Antithrombotic effects of bromophenol, an alga-derived thrombin inhibitor |
| |
| Authors: | Dayong Shi Xiaohong Li Jing Li Shuju Guo Hua Su Xiao Fan |
| |
| Institution: | (1) Department of Chemistry, Dartmouth College, 6128 Burke Laboratory, Hanover, NH 03755, USA |
| |
| Abstract: | Thrombin, the ultimate proteinase of the coagulation cascade, is an attractive target for the treatment of a variety of cardiovascular diseases. A bromophenol derivative named (+)-3-(2,3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1, isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity. In this study, we investigated the inhibition of human thrombin in vitro with this bromophenol derivative, and its antithrombotic efficacy in vivo using the arteriovenous shunt model and the ferric chloride-induced arterial thrombosis model in rats. The results show that the bromophenol derivative is a potential inhibitor of thrombin (IC50=1.03 nmol/L). In antithrombotic experiments in vivo, the bromophenol derivative also shows good effect comparing with the control group. These data indicate that the bromophenol derivative is a potential drug for prophylaxis and the treatment of thrombotic diseases. |
| |
| Keywords: | |
| 本文献已被 SpringerLink 等数据库收录！ |
|
