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Homoerydictyl-7-O-β-D-glycoside-A Receptor Antagonist of Platelet-activating Factor (PAF)

Guan Zengwei, Wang Yinye, Yang Xiuwei, Cui Yuxin   

  1. 1. Medical and Pharmaceutical Analysis Center, Peking University, Beijing 100083;
    2. Department of Molecular and Cellular Pharmacology, Peking University School of Pharmaceutical Sciences, Beijing 100083;
    3. National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, 100083
  • Received:2000-09-01 Revised:2000-12-09 Online:2001-03-15 Published:2001-03-15

Abstract: Homoeriodictyl-7-O-β-D-glycoside, a flavonoid compound isolated from the Chinese medicinal herb, viscum coloratum inhibited platelet aggregation induced by platelet-activating factor(PAF), but it had no inhibitory activity on adenosine diphosphate-induced platelet aggregation. In the present study, we intended to get an insight into the mechanism of its anti-PAF action. Using [3H]PAF receptor binding assay we found that the compound exhibited inhibitory activity. The inhibitory rate was 18.5%, 28.4%, 58.7%, 78% and 78%, respectively, at concentrations of 10-8, 10-7, 10-6, 10-5 and 10-4 mol·L-1, There was a visible dose-effect relationship as well as a correlation between different concentrations and their inhibitory rates (γ = 0.985, P<0.05) when the dose was equal to or less than 1×10-5 mol·L-1, and its IC50 was 8.0×10-7 mol·L-1. The inhibitory rate didn't increase with increasing concentration of the compound when it went beyond 1×10-5 mol·L-1 indicating competitive inhibition of binding of [3H]PAF to PAF receptor reached saturation.

Key words: Homoeriodictyol-7-O-β-D-glycoside, Platelet-activating factor antagonist, Platelet-activating factor receptor, Platelet aggregation

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