Plant Profiler

Hawthorn (Crataegus oxyacanthoides)


Synonyms / Common Names / Related Terms
Aubepine, bei shanzha, bianco spino, bread and cheese tree, Cardiplant®, Chinese hawthorn, cockspur, cockspur thorn, crataegi flos, Crataegi folium, Crataegi folium cum flore, Crataegi fructus, Crataegi herba, Crataegisan , Crataegus azaerolus, Crataegus cuneata, Crataegus fructi, Crataegus monogyna, Crataegus nigra, Crataegus oxyacanthoides, Crataegus pentagyna, Crataegus pinnatifida, Crataegus sinaica boiss, Crataegus special extract WS 1442, Crataegutt®, English hawthorn, epicatechin, epine blanche, epine de mai, Fructus oxyacanthae, Fructus spinae albae, gazels, haagdorn, hagedorn, hagthorn, halves, harthorne, haw, Hawthorne Berry®, Hawthorne Formula®, Hawthorne Heart®, Hawthorne Phytosome®, Hawthorne Power®, hawthorn tops, hazels, hedgethorn, huath, hyperoside, isoquercitrin, ladies' meat, LI 132, may, mayblossoms, maybush, mayhaw, maythorn, mehlbeerbaum, meidorn, nan shanzha, northern Chinese hawthorn, oneseed, oneseed hawthorn, quickset, red haw, RN 30/9, sanza, sanzashi, shanza, shan zha rou, southern Chinese hawthorn, thorn-apple tree, thorn plum, tree of chastity, Washington thorn, weissdorn, Weissdornblaetter mit Blueten, whitethorn, whitethorn herb, WS 1442.

Mechanism of Action
Pharmacology:
  • Constituents: Hawthorn is a flowering shrub of the rose family, common in Europe. Due to widespread hybridization, the species of Crataegus are difficult to distinguish. Multiple species are commonly found in Hawthorn preparations, including: C. laevigata, C. oxyacantha, and C. monogyna. Major pharmacologically active components are believed to be flavonoids, such as hyperoside and vitexin and procyanidins.
  • Antineoplastic effects: Hawthorn may exhibit antineoplastic activity and collagen stabilizing actions. Two triterpenes, uvaol and ursolic acid, were isolated from Crataegus pinnatifida and made responsible for cytotoxicity against human and murine cancer cell lines.6 Triterpenes-enriched fractions of hawthorn extract have demonstrated almost complete inhibition of cultured larynx cancer cell growth and stronger in vitro activity than 6-mercaptopurine solution used as a positive control.4 The exact mechanism of action is not well understood.
  • Cardiovascular effects: Direct effects on the cardiovascular system have been demonstrated. Administration of hawthorn extract has been shown to decrease blood pressure and total peripheral resistance, economize myocardial function and decrease cardiac preload in healthy subjects.7,8 More specifically, hawthorn extract (WS 1442) has shown an inotropic effect on myocardial tissue isolated from patients with terminal left-ventricular heart failure (CHF).9 The inotropic effects of hawthorn may be caused by inhibition of 3',5'-cyclic adenosine monophosphate diesterase10, rather than beta-sympathomimetic activity11.
  • In the isolated perfused guinea pig heart, the inotropic effect of hawthorn extract LI 132 was weaker than digoxin and epinephrine. However, the refractory period was prolonged, perhaps as a result of blockage of repolarizing potassium currents. Thus, hawthorn may be potentially less arrhythmogenic than conventional inotropic agents.12 At a dose of 20mg/kg, crataemon (flavonoid fraction of hawthorn) stopped barium chloride-induced arrhythmia in animals; at doses greater than 30mg/kg, hypotensive effects were seen.5 A hawthorn extract (LI 132) prevented reperfusion arrhythmias and drastically reduced lactate dehydrogenase release in isolated rat hearts.13,1,14 However, in a more recent study, no antiarrhythmic effect on the reperfused rat heart was found.15 The authors suggested an intracellular increase in calcium as the mechanism for inotropy, as well as for the occasional aggravation of arrhythmia.
  • Earlier areas of animal study included the effects of hawthorn upon myocardial perfusion 16 17. In one experiment, crataemon increased rabbit coronary blood flow by 37%, at a dose of 10mg/kg, and decreased myocardial oxygen consumption.5
  • A preventive effect of hawthorn on coronary artery disease18,1,19 and cancer20 has been proposed, as due to hawthorn's antioxidant activities. Free radical properties have been demonstrated in vivo18,21, and may depend on the phenol22 or flavonoid content of the extract.
  • Other pharmacological properties of hawthorn that may influence heart function may include thromboxane A2 biosynthesis inhibition, observed in vitro.23
  • Endocrine effects: Hawthorn may induce reductions in lipids and in rats. Hawthorn tincture has been shown to enhance hepatic lactate dehydrogenase (LDH) receptor activity, to stimulate intrahepatic cholesterol degradation, and to suppress cholesterol biosynthesis.3,24 Hyperoside, isoquercitrin and epicatechin are the major active flavonoid components of the phenolic extract from hawthorn fruits, which demonstrate inhibitory effects in vitro on cupric ion (Cu+2)-mediated low density lipoproteins (LDL) oxidation.25 It has been proposed that the co-occurring components in hawthorn phenolic extract might not have significant effect on the intestinal absorption of the three major hawthorn flavonoids.26
  • Reproductive effects: In vitro study showed that serum containing the root of Crataegus cuneata significantly increased the sperm progressive motility in five and 15 minutes and the motility and progressive motility were both increased significantly in 60 and 120 minutes, compared to controls.2

Pharmacodynamics/Kinetics:

  • Overall, there is insufficient available data on hawthorn. The pharmacokinetics of another botanical (the common grape), whose constituents, like hawthorn, include procyanidins, have been reviewed elsewhere. In the common grape, large quantities of procyanidins have been found unmetabolized in renal and intestinal elimination pathways, suggesting limited metabolic degradation. The procyanidins of the hawthorn berry are reported to have a higher degree of polymerization, yet a lower concentration of flavonoids and procyanidins.

References
  1. Al Makdessi S, Sweidan H, DietzK, and et al. Protective effect of Crataegus oxyacantha against reperfusion arrhythmias after global no-flow ischemia in the rat heart. Basic Res Cardiol 1999;94(2):71-77. 10326654
  2. Hu, L. and Xiong, C. L. [The influence of medicated serum with root of Crataegus cuneata on human sperm motility parameters in vitro]. Zhongguo Zhong Yao Za Zhi 2006;31(4):333-335. 16706029
  3. Rajendran S, Deepalakshmi PD, Parasakthy K, and et al. Effect of tincture of Crataegus on the LDL-receptor activity of hepatic plasma membrane of rats fed an atherogenic diet. Atherosclerosis 1996;123(1-2):235-241. 8782854
  4. Saenz MT, Ahumada MC, and Garcia MD. Extracts from Viscum and Crataegus are cytotoxic against larynx cancer cells. Z Naturforsch 1997;52c:42-44.
  5. Petkov V. Plants with hypotensive, antiatheromatous and coronarodilatating action. Am J Chinese Med 1979;7(3):197-236.
  6. Min, B. S., Kim, Y. H., Lee, S. M., Jung, H. J., Lee, J. S., Na, M. K., Lee, C. O., Lee, J. P., and Bae, K. Cytotoxic triterpenes from Crataegus pinnatifida. Arch Pharm Res 2000;23(2):155-158. 10836742
  7. Mang C, Herrmann V, Butzer R, and et al. Crataegus fructi extract: a placebo-controlled study on haemodynamic effects of single and repetitive doses in normal volunteers. Eur J Clin Pharmacol 1997;52 suppl(abstract 116):A59.
  8. Popping S, Rose H, Ionescu I, and et al. Effect of a hawthorn extract on contraction and energy turnover of isolated rat cardiomyocytes. Arzneim Forsch 1995;45(11):1157-1161.
  9. Brixius K, Frank K, Muench G, and et al. WG 1442 (Crataegus spezialextrakt) works at the insufficient human myocardium contractible force-increasing. Verhandlungen der deutschen Gesellschaft fur Herz und Kreislaufforschung 1998;30:28-33.
  10. Schussler M, Holzl J, and Fricke U. Myocardial effects of flavonoids from Crataegus species. Arzneimittelforschung 1995;45(8):842-845. 7575743
  11. Muller, A., Linke, W., and Klaus, W. Crataegus extract blocks potassium currents in guinea pig ventricular cardiac myocytes. Planta Med 1999;65(4):335-339. 10364839
  12. Joseph G, Zhao Y, and Klaus W. [Pharmacologic action profile of crataegus extract in comparison to epinephrine, amrinone, milrinone and digoxin in the isolated perfused guinea pig heart]. Arzneimittelforschung 1995;45(12):1261-1265. 8595081
  13. Al Makdessi S, Sweidan H, Mullner S, and et al. Myocardial protection by pretreatment with Crataegus oxyacantha: an assessment by means of the release of lactate dehydrogenase by the ischemic and reperfused Langendorff heart. Arzneimittelforschung 1996;46(1):25-27. 8821513
  14. Nasa Y, Hashizume H, Hoque AN, and et al. Protective effect of crataegus extract on the cardiac mechanical dysfunction in isolated perfused working rat heart. Arzneimittelforschung 1993;43(9):945-949. 8240455
  15. Rothfuss, M. A., Pascht, U., and Kissling, G. Effect of long-term application of Crataegus oxyacantha on ischemia and reperfusion induced arrhythmias in rats. Arzneimittelforschung 2001;51(1):24-28. 11215322
  16. Mavers WH and Hensel H. [Changes in local myocardial blood circulation following oral administration of a Crataegus extract in non-narcotized dogs]. Arzneimittelforschung 1974;24(5):783-785. 4408035
  17. Roddewig C and Hensel H. [Reaction of local myocardial blood flow in non-anesthetized dogs and anesthetized cats to the oral and parenteral administration of a Crateagus fraction (oligomere procyanidines)]. Arzneimittelforschung 1977;27(7):1407-1410. 578464
  18. Chatterjee SS, Koch E, Jaggy H, and et al. [In vitro and in vivo studies on the cardioprotective action of oligomeric procyanidins in a Crataegus extract of leaves and blooms]. Arzneimittelforschung 1997;79:821-825. 9324931
  19. Hertog MG, Feskens EJ, Hollman PC, and et al. Dietary antioxidant flavonoids and risk of coronary heart disease: the Zutphen Elderly Study. Lancet 10-23-1993;342:1007-1011. 8105262
  20. Hertog MG, Kromhout D, Aravanis C, and et al. Flavonoid intake and long-term risk of coronary heart disease and cancer in the seven countries study. Arch Intern Med 2-27-1995;155(4):381-386. 7848021
  21. Bahorun T, Gressier B, Trotin F, and et al. Oxygen species scavenging activity of phenolic extracts from hawthorn fresh plant organs and pharmaceutical preparations. Arzneim-Forsch 1996;46(2):1086-1089.
  22. Rakotoarison DA, Gressier B, Trotin F, and et al. Antioxidant activities of polyphenolic extracts from flowers, in vitro callus and cell suspension cultures of Crataegus monogyna. Pharmazie 1997;52(1):60-64. 9035237
  23. Vibes J, Lasserre B, Gleye J, and et al. Inhibition of thromboxane A2 biosynthesis in vitro by the main components of Crataegus oxyacantha (hawthorn) flower heads. Prostaglandins Leukotrienes Essential Fatty Acids 1994;50(4):173-175.
  24. Fan, C., Yan, J., Qian, Y., Wo, X., and Gao, L. Regulation of lipoprotein lipase expression by effect of hawthorn flavonoids on peroxisome proliferator response element pathway. J Pharmacol Sci 2006;100(1):51-58. 16404131
  25. Zhang, Z., Chang, Q., Zhu, M., Huang, Y., Ho, W. K., and Chen, Z. Characterization of antioxidants present in hawthorn fruits. J Nutr Biochem 2001;12(3):144-152. 11257463
  26. Zuo, Z., Zhang, L., Zhou, L., Chang, Q., and Chow, M. Intestinal absorption of hawthorn flavonoids--in vitro, in situ and in vivo correlations. Life Sci 11-25-2006;79(26):2455-2462. 16989871




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