Hydroxychavicol, a novel betel leaf component, inhibits platelet aggregation by suppression of cyclooxygenase, thromboxane production and calcium mobilization

M. C. Chang, B. J. Uang, C. Y. Tsai, H. L. Wu, B. R. Lin, C. S. Lee, Y. J. Chen, C. H. Chang, Y. L. Tsai, C. J. Kao, J. H. Jeng*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

46 Citations (Scopus)


Background and purpose: Platelet hyperactivity is important in the pathogenesis of cardiovascular diseases. Betel leaf (PBL) is consumed by 200-600 million betel quid chewers in the world. Hydroxychavicol (HC), a betel leaf component, was tested for its antiplatelet effect. Experimental approach: We tested the effect of HC on platelet aggregation, thromboxane B 2 (TXB 2) and reactive oxygen species (ROS) production, cyclooxygenase (COX) activity, ex vivo platelet aggregation and mouse bleeding time and platelet plug formation in vivo. The pharmacokinetics of HC in rats was also assessed. Key results: HC inhibited arachidonic acid (AA) and collagen-induced platelet aggregation and TXB 2 production. HC inhibited the thrombin-induced TXB 2 production, but not platelet aggregation. SQ29548, suppressed collagen- and thrombin-induced TXB 2 production, but not thrombin-induced platelet aggregation. HC also suppressed COX-1/COX-2 enzyme activity and the AA-induced ROS production and Ca 2+ mobilization. HC further inhibited the ex vivo platelet aggregation of platelet-rich plasma (>100 nmole/mouse) and prolonged platelet plug formation (>300 nmole/mouse) in mesenteric microvessels, but showed little effect on bleeding time in mouse tail. Moreover, pharmacokinetics analysis found that more than 99% of HC was metabolized within 3 min of administration in Sprague-Dawley rats in vivo. Conclusions and implications: HC is a potent COX-1/COX-2 inhibitor, ROS scavenger and inhibits platelet calcium signaling, TXB 2 production and aggregation. HC could be a potential therapeutic agent for prevention and treatment of atherosclerosis and other cardiovascular diseases through its anti-inflammatory and antiplatelet effects, without effects on haemostatic functions.

Original languageEnglish
Pages (from-to)73-82
Number of pages10
JournalBritish Journal of Pharmacology
Issue number1
Publication statusPublished - 2007 Sept
Externally publishedYes


  • Betel leaf
  • Calcium
  • Cyclooxygenase
  • Hydroxychavicol
  • Platelet aggregation
  • Thromboxane

ASJC Scopus subject areas

  • Pharmacology


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