Yu S M, Chen C C, Ko F N, Huang Y L, Huang T F, Teng C M
Pharmacological Institute, College of Medicine, National Taiwan University, Taipei.
Biochem Pharmacol. 1992 Jan 22;43(2):323-9.
Dicentrine is an antiplatelet agent isolated from the Chinese herb Lindera megaphylla. We examined the in vitro effects of dicentrine on various aspects of platelet reactivity. Dicentrine inhibited the aggregation and ATP release of washed rabbit platelets induced by arachidonic acid (AA), collagen, ADP, platelet-activating factor (PAF), thrombin and U46619. Dicentrine also inhibited the thromboxane B2 formation caused by AA, collagen and thrombin in washed intact platelets or that induced by AA in lysed platelet homogenate, while prostaglandin D2 formation caused by AA was not increased. The generation of inositol monophosphates (in the presence of indomethacin) caused by thrombin, collagen and PAF was not suppressed significantly, nor did dicentrine suppress fibrinogen-induced aggregation of elastase-treated platelets. Dicentrine inhibited the intracellular Ca2+ increase in quin-2/AM-loaded platelets caused by thrombin, PAF, collagen and AA. The cyclic AMP level was elevated by dicentrine in a concentration-dependent manner. These data indicate that the inhibitory effect of dicentrine on platelet aggregation and ATP release was due to the inhibition of thromboxane formation and the elevation of the level of cyclic AMP.
双苄基异喹啉是从中药乌药中分离得到的一种抗血小板药物。我们研究了双苄基异喹啉在体外对血小板反应性各个方面的影响。双苄基异喹啉抑制了花生四烯酸（AA）、胶原、ADP、血小板活化因子（PAF）、凝血酶和U46619诱导的洗涤兔血小板的聚集和ATP释放。双苄基异喹啉还抑制了洗涤完整血小板中由AA、胶原和凝血酶引起的血栓素B2形成，或裂解血小板匀浆中由AA诱导的血栓素B2形成，而由AA引起的前列腺素D2形成并未增加。凝血酶、胶原和PAF引起的肌醇单磷酸生成（在吲哚美辛存在下）未被显著抑制，双苄基异喹啉也未抑制纤维蛋白原诱导的弹性蛋白酶处理血小板的聚集。双苄基异喹啉抑制了凝血酶、PAF、胶原和AA引起的喹吖因/AM负载血小板内Ca2+的增加。双苄基异喹啉以浓度依赖的方式提高了环磷酸腺苷水平。这些数据表明，双苄基异喹啉对血小板聚集和ATP释放的抑制作用是由于对血栓素形成的抑制和环磷酸腺苷水平的升高。
