摘 要：目的 设计合成薯蓣皂苷元衍生物，并评价其体内抗血栓形成活性。方法 以薯蓣皂苷元为先导物，经过酯化等反应得到薯蓣皂苷元酯类衍生物，选择动静脉旁路血栓形成模型，评价体内抗血栓形成活性。结果 合成了6个目标化合物，结构经过1H-NMR、13C-NMR、MS确证。抗血栓形成活性筛选结果显示，目标化合物3β-薯蓣皂苷元丁二酸单酯具有较好的抗血栓形成活性。结论 C-3位适当亲水性基团的引入，有助于增强薯蓣皂苷元的抗血栓形成活性。

Abstract: Objective To design and synthesize diosgenin derivative, and to evaluate their antithrombotic activity in vivo. Methods Taking diosgenin as lead compound, diosgenin derivatives were obtained by esterification reactions, and the antithrombotic effect of synthesized compounds was evaluated with the thrombogenesis model of artery-vein bypass in rats. Results Six target compounds were prepared and their structures were confirmed by 1H-NMR, 13C-NMR, and MS. Among these compounds, 3β- diosgeninyl monosuccinate showed promising antithrombotic activity in screening experiment. Conclusion A proper hydrophilic substitution on C-3 of diosgenin should be possible to improve the antithrombotic activity of diosgenin.

天津市自然科学基金资助项目（07TCZDJC05300）