Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital/West China Medical School, Sichuan University, Chengdu 610041, China; Institute for Nanobiomedical Technology and Membrane Biology, Sichuan University, Chengdu 610041, China.
Steroids. 2013 Nov;78(11):1064-70. doi: 10.1016/j.steroids.2013.07.003. Epub 2013 Jul 24.
Thrombosis in coronary or cerebral arteries is the major cause of morbidity and mortality worldwide. Diosgenin and total steroidal saponins extracted from the rhizome of Dioscorea zingiberensis C.H. Wright are demonstrated to have anti-thrombotic activity. However, few studies describe the anti-thrombotic activity of the diosgenyl saponin monomer. In the present study, a simple and convenient method for the preparation of a new disaccharide saponin, diosgenyl β-D-galactopyranosyl-(1→4)-β-D-glucopyranoside (3), is described. We evaluated the anti-thrombotic effects of diosgenin and four diosgenyl saponins by measuring the bleeding time; the results showed that compound 3 exhibits outstanding efficiency in prolonging the bleeding time. Furthermore, we assessed whether compound 3 could alter platelet aggregation in vitro and in vivo. In addition, activated partial thromboplastin time (APTT), thrombin time (TT), prothrombin time (PT), coagulation factors and protection rate in mice were measured to evaluate the anti-thrombotic effect of compound 3. The results show that compound 3 inhibited platelet aggregation, prolonged APTT, inhibited factor VIII activities in rats, and increased the protection rate in mice in a dose-dependent manner. Taken together, these findings suggested that diosgenyl saponins, especially compound 3, had anti-thrombotic activity. It may execute anti-thrombotic activity through inhibiting factor VIII activities and platelet aggregation.
冠状动脉或脑动脉血栓形成是全球发病率和死亡率的主要原因。从盾叶薯蓣根茎中提取的薯蓣皂苷元和总甾体皂苷已被证明具有抗血栓活性。然而，很少有研究描述薯蓣皂苷元单体的抗血栓活性。本研究描述了一种简单方便的制备新的二糖皂苷，薯蓣皂苷基-β-D-吡喃半乳糖基-(1→4)-β-D-吡喃葡萄糖苷（3）的方法。我们通过测量出血时间来评估薯蓣皂苷元和四种薯蓣皂苷的抗血栓作用；结果表明，化合物 3 能显著延长出血时间。此外，我们评估了化合物 3 是否能改变体外和体内的血小板聚集。此外，还测量了活化部分凝血活酶时间（APTT）、凝血酶时间（TT）、凝血酶原时间（PT）、凝血因子和小鼠的保护率，以评估化合物 3 的抗血栓作用。结果表明，化合物 3 能抑制血小板聚集，延长 APTT，抑制大鼠因子 VIII 活性，并能提高小鼠的保护率，呈剂量依赖性。综上所述，这些发现表明薯蓣皂苷，特别是化合物 3，具有抗血栓活性。它可能通过抑制因子 VIII 活性和血小板聚集来发挥抗血栓作用。
