CHANG ET AL HAWTHORN HERBAL MEDICINE HERBAL MEDICINE Hawthorn Qi Chang, PhD, Zhong Zuo, PhD, Francisco Harrison, MD, and Moses Sing Sum Chow, PharmD H awthorn, a common name of all plant species in the genus Crataegus, is a thorny shrub or small tree that normally has bright green leaves, white flow- ers, and bright red berries (Figure 1), each containing one to three or five seeds, depending on the species. 1 Hawthorn is a member of the Rosaceae family and is recognized to have approximately 280 species primar- ilyfromnortherntemperatezonesinEastAsia,Europe, and eastern North America. 2,3 It is a widely used herb for preventing and treating cardiovascular diseases. At present, more than 20 species of hawthorn are used as herbal drugs or drug materials in the world. 4 Some of them are officially listed in the pharmacopoe- ias of many countries such as China, Germany, France, and England (Table I). HISTORY AND TRADITIONAL USES Hawthorn has a long history of use in traditional Chi- nesemedicine(TCM)andEuropeanherbalmedicine.It was first mentioned for TCM in Tang Ben Cao, 5 the world’s first official pharmacopoeia in 659 A.D. In Eu- rope, the use of hawthorn can be dated back to the time of Dioscorides in the first century A.D. 6 Its use for the treatment of heart disease began in the late 1800s. 7 In TCM, hawthorn fruits are used for stimulating di- gestion and promoting the function of the stomach, im- proving blood circulation, and removing blood stasis. Thus,theyareusedinprescriptionstotreatindigestion with epigastric distension, diarrhea, and abdominal pain;amenorrhea;hypertension;andhyperlipidemia. 8 In Europe, hawthorn fruits, leaves, flowers, or a combination thereof have been traditionally used as an astringent, antispasmodic, cardiotonic, diuretic, hypotensive, and antiatherosclerotic agent. 3 The herb is used to treat various heart problems, including heart failure, New York Heart Association (NYHA) stagesI-II,anginapectoris,hypertensionwithmyocar- dial insufficiency, mild alterations of cardiac rhythm, and atherosclerosis. 8 Both in China and Europe, hawthorn fruit is con- sumed not only for medicinal purposes mentioned above but also as foodstuff (e.g., canned fruit, jam, jelly, drink, and wine). 3 CHEMICAL CONSTITUENTS Hawthorn fruits, leaves, and flowers contain a number of chemical constituents, such as flavonoids (0.1%-1% in fruits, 1%-2% in leaves and flowers), 9-11 oligomeric proanthocyanidins (OPCs, 1%-3% in fruits or leaves with flowers), 10,12,13 triterpene acids (0.5%-1.4% in fruits), 3 organic acids (2%-6%), 14 sterols, and trace amounts of cardioactive amines. 15 Among these, flavonoids and OPCs are the two major groups of bioactive components. Many hawthorn preparations are standardized based on their flavonoid and OPC contents. Specific compounds and their structure, rep- resentative of the main chemical groups, are shown in Figures 2 to 5. J Clin Pharmacol 2002;42:605-612 605 A review with 54 references covers all aspects of hawthorn, the genus Crataegus, including its traditional uses, chemical constituents, pharmacological activities, and clinical effects. Although the effectiveness of hawthorn on the treatment of cardiovascular diseases has received extensive attention worldwide, further scientific research on various areas such as pharmacokinetics, mechanism of actions will be neces- sary to ensure its safe and effective usage. Journal of Clinical Pharmacology, 2002;42:605-612 ©2002 the American College of Clinical Pharmacology From the School of Pharmacy, Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, SAR, PRC (Dr. Chang, Dr. Zuo, Dr. Chow) and Harrison Clinical Research, München, Germany (Dr. Harrison). Submitted for publication December 15, 2001; revised version accepted February 16, 2002. Address for reprints: Dr. Zhong Zuo, School of Pharmacy, Chi- nese University of Hong Kong, Shatin, N.T. Hong Kong.