Sheu J R, Huang T F
Pharmacological Institute, College of Medicine, National Taiwan University, Taipei.
J Pharm Pharmacol. 1994 Jan;46(1):58-62. doi: 10.1111/j.2042-7158.1994.tb03721.x.
Triflavin, an Arg-Gly-Asp-containing snake venom peptide, inhibits platelet aggregation through the blockade of fibrinogen binding to the activated platelets. It binds to fibrinogen receptors associated with the glycoprotein IIb/IIIa complex with a Kd value of 7 x 10(-8) M. In this study, we found that 125I-triflavin reached the maximal binding to human platelets within 5 min at 25 degrees C. In addition, when triflavin was intravenously administered at 1.0 mg kg-1 to rabbits, it reversibly impaired the platelet aggregation of platelet-rich plasma caused by ADP (20 microM) ex-vivo over 30 min. The platelet counts of the experimental rabbits remained unchanged. Triflavin was effective in reducing the mortality of ADP-induced acute pulmonary thromboembolism in mice when administered intravenously at a dose of 2 micrograms g-1. Therefore, triflavin was proven to be an effective antithrombotic agent in preventing ADP-induced acute pulmonary thromboembolism in mice and impairing reversibly the platelet function of rabbits when given intravenously.
三黄素是一种含精氨酸 - 甘氨酸 - 天冬氨酸的蛇毒肽，它通过阻断纤维蛋白原与活化血小板的结合来抑制血小板聚集。它以7×10（-8）M的解离常数（Kd值）与糖蛋白IIb/IIIa复合物相关的纤维蛋白原受体结合。在本研究中，我们发现125I - 三黄素在25℃下5分钟内与人血小板达到最大结合。此外，当以1.0mg kg-1的剂量静脉注射给兔子时，三黄素在30分钟内可逆地损害了体外由ADP（20μM）引起的富含血小板血浆的血小板聚集。实验兔子的血小板计数保持不变。当以2μg g-1的剂量静脉注射时，三黄素可有效降低小鼠ADP诱导的急性肺血栓栓塞的死亡率。因此，已证明三黄素是一种有效的抗血栓形成剂，可预防小鼠ADP诱导的急性肺血栓栓塞，并在静脉注射时可逆地损害兔子的血小板功能。
