[Effect of dauricine on rat and human platelet aggregation and metabolism of arachidonic acid in washed rat platelets].
Dauricine (Dau), an isoquinoline alkaloid extracted from the roots of Menispermum dauricum D. C. and used as an antiarrhythmic agent in China recently, was shown to inhibit rat platelet aggregation induced by arachidonic acid (AA) and ADP, as well as human platelet aggregation induced by AA, ADP and adrenaline (Adr) in vitro in a dose-dependent manner. The concentration of Dau required for 50% inhibition (IC50) of rat platelet aggregation induced by AA and ADP was 26 and 37 mumol/L, respectively. For human platelet aggregation induced by AA, ADP and Adr the IC50 of Dau was found to be 39, 55 and 43 mumol/L, respectively. Dau inhibited the cyclooxygenase pathway metabolites of AA (TXB2 and HHT) in washed intact rat platelets. The production of TXB2 and HHT was reduced by 26% and 19%, respectively, when the Dau concentration was 50 mumol/L and by 46 and 45%, respectively, when the concentration of Dau was 100 mumol/L. The formation of 12-HETE was also inhibited at 100 mumol/L of Dau. The inhibitory effect of Dau on AA metabolism may be one of the mechanisms related to its inhibition of platelet aggregation.
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D019377:12-Hydroxy-5,8,10,14-eicosatetraenoic Acid; D000470:Alkaloids; D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism; D044182:Benzylisoquinolines; D005231:Fatty Acids, Unsaturated / Q000378:metabolism; D006893:Hydroxyeicosatetraenoic Acids / Q000378:metabolism; D007546:Isoquinolines / Q000494:pharmacology*; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors; D051381:Rats; D011919:Rats, Inbred Strains; D044005:Tetrahydroisoquinolines; D013929:Thromboxane B2 / Q000378:metabolism
D000470:Alkaloids; D001095:Arachidonic Acids; D044182:Benzylisoquinolines; D005231:Fatty Acids, Unsaturated; D006893:Hydroxyeicosatetraenoic Acids; D007546:Isoquinolines; D010975:Platelet Aggregation Inhibitors; D044005:Tetrahydroisoquinolines; C008033:12-hydroxy-5,8,10-heptadecatrienoic acid; D013929:Thromboxane B2; D019377:12-Hydroxy-5,8,10,14-eicosatetraenoic Acid; C035934:dauricine