Sheu J R, Yen M H, Peng H C, Chang M C, Huang T F
Graduate Institute of Medical Science, Taipei Medical College, Taiwan.
Eur J Pharmacol. 1995 Dec 27;294(1):231-8. doi: 10.1016/0014-2999(95)00530-7.
Triflavin, an Arg-Gly-Asp-containing peptide from Trimeresurus flavoviridis snake venom (M(r) of 7500 Da) inhibits platelet aggregation through the blockade of fibrinogen binding to activated platelets. The present study demonstrated that the intravenous injection of triflavin (0.1 and 0.25 mg/kg) significantly prolonged the bleeding time about 1.8- to 2.4-fold as compared with control (normal saline) of severed mesenteric arteries in rats, whereas the injection of Gly-Arg-Gly-Asp-Ser (GRGDS) (2-8 mg/kg) failed to increase the bleeding time in this model. Continuous infusion of triflavin (0.08 mg/kg/min) significantly increased the bleeding time about 2.6-fold, and the bleeding time returned to normal within 20 min after the cessation of triflavin infusion. Triflavin (10-20 mg/kg) significantly prolonged the occlusion time of platelet plug formation induced by irradiation of mesenteric venules of fluorescein sodium-pretreated mice. In contrast, trigramin (10-20 mg/kg) and GRGDS (500 and 1000 mg/kg) showed no significant effect. These results suggest that triflavin has an effective antiplatelet effect in vivo and this peptide may be a useful therapeutic agent for arterial thrombosis.
竹叶青毒素是一种来自竹叶青蛇毒液的含精氨酸 - 甘氨酸 - 天冬氨酸的肽(分子量7500道尔顿),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。本研究表明,静脉注射竹叶青毒素(0.1和0.25毫克/千克)可使大鼠切断的肠系膜动脉的出血时间比对照组(生理盐水)显著延长约1.8至2.4倍,而注射甘氨酸 - 精氨酸 - 甘氨酸 - 天冬氨酸 - 丝氨酸(GRGDS)(2 - 8毫克/千克)在该模型中未能增加出血时间。持续输注竹叶青毒素(0.08毫克/千克/分钟)可使出血时间显著增加约2.6倍,并且在停止输注竹叶青毒素后20分钟内出血时间恢复正常。竹叶青毒素(10 - 20毫克/千克)可显著延长荧光素钠预处理小鼠肠系膜小静脉照射诱导的血小板栓形成的闭塞时间。相比之下,三棱毒素(10 - 20毫克/千克)和GRGDS(500和1000毫克/千克)没有显著效果。这些结果表明,竹叶青毒素在体内具有有效的抗血小板作用,并且这种肽可能是一种用于治疗动脉血栓形成的有用治疗剂。