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我们发现黄连素(BR)是一种有效的抗血小板药物。实验证明它对ADP、花生四烯酸(AA)、胶原及钙离子载体A23187诱发的血小板聚集和ATP释放均有不同程度的抑制作用。其中以对胶原诱发的聚集及释放的抑制作用最为强烈(IC_(50)分别为0.12及0.08mmol/L)。BR的作用机理,可能与抑制AA代谢和胞内Ca~(2+)升高和(或)升高cAMP有关。由于心、脑血管中血小板血栓的形成与血管内皮下胶原纤维的暴露有密切关系,因此在这些疾病的防治上可能有重要价值。
We found that berberine (BR) is a potent antiplatelet agent. Experiments show that it has different degrees of inhibition on ADP, arachidonic acid (AA), collagen and calcium ionophore A23187-induced platelet aggregation and ATP release. Among them, the most intense inhibitory effect on the collagen-induced aggregation and release was IC 50 (0.12 and 0.08 mmol / L, respectively). The mechanism of BR may be related to inhibition of AA metabolism and intracellular Ca 2+ increase and / or increase cAMP. Since heart and cerebrovascular platelet thrombosis is closely related to the exposure of subendothelial collagen fibers, it may be of great value in the prevention and treatment of these diseases.