title: Anti-thrombosis effect of diosgenyl saponins in vitro and in vivo.
abstract: 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.
authors.affiliation: 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.
authors.forename: Rui
authors.initials: R
authors.lastname: Zhang
authors.forename: Baozhan
authors.initials: B
authors.lastname: Huang
authors.forename: Dan
authors.initials: D
authors.lastname: Du
authors.forename: Xiurong
authors.initials: X
authors.lastname: Guo
authors.forename: Guang
authors.initials: G
authors.lastname: Xin
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Xing
authors.forename: Yong
authors.initials: Y
authors.lastname: Liang
authors.forename: Younan
authors.initials: Y
authors.lastname: Chen
authors.forename: Qianming
authors.initials: Q
authors.lastname: Chen
authors.forename: Yang
authors.initials: Y
authors.lastname: He
authors.forename: Wen
authors.initials: W
authors.lastname: Huang
mesh_terms: D000818:Animals; D001760:Bleeding Time; D001779:Blood Coagulation Factors / Q000378:metabolism; D001780:Blood Coagulation Tests; D027742:Dioscorea / Q000737:chemistry*; D005343:Fibrinolytic Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D008297:Male; D051379:Mice; D010974:Platelet Aggregation / Q000187:drug effects; D051381:Rats; D027343:Rhizome / Q000737:chemistry; D012503:Saponins / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D013927:Thrombosis / Q000097:blood / Q000188:drug therapy* / Q000503:physiopathology
chemical_list: D001779:Blood Coagulation Factors; D005343:Fibrinolytic Agents; D012503:Saponins
keywords: ADP; Anti-thrombosis; Anticoagulation; Bleeding time; Diosgenyl saponin; PPP; PRP; Platelet aggregation; adenosine 5′-diphosphate; platelet-poor plasma; platelet-rich plasma