Tzeng S H, Ko W C, Ko F N, Teng C M
Department of Pharmacology, Taipei Medical College, Taiwan.
Thromb Res. 1991 Oct 1;64(1):91-100. doi: 10.1016/0049-3848(91)90208-e.
The inhibitory effects of five flavonoids on the aggregation and secretion of platelets were studied. These flavonoids inhibited markedly platelet aggregation and ATP release of rabbit platelets induced by arachidonic acid or collagen, and slightly those by platelet-activating factor. ADP-induced platelet aggregation was also suppressed by myricetin, fisetin and quercetin. The IC50 on arachidonic acid-induced platelet aggregation was: fisetin, 22 microM; kaempferol, 20 microM; quercetin, 13 microM; morin, 150 microM less than IC50 less than 300 microM. The thromboxane B2 formations were also inhibited by flavonoids in platelets challenged with arachidonic acid. Fisetin, kaempferol, morin and quercetin antagonized the aggregation of washed platelets induced by U46619, a thromboxane A2/prostaglandin endoperoxides mimetic receptor agonist. In human platelet-rich plasma, quercetin prevented the secondary aggregation and blocked ATP release from platelets induced by epinephrine or ADP. These results demonstrate that the major antiplatelet effect of flavonoids tested may be due to both the inhibition of thromboxane formation and thromboxane receptor antagonism.
研究了五种黄酮类化合物对血小板聚集和分泌的抑制作用。这些黄酮类化合物显著抑制花生四烯酸或胶原诱导的兔血小板聚集和ATP释放,对血小板活化因子诱导的作用则较弱。杨梅素、非瑟酮和槲皮素也能抑制ADP诱导的血小板聚集。花生四烯酸诱导的血小板聚集的半数抑制浓度(IC50)为:非瑟酮22μM;山奈酚20μM;槲皮素13μM;桑色素,150μM<IC50<300μM。黄酮类化合物也能抑制花生四烯酸刺激的血小板中血栓素B2的形成。非瑟酮、山奈酚、桑色素和槲皮素能拮抗血栓素A2/前列腺素内过氧化物模拟受体激动剂U46619诱导的洗涤血小板聚集。在富含人血小板的血浆中,槲皮素可防止肾上腺素或ADP诱导的血小板二次聚集并阻止ATP释放。这些结果表明,所测试的黄酮类化合物的主要抗血小板作用可能是由于抑制血栓素形成和拮抗血栓素受体。