Plant Part Used
Flower, leaf, and berry
Active Constituents
Flavonoid glycosides (leaf containing quercitin, rutin, fruit containing hyperoside, vitexin-4’-rhamnoside, oligomeric procyanidins), adenosine (leaf).(1),(2)
[span class=alert]This section is a list of chemical entities identified in this dietary supplement to possess pharmacological activity. This list does not imply that other, yet unidentified, constituents do not influence the pharmacological activity of this dietary supplement nor does it imply that any one constituent possesses greater influence on the overall pharmacological effect of this dietary supplement.[/span]
Introduction
Hawthorn is a spiny shrub native to the wooded temperate zones of Europe. Hawthorn is one of the oldest recorded traditional medicines, first reported by the Greek herbalist Dioscoridies.(3) Roman physicians used hawthorn as a heart drug in the first century A.D., but most of the literature from that period focuses on its symbolic use for religious rites and political ceremonies. During the Middle Ages, hawthorn was used for the treatment of dropsy, or congestive heart failure. It was also used for treating other heart ailments as well as for sore throat.
In Phytomedicine, hawthorn supplementation refers to the use of the leaf/flower and/or a mixture with the berry of the genus Crataegus (usually referring to either C. laevigata, syn. C. oxyacantha and C. monogyna). Most studies have been performed on standardized hawthorn leaf and flower, which is also the monograph approved by the German Commission E. Positive human studies have been performed using a standardized berry, leaf, and flower product.(3)
Interactions and Depletions
Interactions
Dosage Info
Dosage Range
250 mg (standardized extract), 1 to 3 times a day.
Berry: 300 mg to 1 g, 3 times a day.
Liquid extract (1:4 w/v): 1-2 ml, 3 times a day.
Leaf and Flowers Extract: 160-900 mg = to 3.5-19.8 mg flavonoids daily.
Most Common Dosage
250 mg (standardized extract), 2 times a day.
Berry: 300 mg, 3 times a day.
Liquid extract (1:4 w/v): 1 ml, 3 times a day.
Leaf and Flowers Extract: 160 mg = to 3.5 mg flavonoids daily.
Standardization
[span class=doc]Standardization represents the complete body of information and controls that serve to enhance the batch to batch consistency of a botanical product, including but not limited to the presence of a marker compound at a defined level or within a defined range.[/span]
The most current available medical and scientific literature indicates that this dietary supplement should be standardized to 2% vitexin-2” rhamnoside OR 20% procyanidins.
Uses
Frequently Reported Uses
- Antioxidant
- Angina
- Chronic heart failure (CHF)
- Peripheral Vascular Disorders
- Hypotension, Hypertension
- Cardiotonic
Other Reported Uses
- Cholesterol Lowering
- Vascular Spasm (Raynaud’s)
- Arrhythmias
Toxicities & Precautions
General
No known toxicities in recommended dosages.(4),(22)
Pregnancy/ Breast Feeding
Based on pharmacology, do not use in pregnancy due to uteroactivity in vivo and in vitro (reduced tone and motility).(4)
Age Limitations
Do not use in children under 2 years of age unless recommended by a physician.
Pharmacology
Hawthorn is currently used extensively by physicians in Europe in its standardized form for NYHA class II heart failure and various other cardiovascular and peripheral circulatory conditions, including angina, cardiac degeneration not yet requiring digitalis, and mild bradycardia.(5),(6),(7) Hawthorn appears to exert a positive inotropic effect while increasing the cardiac refractory period.(8) Extracts have been reported to have a protective effect against reperfusion arrhythmias in laboratory animals.(9),(23) Its combination of effects on the heart leads to its use as a cardiotonic, especially for the elderly where mitral stenosis and chronic heart failure may be present. Laboratory studies have reported a reduction in blood pressure due to arteriosclerosis and chronic nephritis with the use of hawthorn.(10) Hawthorn may also be used for peripheral vascular diseases where circulation is impaired, such as Raynaud’s disease.
Hawthorn is used in Europe by physicians for conditions where digitalis is not yet indicated, and may possibly help in maintaining digoxin levels while decreasing the need for the pharmaceutical medication.(11) Hawthorn is reported to have the ability to regulate both low and high blood pressure, with its bioflavonoids reportedly dilating both peripheral and coronary blood vessels, which leads to its use in angina.(1) The procyanidin content is claimed to support the spasmolytic effects on the vessels.(12) The antioxidant oligoproanthocyanidins (OPC) content is also thought to be responsible for the coronary circulatory effects, increasing the amplitude of the heartbeat.(13) Hawthorn’s glycoside component reportedly may also increase the vagal tone of the heartbeat.(14) Hawthorn has also been reported to have angiotensin-converting enzyme inhibiting effects.(15),(16)
Hawthorn has been reported to improve the functioning of the heart without affecting heart rate or blood pressure at rest, but its use does seemingly result in a decreased rise of these parameters with exercise.(16) Laboratory studies have reported that proanthocyanidins may actually reverse atherosclerotic plaque.(17) Hawthorn reportedly has the ability to increase intracellular vitamin C and has a protective effect on oxidative processes.(18)
A 1994 review of the literature on using standardized hawthorn supplements revealed 15 human clinical trials on 872 patients.(19) In one multicenter, double-blind study, a standardized hawthorn extract compared favorably to captopril (37.5mg daily) in the treatment of 132 individuals with NYHA Stage II cardiac insufficiency.(20) Both captopril and hawthorn are reported to help reduce peripheral blood flow resistance, but hawthorn has the added capability of being a cardio-tonic agent also. A placebo controlled, randomized, parallel group, multicenter trial involving 143 patients with cardiac failure NYHA class II were given standardized extract of Crataegus berries. The results were fatigue and dyspnea did not occur until higher wattage had been reached during bicycle exercise.(21)
In a double blind, randomized, placebo controlled study, 136 patients (NYHA class II heart failure) were administered either 160mg of a hawthorn standardized extract per day or placebo. The difference between the pressure/heart rate product (PHRP) at a 50-W load versus rest was measured before and after treatment, with the change in this parameter defined as the primary target parameter. The group receiving the standardized hawthorn supplement reported a significant improvement in the PHRP, whereas, in the placebo group, this parameter tended to deteriorate. Patients subjectively reported perceived benefits from hawthorn use, such as a decrease in symptoms of circulatory insufficiency and an increase in the quality of life.(6)
The cardio-protective qualities of an oral standardized hawthorn extract were demonstrated in a placebo controlled, laboratory animal study.(7) An ischemia/reperfusion model was used, where one group of rats received placebo and another a standardized extract of hawthorn leaf/flower. Treatment with the hawthorn supplement effectively protected the animals from reperfusion-induced arrhythmia, mortality, and hypotensive crisis, as observed in the control animals after 7 minutes of coronary occlusion. The authors concluded that these findings may indicate uses of hawthorn to include not only early but also in advanced stages of heart failure and for secondary prevention after myocardial infarction.
A 2008 Cochrane Database System Review looked at 14 randomized, double-blind, and placebo controlled studies using hawthorn leaf and flower extract in the treatment of chronic heart failure (CHF).(24) In most of the studies, hawthorn was used as an adjunct to conventional treatment.,Hawthorn extract was more beneficial than placebo for the physiologic outcome of maximal workload, exercise tolerance was significantly increased, the pressure-heart rate product (an index of cardiac oxygen consumption) was improved, and symptoms such as shortness of breath and fatigue improved significantly. The authors concluded that based on clinical studies, hawthorn extract is an effective adjunctive treatment for chronic heart failure.
Another randomized, double-blind, placebo-controlled multicenter study in adults with NYHA class II or III CHF and reduced left ventricular ejection found that giving 900mg/day of standardized hawthorn extract reduced sudden cardiac death by 39.7%.(25)
However, a 2009 randomized, double-blind, placebo-controlled trial in 120 ambulatory patients with New York Heart Association (NYHA) class II-III chronic heart failure received conventional treatment along with either hawthorn 450 mg twice daily or placebo for 6 months.(26) Hawthorn was found to provide no symptomatic or functional benefit when given with standard medical therapy to patients with heart failure. Another study reported patients with mild to moderate CHF receiving standardized hawthorn extract were 3.9 times more likely to experience an increase in the early risk of HF progression.(27) Further research should be performed in these areas.
Of interest is an in vitro study using hawthorn extract incubated with cultured blood lymphocytes from human volunteers.(28) The researchers found that after exposure of the lymphocytes to radiation, hawthorn extract ingestion seemed to protect the lymphocytes from radiation damage, suggesting a potential role of hawthorn in radiation exposure protection.
References
- Wagner H, et al. Cardioactive Drugs IV. Cardiotonic Amines from Crataegus oxyacantha. Planta Medica. 1982;45:99-101.
- Nikolov N, et al. New Flavonoid-glycoside from Crataegus monogyna and Crataegus pentagyna. Planta Medica. 1982;44:50-53.
- Blumenthal M, Goldberg A, Brinckmann J. Herbal Medicine: Expanded Commission E Monographs. Newton, MA: Integrative Medicine Communitcations; 2000:182-191.
- Ammon HPT, et al. Crataegus, Toxicology and Pharmacology. Part I: Toxicity. Planta Medica. 1981;43(2):105-20.
- View Abstract: Petkov V. Plants and Hypotensive, Antiatheromatous and Coronarodilatating Action. Am J Chinese Med. 1979;7:197-236.
- View Abstract: Weikl A, Assmus KD, Neukum-Schmidt A, et al.[Crataegus Special Extract WS 1442: Assessment of Objective Effectiveness in Patients with Heart Failure]. Fortschr Med. 1996;114:291–296.
- Krzeminski T, Chatterjee SS. Ischemia and Early Reperfusion Induced Arrhythmias: Beneficial Effects of an Extract of Crataegus oxyacantha L. Pharm Pharmacol Lett. 1993;3:45–48.
- Gildor A. Crataegus oxyacantha and Heart Failure. Circulation. Nov1998;98(19):2098.
- View Abstract: al Makdessi S, Sweidan H, Dietz K, et al. Protective Effect of Crataegus oxyacantha Against Reperfusion Arrhythmias after Global No-flow Ischemia in the Rat Heart. Basic Res Cardiol. Apr1999;94(2):71-7.
- Racz-Kotilla E, et al. Salidiuretic and Hypotensive Action of Ribes-Leaves. Planta Medica. 1980;29:110-14.
- View Abstract: Blesken R. Crataegus in cardiology. Fortschr Med. 1992;110(15):290-292.
- Rewerski W, et al. Some Pharmacological Properties of Flavan Polymers Isolated from Hawthorn. Arzneim-Forsch/Drug Res. 1967;17:490-91.
- View Abstract: Taskov M. On the Coronary and Cardiotonic Action of Crataemon. Acta Physiol Pharmacol Bulg. 1977;3(4):53-57.
- Petkov E, et al. Inhibitory Effect of Some Flavonoids and Flavonoid Mixtures on Cyclic AMP Phosphodiesterase Activity of Rat Heart. Planta Medica. 1981;43:183-86.
- View Abstract: Lacaille-Dubois, Franck U, Wagner H. Search for Potential Angiotensin Converting Enzyme (ACE)-Inhibitors from Plants. Phytomedicine. Jan2001;8(1):47-52.
- View Abstract: Uchida S, et al. Inhibitory Effects of Condensed Tannins on Angiotensin Converting Enzyme. Jap J Pharmacol. 1987;43(2):242-46.
- View Abstract: Wegrowski J, Robert AM, Moczar M. The Effect of Procyanidolic Oligomers on the Composition of Normal and Hypercholesterolemic Rabbit Aortas. Biochem Pharm. 1984;33:3491-97.
- Gabor M. Pharmacologic Effects of Flavonoids on Blood Vessels. Angiologica. 1972;9:355-74.
- Reuter H. Crataegus (Hawthorn): A Botanical Cardiac Agent. Z Phytother. 1994;15:73-81.
- Tauchert M, Ploch M, Huebner WD. Effectiveness of Hawthorn Extract LI132 Compared with the ACE Inhibitor Captopril: Multicenter double-blind study with 132 NYHA Stage II. Muench Med Wochenschr. 1994;136(supp):S27-S33.
- View Abstract: Degenring FH, Suter A, Weber M, Saller R. A randomised double blind placebo controlled clinical trial of a standardised extract of fresh Crataegus berries (Crataegisan) in the treatment of patients with congestive heart failure NYHA II. Phytomedicine. 2003;10(5):363-9.
- Daniele C, Mazzanti G, Pittler MH, Ernst E. Adverse-event profile of Crataegus spp.: a systematic review Drug Saf. 2006;29(6):523-535.Review.
- Swaminathan JK, Khan M, Mohan IK, et al. Cardioprotective properties of Crataegus oxycantha extract against ischemia-reperfusion injury. Phytomedicine. 17 Feb 2010. [Epub ahead of print]
- Pittler MH, Guo R, Ernst E. Hawthorn extract for treating chronic heart failure. Cochrane Database Syst Rev. 23 Jan 2008;(1):CD005312. Review.
- Holubarsch CJ, Colucci WS, Meinertz T, Gaus W, Tendera M; Survival and Prognosis: Investigation of Crataegus Extract WS 1442 in CHF (SPICE) trial study group. The efficacy and safety of Crataegus extract WS 1442 in patients with heart failure: the SPICE trial. Eur J Heart Fail. Dec 2008;10(12):1255-1263. Epub 2008 Nov18.
- Zick SM, Vautaw BM, Gillespie B, Aaronson KD. Hawthorn Extract Randomized Blinded Chronic Heart Failure (HERB CHF) trial. Eur J Heart Fail. Oct 2009;11(10):990-999.
- Zick SM, Gillespie B, Aaronson KD. The effect of Crataegus oxycantha Special Extract WS 1442 on clinical progression in patients with mild to moderate symptoms of heart failure. Eur J Heart Fail. Jun 2008;10(6):587-593. Epub 2008 May19.
- Hosseinimehr SJ, Mahmoudzadeh A, Azadbakht M, Akhlaghpoor S. Radioprotective effects of Hawthorn against genotoxicity induced by gamma irradiation in human blood lymphocytes. Radiat Environ Biophys. Feb 2009;48(1):95-98. Epub 2008 Sep 4.
