Randolph Horner 04.01.02
Nearly five million Americans are afflicted with congestive heart failure (CHF), with 400,000 new cases and 200,000 fatalities per year. Half of patients diagnosed die within five years, a survival rate comparable to some forms of cancer. The medical costs associated with CHF in the U.S. total $5 billion per year and is projected to increase as the population ages1.
The underlying pathology in CHF is an inability to maintain cardiac output, accommodate venous return and maintain the metabolic requirements of the body. The reduced circulation results in metabolic cyanosis, reduced renal excretion during the day and increased renal excretion at night. In an effort to compensate for insufficient circulation, the heart increases the number of contractions. This results in an enlargement of the heart, progressive thickening of the heart muscle fibers and enlarged chamber volume. Resulting heart remodeling and increased tissue mass increases the oxygen requirement of the organ1.
Hawthorn extract made from leaves with flower (flowering twig tips) has been researched and found to be effective for CHF. Extracts, principally of the species Crataegus monogyna and C. oxycantha, may be standardized to flavone glycosides or oligomeric proanthocyanidins. Many quality European products are standardized to 1.8 to 2.2% vitexin1.
German studies have shown an increased cardiac stroke volume and elevated coronary blood flow with the use of hawthorn extract. This improves coronary perfusion and cardiac efficiency, while promoting heart health. It has been proposed that hawthorn flavonoids inhibit cellular phosphodiesterase and increase cellular concentrations of cyclic adenosine monophosphate (cAMP). Therapeutic dosages referenced in clinical trials are 160-480 mg per day and a prophylactic dosage is 80 mg 1-2 times a day1.
There are approximately 280 known species of hawthorn in the genus Crataegus2. The plant material used for botanical extraction is a spiny shrub native to the northern wooded temperate zones of eastern North America and Europe, including the U.K. and other European countries3, Albania, Bulgaria, Romania, the former Yugoslavia and Poland4.
During its long history of use hawthorn has maintained a record of confirmed safety, with clinical evidence to support its cardiovascular benefits. The fruits (berries) of various species, well known to traditional European herbal medicine, are edible5. Hawthorn was noted by the first century Greek herbalist Dioscorides and later by Swiss physician Paracelsus6. However, clinical use for heart disease and cardiovascular disorders did not begin in Europe until the nineteenth century7, 8.
Hawthorn leaf with flower consists of dried flowering twig tips of Crataegus monogyna Jaquin (Lindman) or other members of the Crataegus genus, containing 1-3% oligomeric proanthocyanidins; 1-2% flavonoids, including flavonols and flavone derivatives such as hyperoside, vitexinrhamnose, rutin and vitexin; amines (choline, acetylcholine, trimethylamine); catechins; phenol carboxylic acids (e.g., chlorogenic acid); purines; sterols and approximately 0.6% triterpene acids (oleanolic, ursolic and crataegolic acids)4,9,10.
Pharmacological investigations have shown that the most important components in terms of improving the peripheral vascular system are flavonoids, flavonglycosides (quercetin, rutin, hyperoside and vitexin), procyanidine derived from catechin or epicatechin (oligomeric procyanidines), pentacyclical triterpenes and aromatic carbon dioxides. As long as a specific effectiveness can't be assigned to a single substance, the entire Crataegus extract must be viewed as the effective treatment11.
The New York Heart Association classifies Stage II cardiac insufficiency (Stage II NYHA) as resulting in "fatigue or shortness of breath during heavy exertion and possibly during normal activities12." In an eight week, multicenter, double blind study of exercise ability, 78 patients were measured for work output on the ergometer bicycle. Work capacity increased significantly for the group taking 200 mg of hawthorn extract three times daily, along with decreases in systolic blood pressure, heart rate and subjectively reported feelings of health, while the placebo group exhibited no change13. In a similar study of 136 Stage II patients,a clear improvement was confirmed in major symptoms such as restricted physical performance, shortness of breath (dyspnea) and ankle edema. Moreover, improvement in quality of life was noted, including a "better sense of mental well being14." When compared with the ACE inhibitor captopril in a multicenter, double blind study of 132 NYHA Stage II subjects, 900 mg daily of hawthorn extract produced benefits similar to those of the pharmaceutical product, without any serious adverse effects15.
Investigations of acute toxicity using a hydroalcoholic dry extract (drug/extract ratio 5:1, standardized for oligomeric procyanidins) recorded no fatal events occurring after oral or peritoneal administration in mice or rats in doses of up to 3 g per kg of body weight. No toxic effects were observed after oral administration of 30, 90 and 300 mg aqueous/ethanolic dry extract per kg body weight in rats and dogs over a period of 26 weeks. For this extract, the "no effect" dose was 300 mg per kg body weight. Isolated human artery studies have concluded that Crataegus extract dilates the coronary arteries to cause a more effective flow of blood to the heart11. Observations in human subjects confirm the experimental results: improvement of symptoms and of electrocardiogram (ECG) readings in patients with mild cardiac insufficiency (with long term oral administration of aqueous extract), decrease in rhythm and improvement of systolic contraction16.
Commission E approved the use of hawthorn leaf with flower for cases of decreased cardiac output as described in functional Stage II (NYHA). Hawthorn has been used in cases of mild bradyarrhythmia, paroxymsmal tachycardia, hypertension, arteriosclerosis, Buerger's disease and for relief of the feeling of pressure and tightness in the cardiac region4. Hawthorn is often combined with conventional cardiovascular medications (such as digitalis and oubain) to speed up cardiac compensation and prevent the indigestion and nausea associated with these treatments. It is additionally used as a sedative, antispasmodic and as a general source of flavonoids17.
It is important to note that package inserts, which accompany European over-the-counter (OTC) extracts, state that a physician must be consulted in cases where symptoms continue unchanged for longer than six weeks or in case of swelling of the legs. Medical diagnosis is absolutely necessary when pains occur in the region of the heart, spreading out to the arms, upper abdomen or the area around the neck, or in cases of dyspnea18.
Clearly, standardized hawthorn extract has been shown to be an effective phytomedicine through extensive use in Europe. Its benefit in supporting healthy heart function is due to improved utilization of oxygen and energy by the heart, along with additional cardioprotective relief from hypertension and atherosclerosis. Most significantly, it can be used in combination therapies to reduce dosages of digoxin type cardiac glycosides, lessening the risk of glycoside toxicity19.
Despite substantial history of herbal medicine and folk use of a variety of hawthorn products, however, dietary supplement applications in the U.S. should not take place in a setting of uninformed self medication, since the most profound health benefits are seen only in those individuals whose cardiovascular conditions require that they be under medical supervision. NW
About the authors: Randolph Horner is managing director of New World Nutrition, New City, NY, and clinical nutritionist Judith Eaton is nutrition science director. They develop and market functional food and beverage ingredients and products, nutraceuticals, and dietary supplements, in collaboration with manufacturers worldwide. They can be reached at New World Nutrition, 845-638-4041.
References
1. Woodman, G. 2002. Personal communication to R. Horner and J. Eaton. Feb. 25.
2. Blumenthal, M., Busse,W., Hall,T., Goldberg,A., Gruenwald,J., Riggins,C., Rister,S., editor(s), 1998. The Complete German commission E monographs-Therapeutic guide to Herbal Medicines. Klein,S. Translator. Austin: Am Bot Council. 685 p. Translation of Kommission E. Material Used with permission of the American Botanical Council.
3. British Herbal Pharmacopoeia (BHP). 1996. Exeter, U.K.: British Herbal Medicine Association. 98-101.
4. Wichtl, M. and N.G. Bisset (eds.). 1994. Herbal Drugs and Phytopharmaceuticals. Stuttgart: Medpharm Scientific Publishers.161-166.
5. Hedrick, U.P. (ed.). 1972. Sturtevant's Edible Plants of the World. New York: Dover Publications [reprint of 1919 original].
6. Weihmayr, T. and E. Ernst. 1996. "Therapeutic effectiveness of Crataegus" [In German]. Fortschr Med 114(1-2):27-29.
7. Anschutz, E.P. 1900. New, Old and Forgotten Remedies. Philadelphia, PA:Boericke and Tafel.
8. Hobbs, C. and S. Foster. 1990. "Hawthorn-a literature review." HerbalGram 22:19-33.
9. Budavari, S. (ed.). 1996. The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals, 12th ed. Whitehouse Station, N.J.: Merck & Co, Inc. 435.
10. Meyer-Buchtela, E. 1999. "Tee-Rezepturen-Ein Handbuch für Apotheker und Ärzte." Stuttgart: Deutscher Apotheker Verlag.
11. Reuter, H. 1994. "Crataegus (Hawthorn): A Botanical Cardiac Agent." Z Phytother 15:73-81.
12. New York Heart Association (NYHA). 1994. Revisions to Classification of Functional Capacity and Objective Assessment of Patients with Diseases of the Heart.
13. Schmidt, U., U. Kuhn, M. Ploch, W.D. Hubner. 1994. "Efficacy of the hawthorn (Crataegus) preparation LI 132 in 78 patients with chronic congestive heart failure defined as NYHA functional class II." Phytomedicine1:17-24.
14. Weikl, A. et al. 1996. "Crataegus special extract WS 1442. Assessment of objective effectiveness in patients with heart failure." Fortschr Med 114(24)291-296.
15. Tauchert, M., M. Ploch, W.D. Hubner. 1994. "Effectiveness of hawthorn extract LI 132 compared with the ACE inhibitor Captopril: Multicenter double blind study with 132 NYHA Stage II." Muench Med Wochenschr 136 suppl:S27-S33.
16. Bruneton, J. 1995. Pharmacognosy, Phytochemistry, Medicinal Plants. Paris:Lavoisier Publishing.
17. Upton, R. (ed.) et al. 1999b. Hawthorn Leaf with Flower. Santa Cruz, CA: American Herbal Pharmacopoeia.
18. Busse,W."Standardized Crateegus Extract Clinical Monograph." Quarterly Review of Natural Medicine, Fall 1996. 189-97.
19. McKenna,D.,Hughes,K., Jones,K., et.al., editor(s), 1998. Hawthorn Monograph on Botanical and Dietary Supplements, in Natural Dietary Supplements: A Desktop Reference. INPR, Marine on St. Croix, MN.
The underlying pathology in CHF is an inability to maintain cardiac output, accommodate venous return and maintain the metabolic requirements of the body. The reduced circulation results in metabolic cyanosis, reduced renal excretion during the day and increased renal excretion at night. In an effort to compensate for insufficient circulation, the heart increases the number of contractions. This results in an enlargement of the heart, progressive thickening of the heart muscle fibers and enlarged chamber volume. Resulting heart remodeling and increased tissue mass increases the oxygen requirement of the organ1.
Overview
Hawthorn extract made from leaves with flower (flowering twig tips) has been researched and found to be effective for CHF. Extracts, principally of the species Crataegus monogyna and C. oxycantha, may be standardized to flavone glycosides or oligomeric proanthocyanidins. Many quality European products are standardized to 1.8 to 2.2% vitexin1.
German studies have shown an increased cardiac stroke volume and elevated coronary blood flow with the use of hawthorn extract. This improves coronary perfusion and cardiac efficiency, while promoting heart health. It has been proposed that hawthorn flavonoids inhibit cellular phosphodiesterase and increase cellular concentrations of cyclic adenosine monophosphate (cAMP). Therapeutic dosages referenced in clinical trials are 160-480 mg per day and a prophylactic dosage is 80 mg 1-2 times a day1.
There are approximately 280 known species of hawthorn in the genus Crataegus2. The plant material used for botanical extraction is a spiny shrub native to the northern wooded temperate zones of eastern North America and Europe, including the U.K. and other European countries3, Albania, Bulgaria, Romania, the former Yugoslavia and Poland4.
During its long history of use hawthorn has maintained a record of confirmed safety, with clinical evidence to support its cardiovascular benefits. The fruits (berries) of various species, well known to traditional European herbal medicine, are edible5. Hawthorn was noted by the first century Greek herbalist Dioscorides and later by Swiss physician Paracelsus6. However, clinical use for heart disease and cardiovascular disorders did not begin in Europe until the nineteenth century7, 8.
Description, Chemistry and Pharmacology
Hawthorn leaf with flower consists of dried flowering twig tips of Crataegus monogyna Jaquin (Lindman) or other members of the Crataegus genus, containing 1-3% oligomeric proanthocyanidins; 1-2% flavonoids, including flavonols and flavone derivatives such as hyperoside, vitexinrhamnose, rutin and vitexin; amines (choline, acetylcholine, trimethylamine); catechins; phenol carboxylic acids (e.g., chlorogenic acid); purines; sterols and approximately 0.6% triterpene acids (oleanolic, ursolic and crataegolic acids)4,9,10.
Pharmacological investigations have shown that the most important components in terms of improving the peripheral vascular system are flavonoids, flavonglycosides (quercetin, rutin, hyperoside and vitexin), procyanidine derived from catechin or epicatechin (oligomeric procyanidines), pentacyclical triterpenes and aromatic carbon dioxides. As long as a specific effectiveness can't be assigned to a single substance, the entire Crataegus extract must be viewed as the effective treatment11.
The Research
The New York Heart Association classifies Stage II cardiac insufficiency (Stage II NYHA) as resulting in "fatigue or shortness of breath during heavy exertion and possibly during normal activities12." In an eight week, multicenter, double blind study of exercise ability, 78 patients were measured for work output on the ergometer bicycle. Work capacity increased significantly for the group taking 200 mg of hawthorn extract three times daily, along with decreases in systolic blood pressure, heart rate and subjectively reported feelings of health, while the placebo group exhibited no change13. In a similar study of 136 Stage II patients,a clear improvement was confirmed in major symptoms such as restricted physical performance, shortness of breath (dyspnea) and ankle edema. Moreover, improvement in quality of life was noted, including a "better sense of mental well being14." When compared with the ACE inhibitor captopril in a multicenter, double blind study of 132 NYHA Stage II subjects, 900 mg daily of hawthorn extract produced benefits similar to those of the pharmaceutical product, without any serious adverse effects15.
Investigations of acute toxicity using a hydroalcoholic dry extract (drug/extract ratio 5:1, standardized for oligomeric procyanidins) recorded no fatal events occurring after oral or peritoneal administration in mice or rats in doses of up to 3 g per kg of body weight. No toxic effects were observed after oral administration of 30, 90 and 300 mg aqueous/ethanolic dry extract per kg body weight in rats and dogs over a period of 26 weeks. For this extract, the "no effect" dose was 300 mg per kg body weight. Isolated human artery studies have concluded that Crataegus extract dilates the coronary arteries to cause a more effective flow of blood to the heart11. Observations in human subjects confirm the experimental results: improvement of symptoms and of electrocardiogram (ECG) readings in patients with mild cardiac insufficiency (with long term oral administration of aqueous extract), decrease in rhythm and improvement of systolic contraction16.
Uses of Hawthorn
Commission E approved the use of hawthorn leaf with flower for cases of decreased cardiac output as described in functional Stage II (NYHA). Hawthorn has been used in cases of mild bradyarrhythmia, paroxymsmal tachycardia, hypertension, arteriosclerosis, Buerger's disease and for relief of the feeling of pressure and tightness in the cardiac region4. Hawthorn is often combined with conventional cardiovascular medications (such as digitalis and oubain) to speed up cardiac compensation and prevent the indigestion and nausea associated with these treatments. It is additionally used as a sedative, antispasmodic and as a general source of flavonoids17.
It is important to note that package inserts, which accompany European over-the-counter (OTC) extracts, state that a physician must be consulted in cases where symptoms continue unchanged for longer than six weeks or in case of swelling of the legs. Medical diagnosis is absolutely necessary when pains occur in the region of the heart, spreading out to the arms, upper abdomen or the area around the neck, or in cases of dyspnea18.
Clearly, standardized hawthorn extract has been shown to be an effective phytomedicine through extensive use in Europe. Its benefit in supporting healthy heart function is due to improved utilization of oxygen and energy by the heart, along with additional cardioprotective relief from hypertension and atherosclerosis. Most significantly, it can be used in combination therapies to reduce dosages of digoxin type cardiac glycosides, lessening the risk of glycoside toxicity19.
Despite substantial history of herbal medicine and folk use of a variety of hawthorn products, however, dietary supplement applications in the U.S. should not take place in a setting of uninformed self medication, since the most profound health benefits are seen only in those individuals whose cardiovascular conditions require that they be under medical supervision. NW
About the authors: Randolph Horner is managing director of New World Nutrition, New City, NY, and clinical nutritionist Judith Eaton is nutrition science director. They develop and market functional food and beverage ingredients and products, nutraceuticals, and dietary supplements, in collaboration with manufacturers worldwide. They can be reached at New World Nutrition, 845-638-4041.
References
1. Woodman, G. 2002. Personal communication to R. Horner and J. Eaton. Feb. 25.
2. Blumenthal, M., Busse,W., Hall,T., Goldberg,A., Gruenwald,J., Riggins,C., Rister,S., editor(s), 1998. The Complete German commission E monographs-Therapeutic guide to Herbal Medicines. Klein,S. Translator. Austin: Am Bot Council. 685 p. Translation of Kommission E. Material Used with permission of the American Botanical Council.
3. British Herbal Pharmacopoeia (BHP). 1996. Exeter, U.K.: British Herbal Medicine Association. 98-101.
4. Wichtl, M. and N.G. Bisset (eds.). 1994. Herbal Drugs and Phytopharmaceuticals. Stuttgart: Medpharm Scientific Publishers.161-166.
5. Hedrick, U.P. (ed.). 1972. Sturtevant's Edible Plants of the World. New York: Dover Publications [reprint of 1919 original].
6. Weihmayr, T. and E. Ernst. 1996. "Therapeutic effectiveness of Crataegus" [In German]. Fortschr Med 114(1-2):27-29.
7. Anschutz, E.P. 1900. New, Old and Forgotten Remedies. Philadelphia, PA:Boericke and Tafel.
8. Hobbs, C. and S. Foster. 1990. "Hawthorn-a literature review." HerbalGram 22:19-33.
9. Budavari, S. (ed.). 1996. The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals, 12th ed. Whitehouse Station, N.J.: Merck & Co, Inc. 435.
10. Meyer-Buchtela, E. 1999. "Tee-Rezepturen-Ein Handbuch für Apotheker und Ärzte." Stuttgart: Deutscher Apotheker Verlag.
11. Reuter, H. 1994. "Crataegus (Hawthorn): A Botanical Cardiac Agent." Z Phytother 15:73-81.
12. New York Heart Association (NYHA). 1994. Revisions to Classification of Functional Capacity and Objective Assessment of Patients with Diseases of the Heart.
13. Schmidt, U., U. Kuhn, M. Ploch, W.D. Hubner. 1994. "Efficacy of the hawthorn (Crataegus) preparation LI 132 in 78 patients with chronic congestive heart failure defined as NYHA functional class II." Phytomedicine1:17-24.
14. Weikl, A. et al. 1996. "Crataegus special extract WS 1442. Assessment of objective effectiveness in patients with heart failure." Fortschr Med 114(24)291-296.
15. Tauchert, M., M. Ploch, W.D. Hubner. 1994. "Effectiveness of hawthorn extract LI 132 compared with the ACE inhibitor Captopril: Multicenter double blind study with 132 NYHA Stage II." Muench Med Wochenschr 136 suppl:S27-S33.
16. Bruneton, J. 1995. Pharmacognosy, Phytochemistry, Medicinal Plants. Paris:Lavoisier Publishing.
17. Upton, R. (ed.) et al. 1999b. Hawthorn Leaf with Flower. Santa Cruz, CA: American Herbal Pharmacopoeia.
18. Busse,W."Standardized Crateegus Extract Clinical Monograph." Quarterly Review of Natural Medicine, Fall 1996. 189-97.
19. McKenna,D.,Hughes,K., Jones,K., et.al., editor(s), 1998. Hawthorn Monograph on Botanical and Dietary Supplements, in Natural Dietary Supplements: A Desktop Reference. INPR, Marine on St. Croix, MN.
