 1):S54-
6
43. Kahn RS, et al. L-5-hydroxytryptophan in the treatment of anxiety disorders. J Affect Disord Mar1985;8(2):197-200
44. Muller WE, et al. Effects of Hypericum Extract (LI 160) in Biochemical Models of Antidepressant Activity. Pharmacopsychiatry.
1997;30(Supp 2):102-07
45. Linde K, et al. St. John's Wort for Depression--An Overview and Meta-analysis of Randomised Clinical Trials. BMJ. 1996;313m:253-58
46. Demott K. St. John’s Wort Tied to Serotonin Syndrome. Clin Psychiatry News 1998;26:28.
47. Suzuki O, et al. Inhibition of Monoamine Oxidase by Hypericin. Planta Medica 1984;50:272-74.
48. Bladt S, et al. Inhibition of MAO by Fractions and Constituents of Hypericum Extract. J Geriatric Psychiatry and Neurology 1994;7:S57-
S59
49. Gordon JB. SSRIs and St.John's Wort: possible toxicity? Am Fam Physician Mar1998;57(5):950,953
50. Lantz MS, Buchalter E, Giambanco V. St. John's wort and antidepressant drug interactions in the elderly. J Geriatr Psychiatry Neurol
1999;12(1):7-10.
51. Okpanyi SN, et al. Animal experiments on the psychotropic action of a hypericum extract. Arzneimittelforschung Jan1987;37(1):10-3
52. Johne A et al. Pharmacokinetic interaction of digoxin with an herbal extract from St John’s wort (Hypericum perforatum) Clin Pharmacol
Ther Oct1999;66(4):338-45
53. Nebel A, et al. Potential metabolic interaction between St. John’s wort and Theophylline. Ann Pharmacother Apr1999;33(4):p502
54. Ruschitzka F, et al. Acute heart transplant rejection due to St. John’s wort. Lancet Feb2000;355(9203):548-9
55. Rey JM, et al. Hypericum perforatum (St John;s Wort) in depression: Pest or blessing? Med J Aust Dec1998;169(11-12):583-6
56. Yue Qy, Bergquist C, Gerden B. Safety of St. John’s wort (Hypericum perforatum), correspondence. Lancet 2000;355:576-7
57. Ernst E. Second thoughts about safety of St John’s Wort. Lancet Dec1999;354(9195):2014-6
58. Piscitelli SC, et al. Indinavir concentrations and St. John’s Wort. Lancet Feb2000;355(9203):547-8
59. Mills S, Bone K. Principles and Practice of Phytotherapy. Churchill Livingstone 2000:548-9
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Stinging Nettle or Nettle ( Urtica Dioica)
General Features
Nettle resembles a noxious weed that can cause a pruritic rash upon contact with the skin. The aerial parts and the
roots (rhizomes) of two species (Urtica dioica L. and Urtica urens L.) are used medicinally. 1,2,3,4 Stinging Nettle
extract is commonly used in formulations to treat benign prostatic hyperplasia in many regions of Europe. 5,6 It may
also have value in the management of arthritis symptoms, gout and the treatment of hayfever, but these applications
are less well substantiated than its accepted use in the treatment of benign prostatic hyperplasia. 7,8,21,22,23
Principle Active Constituents
- Flavonoids (Leaf)
- Sterols – including beta-sitosterol and sitosterol –3 –D – glucoside (roots)
- Lignans (roots)
- Fatty acids (roots) 9
- Polysaccharides and Lectins 21
There is controversy as to which of the above constituents are most important in the treatment of BPH, arthritis, and
allergic conditions. 21
Clinical Application and Mechanism of Action
1. Benign Prostatic Hyperplasia (BPH)
Nettle is most commonly combined with other phytonutrients, such as Saw Palmetto, Pygeum Africanum and Beta-
sitosterol, in the treatment of BPH.10,11,21,22 However, it has been used a singular treatment agent in at least two
double-blind studies involving men with BPH.
In these studies Nettle proved to be superior to placebo, but showed less impressive results than studies using Saw
Palmetto, Pygeum and/or Cernilton. 12,13,22 Urtica extract has been shown to block the action of dihydrotestosterone
(DHT). Like saw palmetto extract, Urtica extract appears to interact with the binding of DHT to cytosolic and nuclear
receptors hence, decreasing the impact of DHT’s effect on the cell division rate of prostate cells. DHT tends to cause
excessive cell division leading to BPH, if it builds up intraprostatically. 14
Other studies indicate that Urtica extract inhibits the binding of sex hormone-binding globulin to human prostatic tissue,
thus, reducing excessive androgen stimulation to the gland.
It may also inhibit the aromatase enzyme, which converts androstenedione to estrone hormone within fat tissue.
Estrone hormone is linked to increased BPH symptoms and a build up of DHT in the prostate gland, as this form of
estrogen decreases the hydroxylation (breakdown or detoxification) and elimination of DHT. 2,15
Experimental evidence has repeatedly shown that Urtica extract exerts anti-proliferative effects on human prostate
cells as well as on human prostate cancer cells in in-vitro, and in-vivo animal studies. 16,17
Urtica dioica extract is also a weak inhibitor of the 5 alpha-reductase enzyme, which converts testosterone to
dihydrotestosterone (DHT). 19
All of these biological mechanisms are beneficial in the treatment of BPH. Some authorities suggest that Nettle
contains numerous biologically active chemicals that may influence the function of the prostate gland, interact with sex
hormones, slow the growth of prostate cells, fight prostate cancer, and reduce inflammation. 22
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A number of open studies involving at least 15,000 men, although less reliable than double-blind placebo controlled
studies, have also shown Nettle extract to be useful in the treatment of symptoms associated with BPH.
2. Hayfever (allergic rhinitis)
A small study of 69 subjects demonstrated that Nettle supplementation reduced hayfever symptoms to a significant
degree, under double-blind, placebo-controlled conditions. 25
3. Arthritis
A small double-blind study, along with historical use of Nettle, suggests that by applying Stinging Nettle leaf topically
over arthritic joints, symptoms of pain, swelling and stiffness may improve. 26
Dosage and Standardized Grade
1. BPH: As a single agent, Urtica dioica extract is usually taken at 300-600 mg per day, in divided doses. 18, 21 As
part of a combination formula lower doses of Nettle extract are usually employed. 18 A 5:1 extract is commonly
used therapeutically, consisting of an Urtica product standardized to 1-2% silica content. 23
2. Hayfever: 300 mg of Urtica extract, twice per day. 25
Adverse Side Effects, Toxicity and Contraindications
Adverse side effects are rare. Infrequent reports of scanty urination, skin irritation, and gastric distress occur in some
patients. 2,20 In one study involving 4,087 subjects who took 600 to 1,200 mg of Nettle root daily for 6 months, less
than 1% reported mild stomach upset, and only 0.19% experienced allergic skin reactions (skin rash). 27
Drug-Nutrient Interactions
There are no well-known drug nutrient interactions for stinging Nettle. Theoretically, Nettle may potentiate the effect of
antihypertensive drugs and antagonize the effects of oral hypoglycemic drugs in type II diabetics, and possibly interact
with sedative medications, but no clinical evidence exists to establish these interactions as a contraindication to the
use of Urtica dioica at this time. 20,22
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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. Leung A, Foster S. Encyclopedia of Common Natural Ingredients Used in Food, Drugs and Cosmetics. New York, NY: John Wiley and
Sons 1996:p649
2. ESCOP. Urticae Radix/Nettle Root. In: ESCOP Monographs (Fascicule 2) Exeter: ESCOP 1996:p58
3. ESCOP.Urticae Folium/Herba (Nettle Leaf). In: ESCOP Monographs (Fascicule 4) Exeter: ESCOP 1997:p58
4. Weiss RF. Herbal medicine. Beaconsfield, England: Beaconsfield Publishers Ltd 1988:p362
5. Dreikorn K, Schonhofer P. Status of phytotherapeutic drugs in the treatment of benign prostatic hyperplasia. [German] Urologe A
1995;34(2):119-29
6. Buck A. Phytotherapy for the prostate. British Journal of urology 1996;78:325-36
7. Chrubasik S, Enderlein W, Bauer R, Grabner W. Evidence for antirheumatic effectiveness of herba urticae dioicae in acute arthritis: A
pilot study. Phytomedicine 1997;4(2):105-8
8. Rand J. pilot study indicates that tewed herba urticae diocae may potentiate the effects of diclofenac in acute arthritis. Focus on
Alternative and Complementary Therapies 1997;2(4):156-7
9. The Botanical Pharmacy. Quarry Health Books 1999. Boon H and Smith M:256-9
10. Schneider HJ, Honold E, Mashur T. Treatment of benign prostatic hyperplasia. Results of a surveillance study in the practices of
urological specialists using a combined plant-based preparation. Forschritte der Medizin 1995;113:37-40
11. Harmann R, Mark M, Soldati F. Inhibition of 5 alpha reductase and aromatase by PHL-00801 (Prostatonin), a combination of PY102
(Pygeum africanum) and UR102 (Urtica dioica) extracts. Phytomedicine 1996;3(2):121-8
12. Belaiche P et al. Clinical studies on the palliative tratment of prostate adenoma with extract of urtica root. Phytother Res 1991;5:267-9
13. Romics I. Observations with Bazotion in the management of prostatic hyperplasia. Int Urol Nephrol 1987;19(3):293-7
14. Wagner H et al. Search for the anti-prostatic principle of stinging nettle (urtica dioica) roots. Phytomedicine 1994;1:213-24
15. Hyrb D, Khan M, Romas N, Rosner W. The effect of extracts of the roots of the the stinging nettle (Urtica dioica) on the interaction of
SHBG with its receptor on human prostatic membranes. Planta Medica 1995;61:31-2
16. Konrad L et al. Antiproliferative effect on human prostate cancer cells by a stinging nettle root (urtica dioica) extract. Planta med
2000;66(1):44-7
17. Lichius JJ et al. Antiproliferative effect of a polysaccharide fraction of a 20% methanolic extract of stinging nettle roots upon epithelial cells
of the human prostate (LNCaP) Pharmzie 1999;54(10):768-71
18. Pizzorno J, Murray M. Encyclopedia of Natural Medicine (2nd ed) Prima Health 1998:p762
19. Benign Prostatic Hyperplasia. Medical Post. Oct 17, 2000
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20. Newall C, Anderson L, Phillipson J. herbal medicines: A Guide for health Care professionals. London: The Pharmaceutical Press
1996:p296
21. Healthnotes, Inc 2001. www.healhnotes.com: nettle
22. Natural Products Encyclopedia. www.consumerslab.com: nettle
23. Dietary Supplement Information Bureau. www.content.intramedicine.com: Stinging Nettle
24. European Scientific Cooperative on Phytotherapy. Urticae radix. Exeter, UK: ESCOP, 1996-1997:4-5. Monographs on the uses of plant
drugs, fascicule 2.
25. Mittman P. Randomized, double-blind study of freeze-dried Urtica dioica in the treatment of allergic rhinits. Planta Med 1990;56:44-7
26. Randall C, Randall H, Dobbs F et al. Randomized controlled trial of nettle sting for the treatment of base-of-thumb pain. J R Soc Med
2000;93:305-9
27. Shulz V, Hansel R, Tyler VE. Rational Phytotherapy: A Physician’s Guide to Herbal medicine. 3rd ed. Berlin, Germany: Springer-Verlag
1998:201-2
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Tribulus Terrestris (Puncture Vine)
General Features
Tribulus Terrestris is an annual plant, which has been commonly used in folk medicine for a number of purposes.1
Most recently, it has been researched for its ability to reverse erectile dysfunction, enhance libido and as a treatment
for angina pectoris.2,3
Tribulus Terrestris is a rich source of saponins, of which protodioscin has received a significant amount of attention in
regards to sexual dysfunction issues.2,3
Principle Active Constituents
Steroidal Saponins (Furanosterols)4,5
Clinical Application and Mechanism of Action
1. Erectile Dysfunction
Tribulus Terrestris supplementation has been shown to reverse erectile dysfunction problems and improve or
enhance
sexual
desire
in
men
and
women.3,6
Evidence exists to demonstrate that protodioscin (saponin) from Tribulus Terrestris can be converted in the body to
dehydro-epiandrosterone (DHEA), a precursor to the synthesis of testosterone and estrogen.3 It is thought that
Tribulus Terrestris can increase testosterone levels in men and estrogen levels in women.6 However, some
evidence
refutes
this.7
An alternate explanation suggests that protodioscin (saponin) increases the release of nitric oxide from the arterial
endothelium and nitrergic nerve endings in the region of the genitalia, facilitating increased blood flow to the corpus
cavernosum.2
This effect appears to be more likely than the elevation of testosterone, as studies with body builders fail to
demonstrate a rise in serum testosterone in these athletes after supplementation with Tribulus Terrestris.7
2. Angina Pectoris
Tribulus Terrestris is known to dilate coronary arteries and improve angina pectoris in afflicted patients as
demonstrated in a clinical and cross-over trial of 406 cases of angina pectoris. This appears to confirm the effect of
protodioscin as a mediator to enhance the release of nitric oxide locally, dilating arteries and increasing blood flow
through the coronary blood vessels of the heart as mentioned above. 8 This application requires cooperation with
the attending physician.8
Dosage and Standardized Grade
Erectile Dysfunction and Libido-Enhancement – 250 mg (Standardized extract containing 40 percent saponins), three
times daily is a common daily dosage in these cases. A daily dosage of up to 1500 mg per day has also been used
safely.6
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Adverse Side Effects, Toxicity and Contraindications
The LD 50 in rats is greater than 10 gm per kg of body weight. Tribulus Terrestris appears to be very safe at
recommended doses with no major adverse side effects reported.6,8
Tribulus Terrestris should probably be avoided in cases of reproductive cancers (e.g., prostate, breast cancers)
Drug-Nutrient Interactions
There are no well-known drug-nutrient interaction for tribulus terrestris. Author’s Note: It is probably wise to not take it
concurrently with other vasodilating agents such as nitroglycerine or sildenofil (viagra).
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. Arcasoy HB, et al. Effect of tribulus terrestris L. saponins mixture on smooth muscle preparations: a preliminary study. Boll Chim Farm
1998;137(11):473-5
2. Adaikan PG, et al. Proerectile pharmacological effects of tribulus terrestris extract on the rabbit corpus cavernosum. Ann Acad med
Singapore 2000;29(1):22-6
3. Adimoelja A. Phytochemicals and the breakthrough of traditional herbs in the management of sexual dysfunctions. Int J Androl
2000;23(suppl 2):82-4
4. Selected Medicinal Plants of India. Chemexil 1992:323-5
5. Mahato S, et al. J Chem Soc, Perkin Trans 1981;1:2405
6. Wright J. Muscle and Fitness. Sept 1996;p140-2,p224
7. Brown GA, et al. Effects of anabolic precursors on serum testosterone concentrations and adaptations to resistance training in young
men. Int J Sport Nutr Exerc Metab 2000;10(3):340-59
8. Wang B, et al. 406 cases of angina pectoris in coronary heart disease treated with saponins of tribulus terrestris. Zhong Xi Ti Jie he Z|a
Zhi 1990;10(2):85-7
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Turmeric ( Curcumin)
General Features
Turmeric is a member of the ginger family. It has been used historically as a major ingredient in curry powder (flavour)
and for colouring (i.e. preparation of mustard).
The medicinal portions of Turmeric are the primary and secondary rhizomes. It is us