Tong L, Yue T L
Yao Xue Xue Bao. 1989;24(2):85-8.
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.
蝙蝠葛碱(Dau)是从蝙蝠葛的根中提取的一种异喹啉生物碱,最近在中国用作抗心律失常药物。体外实验表明,它能剂量依赖性地抑制花生四烯酸(AA)和二磷酸腺苷(ADP)诱导的大鼠血小板聚集,以及AA、ADP和肾上腺素(Adr)诱导的人血小板聚集。抑制AA和ADP诱导的大鼠血小板聚集50%所需的蝙蝠葛碱浓度(IC50)分别为26和37μmol/L。对于AA、ADP和Adr诱导的人血小板聚集,蝙蝠葛碱的IC50分别为39、55和43μmol/L。蝙蝠葛碱抑制洗涤后的完整大鼠血小板中AA的环氧化酶途径代谢产物(TXB2和HHT)。当蝙蝠葛碱浓度为50μmol/L时,TXB2和HHT的生成分别减少26%和19%;当蝙蝠葛碱浓度为100μmol/L时,分别减少46%和45%。在100μmol/L的蝙蝠葛碱作用下,12-羟基二十碳四烯酸(12-HETE)的形成也受到抑制。蝙蝠葛碱对AA代谢的抑制作用可能是其抑制血小板聚集的相关机制之一。