Wang J P, Hsu M F, Tsai H Y, Huang L J, Teng C M
Thromb Res. 1984 Oct 15;36(2):113-22. doi: 10.1016/0049-3848(84)90333-5.
XC386 was a new antiplatelet compound, which inhibited the aggregation and release reaction of rat platelet-rich plasma induced by collagen. This inhibition was dose-dependent and the IC50 was calculated to be 1 mM on collagen-induced aggregation. In washed platelets, the aggregations induced by ADP and collagen were much more markedly inhibited by XC386 than those induced by thrombin, A23187 and arachidonate. High calcium (4 to 8 mM) could not antagonize the inhibition. XC386 did not alter the malondialdehyde (MDA) and thromboxane B2 (TXB2) levels of resting platelets. But MDA formation induced by collagen, thrombin and A23187, and TXB2 formation induced by collagen and thrombin were significantly inhibited, while both formations induced by arachidonate were not changed. Combination of indomethacin or CP/CPK and XC386 enhanced markedly the inhibitory effect of XC386 on collagen- or A23187-induced aggregation. It was concluded that XC386 might inhibit platelet aggregation before the step of arachidonic acid release by phospholipase A2.
XC386是一种新型抗血小板化合物，它能抑制胶原蛋白诱导的大鼠富血小板血浆的聚集和释放反应。这种抑制作用呈剂量依赖性，在胶原蛋白诱导的聚集中，计算得出的IC50为1毫摩尔。在洗涤后的血小板中，XC386对ADP和胶原蛋白诱导的聚集的抑制作用比对凝血酶、A23187和花生四烯酸诱导的聚集的抑制作用更为明显。高钙（4至8毫摩尔）不能拮抗这种抑制作用。XC386不会改变静息血小板的丙二醛（MDA）和血栓素B2（TXB2）水平。但是，胶原蛋白、凝血酶和A23187诱导的MDA形成以及胶原蛋白和凝血酶诱导的TXB2形成均受到显著抑制，而花生四烯酸诱导的这两种形成均未改变。吲哚美辛或CP/CPK与XC386联合使用可显著增强XC386对胶原蛋白或A23187诱导的聚集的抑制作用。得出的结论是，XC386可能在磷脂酶A2释放花生四烯酸的步骤之前抑制血小板聚集。
