Mechanisms involved in the antiplatelet activity of tetramethylpyrazine in human platelets

Joen Rong Sheu, Ya Chen Kan, Wei Chun Hung, Wun Chang Ko, Mao Hsiung Yen

研究成果: 雜誌貢獻文章同行評審

45 引文 斯高帕斯(Scopus)

摘要

Tetramethylpyrazine is the active ingredient of a Chinese herbal medicine. In this study, tetramethylpyrazine was tested for its antiplatelet activities in human platelet suspensions. In human platelets, tetramethylpyrazine (0.5-1.5 mM) dose-dependently inhibited both platelet aggregation and ATP-release reaction induced by a variety of agonists (i.e., ADP, collagen, and U46619). Tetramethylpyrazine (0.5 mM) did not significantly change the fluorescence of platelet membranes labeled with diphenylhexatriene, even at the high concentration (1.5 mM). Furthermore, tetramethylpyrazine (0.5-1.5 mM) dose-dependently inhibited [3H]inositol monophosprate formation stimulated by collagen (5 μg/ml) in [3H]myoinositol loaded platelets. Tetramethylpyrazine (0.5-1.5 mM) also dose-dependently inhibited the intracellular free Ca+2 rise of Fura 2-AM loaded platelets stimulated by collagen (5 μg/ml). Moreover, tetramethylpyrazine (0.5-1.5 mM) inhibited thromboxane B2 formation stimulated by collagen. At a higher concentration (1.0 mM), tetramethylpyrazine has also been shown to influence the binding of FITC-triflavin to platelet glycoprotein IIb/IIIa complex. Triflavin, a specific glycoprotein IIb/IIIa complex antagonist purified from Trimeresurus flavoviridis venom. It is concluded that the antiplatelet activity of tetramethylpyrazine may possibly involve two pathways: 1) at a lower concentration (0.5 mM), tetramethylpyrazine is shown to inhibit phosphoinositide breakdown and thromboxane A2 formation; and 2) at a higher concentration (1.0 mM), it leads to the inhibition of platelet aggregation through binding to the glycoprotein IIb/IIIa complex.

原文英語
頁(從 - 到)259-270
頁數12
期刊Thrombosis Research
88
發行號3
DOIs
出版狀態已發佈 - 十一月 1 1997

ASJC Scopus subject areas

  • 心臟病學與心血管醫學
  • 血液學

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