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W007B是一个新合成的新木脂素类衍生物。本研究利用不同的体内、体外模型观察它对血小板聚集和血栓形成的作用。用ADP、凝血酶、花生四烯酸和胶原为诱导剂,进行体外血小板聚集实验。分别用动静脉旁路血栓模型、电刺激颈总动脉血栓形成模型、急性肺栓塞模型和尾出血实验评价W007B对动脉血栓形成的作用。实验结果显示:W007B对ADP、凝血酶、胶原、花生四烯酸诱导的血小板聚集均有抑制作用,IC50分别是899.5μM,212.9μM,266.0μM,52.5μM;W007B(2–10 mg/kg,ig)单次给药可明显减轻大鼠动静脉旁路血栓重量;显著延长大鼠电刺激颈总动脉血栓形成时间。W007B(2.8–14 mg/kg,ig)单次给药明显降低ADP诱导的小鼠急性肺栓塞的死亡率;显著延长小鼠尾出血时间。这些结果表明:W007B对多种诱导剂诱导的血小板聚集均有抑制作用,其中对花生四烯酸诱导的血小板聚集抑制作用最强;W007B在多种动脉血栓形成模型上都有较强的抗血栓作用,可作为新的抗血栓候选药进一步研发。
W007B is a newly synthesized neolignan derivative. In this study, different in vivo and in vitro models were used to observe its effect on platelet aggregation and thrombosis. In vitro platelet aggregation experiments were performed with ADP, thrombin, arachidonic acid and collagen as inducers. The effects of W007B on arterial thrombosis were evaluated by arterial venous bypass thrombosis model, electrical stimulation of common carotid artery thrombosis model, acute pulmonary embolism model and tail bleeding test respectively. The results showed that W007B could inhibit platelet aggregation induced by ADP, thrombin, collagen and arachidonic acid with IC50 of 899.5μM, 212.9μM, 266.0μM and 52.5μM, respectively; W007B (2-10 mg / kg, ig) single administration can significantly reduce the rat arteriovenous bypass thrombosis weight; significantly extend the electrical stimulation of the common carotid artery thrombosis time. Single administration of W007B (2.8-14 mg / kg, ig) significantly reduced ADP-induced mortality in acute pulmonary embolism; significantly prolonged tail bleeding in mice. These results indicate that W007B inhibits platelet aggregation induced by various inducers and has the strongest inhibitory effect on arachidonic acid-induced platelet aggregation. W007B has a stronger antithrombotic effect on various arterial thrombosis models Role, can be used as a new anti-thrombotic drug further research and development.