14. Satyavati GV. Gum guggul (Commiphora mukul) – The success of an ancient insight leading to a modern discovery. Indian J Med
1988;87:327-35
15. Singh RB, Niaz MA, Ghosh S. Hypolipidemic and antioxidant effects of Commiphora mukul as an adjunct to dietary therapy in patients
with hypercholesterolemia. Cardiovasc Drugs Ther 1994;8:659-64
16. Singh K, Chander R, Kapoor NK. Guggulsterone, a potent hypolipidaemic, prevents oxidation of low density lipoprotein. Phytother Res
1997;11:291-4
17. Mester L, Mester M, Nityanand S. Inhibition of platelet aggregration by guggulu steroids. Planta Med 1979;37:367-9
18. Thappoa DM, Dogra J. Nodulocystic acne: oral gugulipid versus tetracycline. J Dermatol 1994;21:729-31
19. Satyavati GV et al. Experimental studies on the hypocholesterolemic effect of commiphora mukul. Indian J Med Res 1969;57(10):1950-62
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20. Nityanand S et al. Clinical trials with gugulipid. A new hypolipidaemic agent. J Assoc Physicians India 1989;37(5):323-8
21. **Satyavati GV et al. Guggulipid: a promising Hypolipidemic agent from gum guggul (Commiphora Wightii). Econ Med Plant Res
1991;5:48-82
22. **Satyavati GV et al. Guggulipid: a promising Hypolipidemic agent from gum guggul (Commiphora Wightii). Econ Med Plant Res
1991;5:48-82
23. Tripathi YB et al. Thyroid stimulatory action of (Z)-Guggulsterone: mechanism of action. Planta Med 1988;54(4):271-7
24. Panda S, Kar A. Gugulu (Commiphora mukul) induces triiodothyronine production: possible involvement of lipid peroxidation. Life Sci
1999;65(12):PL137-41
25. **Dalvi SS et al. Effects of gugulipid on bioavailability of diltiazem and propranolol. J Assoc Physicians India 1994;42(6):454-5
26. **Dalvi SS et al. Effects of gugulipid on bioavailability of diltiazem and propranolol. J Assoc Physicians India 1994:42(6):454-5
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Hawthorn (Crataegus oxyacantha)
General Features
Hawthorn is a spiny shrub or tree, and is a member of the crataegus family. It has been used medicinally since
ancient times and during the first century, Roman physicians used Hawthorn as a drug to treat a variety of heart and
cardiovascular conditions. During the Middle Ages Hawthorn was used for the treatment of congestive heart failure
(dropsy), an application that has proven to be valid according to modern day evidence-based research. 1,11,12,13,14
Principle Active Constituents
Hawthorn flowers, berries, and leaves contain flavonoid compounds that appear to account for its positive effects on
cardiac function. These flavonoids account for the red color of Hawthorn berries. The flavonoids found in Hawthorn
include olgomeric procyanidins (OPCs), vitexin, vitexin 4 – 0 – rhamnoside, quercetin, and hyperoside. Standardized
extracts of Hawthorn are usually validated by their vitexin and procyanidin content, which ensure that sufficient levels
of flavonoids are present to yield the desired outcomes on cardiovascular health.11,12, 13,14
Hawthorn flower extract is the primary compound used medicinally and is particularly rich in the following flavonoids:
Quercitin
Quercitin-3-galactoside
Vitexin
Vitexin-4-rhamnoside
In addition to proanthocyanidins, Hawthorn extract also contains cardiotonic amines, which include:
Phenylethylamine
Methoxyphenylamine
Tyramine
Isobutilamine 1,2,3
Clinical Application and Mechanism of Action
Cardiovascular Effects:
Angina: Dilation of Coronary Vessels - Evidence exists to show that Hawthorn extract may improve coronary artery
blood flow and strengthen the contractions of the heart muscle. This has lead to findings that Hawthorn extract can
benefit patients with a history of angina by preventing or reducing angina attacks and improving other indices of
cardiovascular function, according a small number of clinical trials. 4,5,6,7,8,15, 16
Congestive Heart Failure: Hawthorn increases cyclic AMP (adenosine monophosphate) in the Myocardium (heart
muscle) due to its effects on inhibiting the enzyme phosphodiesterase, which breaks down cyclic AMP (cAMP). The
oral administration of Hawthorn extract results in higher myocardial concentrations of cAMP in patients suffering from
various cardiomyopathies (heart conditions). As cAMP can be further phosphorylated to ADP (adenosine
diphosophate) and then to ATP (adenosine triphosphate-the energy source used by the heart muscle to pump blood
through the system), higher myocardial concentrations of cAMP enables the heart muscle to pump more efficiently.
The net result is an increase in the heart muscle’s force of contraction. This effect has been shown to be of great
benefit for patients with congestive heart failure, who by definition, have a weakened heart muscle. A number of well-
controlled clinical trails have demonstrated that Hawthorn extract can reverse many cases of congestive heart failure
via its inotropic effect (increasing the amount of available energy) on cardiac muscle. 9,10,11.
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High Blood Pressure: Inhibits Angiotensin – Converting Enzyme (acting as an ACE-inhibitor) – by inhibiting the
angiotensin-converting enzyme Hawthorn extract reduces the conversion of angiotensin I to angiotensin II, which is a
potent constrictor of blood vessels and stimulates adrenal production of aldosterone. Thus, in a similar fashion to
ACE-inhibitor drugs, Hawthorn extract has been shown to exert a blood pressure lowering effect. However, Hawthorn
has been shown to have a modest effect on lowering blood pressure in hypertensive patients relative to more powerful
ACE-inhibitor medications. In one study, systolic blood pressure dropped from 205 to 148 mm Hg, but other studies
have shown a more modest reduction in blood pressure (e.g., systolic decline from 160 – 150 mm Hg, diastolic decline
from 89 – 84 mm Hg) with Hawthorn extract supplementation. 7,11,15
Clinical trials show that Hawthorn extract can be an effective adjunct to the lowering of high blood pressure, but its
hypotensive effects often require two to four weeks to manifest themselves. Hawthorn does not further lower blood
pressure in subjects who demonstrate normal blood pressure, but rather selectively appears to reduce blood pressure
only in hypertensive individuals. 23
Thus, the cardiovascular conditions that may be responsive to Hawthorn include congestive heart, angina, and high
blood pressure. In particular, Hawthorn has a long history of use in the treatment of congestive heart failure.
Congestive Heart Failure Clinical Trials: At least 8 double-blind, placebo-controlled trials, involving a total of more than
400 participants, have shown that Hawthorn extract is an effective intervention for mild to moderate congestive heart
failure. 17 One study, involving more than 200 patients, found that Hawthorn extract was helpful in more severe
congestive heart failure cases. 18 Even in more severe cases of congestive heart failure patients receiving high dose
Hawthorn extract reported improvement in subjective symptoms ( shortness of breath, fatigue, etc.) as well as
objective improvement in exercise capacity. 18 A comparative study has indicated that Hawthorn extract is about as
effective as low dose captopril, a drug commonly used to treat congestive heart failure. 19
Hawthorn appears to act in a similar manner as other cardiac glycoside drugs, such as digoxin and digitalis, which
exert an inotropic effect on the myocardium; enhancing ATP production through bioenergetic pathways. Studies
reveal that Hawthorn provides similar benefits as these drugs, and exhibits a much safer profile. Digoxin and related
cardiac glycoside prescription drugs increase the strength of the heart pump, but also increase the likelihood of
dangerous arrhythmias. This occurs because these drugs shorten the refractory period between heartbeats (the
period in which the heart can not contract between beats), which increases the chances of premature beats arising
from areas outside or inside the heart’s natural pacemaker. In turn, this disturbs the necessary synchronized and
rhythmic contraction pattern that the heart muscle must follow to perform its function properly. The result is the
development of cardiac arrhythmia, which can be life threatening. It is well documented that digoxin and related drugs
have a narrow index of safety for this reason. In contrast to this, Hawthorn extract is able to strengthen the heart
muscle, and has been shown to lengthen the refractory period between heartbeats, which reduces the likelihood of
developing cardiac arrhythmias. As well, Hawthorn exhibits much lower toxicity than digoxin and is reported to have
an enormously large range of safety, in regards to daily dosage (a number of studies have used doses as high as 600
mg per day with no significant side effects reported). 20,21,22, 13, 15
The major precautionary note pertains to the fact that it is not known if Hawthorn can be used safely with other cardiac
glycoside drugs or with other medications (usually ACE- inhibitors) that are now more commonly prescribed in the
treatment of congestive heart failure. 13 Some authorities suggest that Hawthorn’s effects are synergistic to the
biological actions of cardiac glycoside drugs and ACE-inhibitors, indicating that they can be used concurrently as long
as the attending physician is able to monitor patient response and adjust the dosing of these drugs accordingly. 15
From an historical standpoint, Hawthorn has been used alone and in combination with other cardiac glycoside drugs in
the management of congestive heart failure.11, 15
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Anti- Aging: (Author’s Note) Hawthorn may be an important herb in the prevention of cardiovascular disease and age-
related cardiac decline leading to the development of congestive heart failure. Studies demonstrate that after the age
of 35- 40 the heart muscle appears to make less ATP energy in a certain percentage of individuals. This has been
shown to result from a marked reduction in Coenzyme Q10 synthesis, which is required to maximize the conversion of
ADP to ATP. Theoretically, supplementation with both Coenzyme Q10 and Hawthorn extract may help to stave of
age-related declines in ATP production, due to their known inotropic effects on heart muscle. Many practitioners
involved in anti-aging medicine subscribe to this practice and recommend these supplements on a preventive basis to
their patients over 40 – 50 years of age. (see also Coenzyme Q10 in this document).
Dosage and Standardized Grade
1. Hawthorn flower extract should be standardized to contain 18 - 20 percent procyanidins or 2 –5% flavonoid content,
of which at least 1.5% is the flavonoid vitexin. 11,12,13,14,15
2. Congestive Heart Failure: In a 1993 study of 30 patients with congestive heart failure 80 mg of standardized
Hawthorn extract taken twice per day for eight weeks showed a statistically significant improvement in heart
function vs. the placebo. There were no side effects (Leuchtgens H, 1993). Blood pressure was also mildly
reduced. 10 However, other studies have used 300 – 600 mg of Hawthorn extract, three times per day, and have
shown good results in cases of congestive heart failure without generating any side effects. Thus, the dosage
range for this application is vast, ranging from 80 to 600 mg, two to three times per day, and is based upon the
severity of the condition; as more severe congestive heart failure has been shown to respond better to higher
doses. 11,12,13,14,15
3. Angina: 180 mg per day (e.g., 60 mg, three times per day) 15
4. High Blood Pressure: 100 – 250 mg, one to three times per day 23
5. Anti- Aging: For general prevention purposes 70-100 mg of standardized Hawthorn extract may be appropriate after
age 40 – 50 1,2,3,4,5,6,7
Adverse Side Effects, Toxicity and Contraindications
Hawthorn is regarded as being very safe. The German Commission E lists no known risks, contraindications, or drug
interactions with Hawthorn. Animals given very large doses of Hawthorn extract have not shown any signs of toxicity.
In clinical trials with congestive heart failure and other cardiovascular patients, reported side effects have been rare,
consisting of stomach upset and occasional allergic skin reaction.1,13,14,15
Drug-Nutrient Interactions
Hawthorn may potentiate the action of the following drugs, and therefore, requires appropriate physician monitoring if
taken concurrently with these medications. This is extremely important in the case of digitalis, digoxin and other
cardiac glycoside drugs, as it is plausible that a drug nutrient interaction of this nature could lead to life threatening
consequences.
Interactions of concern include:
1. Digitalis, digoxin and other cardiac glycoside medications 24
2. Antiarrhythmic Medications 25
3. Anti-hypertensive Medications: As Hawthorn extract is known to lower high blood pressure to some degree, it may
work synergistically with a variety of antihypertensive drugs, reducing the required dosage of the drug. 26, 27
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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. Petkov V, Plants with Hypotensive, Antiatheromatous and Coronarodilating Action, Am J Clin Med 7, 1979, 197-236.
2. Wagner H, Bladt S, and Zgainski EM, Plant Drug Analysis, Springer-Verlag, New York, 1984, 166 & 178-179.
3. Ammon HPT, Handel M, Crataegus, Toxicology and Pharmacology, I Toxicity, Planta Medica 43, 1981, 105-120, II Pharmacodynamics,
Planta Medica 43, 1981, 209-239, III Pharmacodynamics and Pharmacokinetics, Planta Medica 43(4), 1981, 313-322.
4. Mavers VWH, and Hensel H, Changes in Local Myocardial Blood Flow Following Oral Administration of a Crataegus Extract to Non-
anesthetized Dogs, Arzneimittel-Forsch 24, 1974, 783-785.
5. Roddewig VC, and Hensel H, Reaction of Local Myocardial Blood Flow in Non-anaesthetic Dogs and Anesthetized Cats to Oral and
Parental Application of Crataegus Fraction (Ologomer Procyanidins), Arzneimittel-Forsch 27, 1977, 1407-1410.
6. Rewerski VW, et.al., Some Pharmacological Properties of Oligometric Procyanidin Isolated from Hawthorn (Crataegus Oxyacantha),
Arzneimittel-Forsch 17, 1967, 490-491.
7. Uchida S, et.al., Inhibitory Effects of Condensed Tannins on Angiotensin Converting Enzyme, Jpn J Pharmacol 43, 1987, 242-245.
8. Blesken R, Crataegus in Cardiology, Forschr Med 110, 1992, 290-292.
9. O’Connoly VM, et.al., Treatment of Cardiac Performance (NYHA Stages I to II) in Advanced Age with Standardized Crataegus Special
Extract, Forschr Med 104, 1986, 805-808.
10. Leuchrgens H, Crataegus Special Extract WS 1442 in NYHA II heart failure. A Placebo Controlled Randomized Double-blind Study,
Forschr Med 111, 1993, 352-354.
11. Murray MT, The Healing Power of Herbs (2nd edition), Prima Publishing, 1995.
12. Dietary Supplement Information Bureau.www. content.intramedicine.com: Hawthorn
13. Natural Products Encyclopedia. www.consumereslab.com: Hawthorn
14. Healthnotes, Inc. 2001. www.healthnotes.com: Hawthorn
15. Principles and Practice of Phytotherapy. Mills M and Bone K. Churchill Livingstone.2000: 444-445
16. Wagner H et al. Cardioactive Drugs IV. Cardiotonic amines from crataegus oxyacantha. Planta Medica 1982;45:99-101
17. Weihmayr T, Ernst E. Therapeutic effectiveness of crataegus. Forschr Med 1996;114:27-9
18. Tauchert M. Efficacy and safety of crataegus extract WS 1442 in comparison with placebo in patients with chronic stable New York heart
Association class-III heart failure. Am Heart J 2002;143(5):910-5
19. Tauchert M, Siegel G, Schulz V. Hawthorn extract as plant medication for the heart; a new evaluation of it therapeutic effectivenss
[translated from German]. MMW Munch Med Wochenschr. 1994;136(suppl 1):S3-S5
20. Popping S, Rose H, Ionescu I et al. Effect of a hawthorn extract on contraction and energy turnover of isolated rat cardiomyocytes.
Arzneimittelforschung 1995;45:1157-61
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21. Joseph G, Zhao Y, Klaus W. Pharmacolgic action profile of crataegus extract in comparison to epinephrine, amirinone, milrinone and
digoxin in the isolated perfused guinea pig heart [in German; English abstract]. Arzneimittelforschung 1995;45:1261-5
22. Schulz V, Hansel R, Tyler VE. Rational Phytotherapy: A Physician’s Guide to Herbal medicine. 3rd ed. Berlin, Germany, Springer-Verlag
1998:91-4
23. Murray M, Pizzonro J. Encylopedia of Natural Medicine (2nd ed) Prima Publishing 1997:524-35
24. Petkov V. Plants and hypotensive, Antiatheromatous and coronarodilatating action. Am J Chinese Med 1979;7:197-236
25. Wagner H et al. Cardioactive Drugs IV. Cadiotonic amines from crataegus oxyacantha. Planta Medica 1982;45:99-101
26. Uchida S et al. Inhibitory effects of condensed tannins on agiotensin converting enzyme. Jap J Pharmacol 1987;43(2):242-6
27. Taskov M. On the coronary and cardiotonic action of crataemon. Acta Physiol Pharmacol Bulg 1977;3(4):53-7
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Horsechestnut seed (Aesculus hippocastanum)
General Features
The Horsechestnut tree is native to Asia and Northern Greece, but is now cultivated in many areas of Europe and
North America and is mainly grown as an ornamental tree in parks and gardens. Unlike true chestnuts, the seeds
(nuts) of the Horsechestnut are not edible, but an extract containing active ingredients from the seed has been used
for a few centuries in Germany for the treatment of chronic venous insufficiency. In fact, in Germany more
prescriptions are written for the oral, standardized Horsechestnut extract as a treatment for chronic venous
insufficiency, than for any other drug or supplement.1,2,3,4 Numerous clinical trials have documented the efficacy of
Horsechestnut supplementation in the treatment of chronic venous insufficiency and related circulatory problems.1
Principle Active Constituents
The major active constituents are considered to be saponins, referred to as escin, which is a complex and unique
mixture of over thirty individual pentacyclic triterpene diester glycosides.
Other key constituents include flavonoids, sterols and lipids.1,4,5,6,7,8,9
Clinical Application and Mechanism of Action
1. Chronic Venous Insufficiency
Chronic Venous Insufficiency is an imprecise term, which refers to the impairment of venous return, usually from
the legs, and often involves edema (swelling), leg pain, fatigue and/or heaviness upon standing or walking, and
possibly skin discoloration.1,7,9,10,11,12 Other terms used to describe the same condition include deep vein
incompetence, peripheral venous incompetence and early stage varicose veins.1,4 This condition has been reported
to affect 10-15% of men and 20-25% of women.9 Numerous clinical trials have shown that the oral administration of
the standardized grade of Horsechestnut seed can effectively treat chronic venous insufficiency in a large
percentage of cases. Many double-blind, placebo-controlled studies reveal that it has proven to be effective on a
consistent basis and can outperform the use of compression stockings, which are often used in the management of
this condition. Studies reveal that Horsechestnut supplementation objectively improves venous tone, without
arterial constriction or a rise in blood pressure. It has been shown to reduce leg volume in these patients versus
the placebo group, and has outperformed use of support stockings in regards to this outcome. Overall, patients
consistently report reduced leg pain, swelling, heaviness, pain, and fatigue with the use of Horsechestnut seed
extract.1,4,7,9,10,11,12,13,14,15
As for the mechanism of action, the escin component (triterpene saponins) of Horsechestnut extract acts by
reducing capillary permeability to water, essentially helping to seal off the escape of water out of veins into the
extravascular space. It has also been shown to improve tone of connective tissues within veins and block the
breakdown of ground substance (proteoglycans), which provides important structural integrity to veins.
Horsechestnut seed ingredients have been shown to inhibit the enzymes that breakdown these important
proteoglycans and to inhibit lysosomal enzymes and hyaluronidase enzyme, which are both known to break down
tissue structure. Horsechestnut seed extract has also been shown to possess antioxidant properties. The
combination of these effects accounts for the ability of this supplement to reduce localized edema and
inflammation, increase venous pressure and flow, reduce venous deformity and distension, and reduce leg, ankle
and foot circumference in afflicted individuals and in healthy subjects studied during a 15-hour air flight, who fared
better in these measurements than did the placebo group.1,6,8
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