Antithrombotic effects of bromophenol, an alga-derived thrombin inhibitor

• Published in: Chinese journal of oceanology and limnology Vol. 28; no. 1; pp. 96 - 98
• Main Author: 史大永 李晓红 李敬 郭书举 苏华 范晓
• Format: Journal Article
• Language: English
• Published: Heidelberg SP Science Press 2010; Springer Nature B.V
• Subjects: Algae; Benzofuran; Cardiovascular disease; Cardiovascular diseases; Coagulation; Disease prophylaxis; Earth and Environmental Science; Earth Sciences; Enzymes; Ferric chloride; Inhibitors; Leathesia nana; Oceanography; Pharmacology; Prophylaxis; Proteinase; Proteinase inhibitors; Thrombin; Thromboembolism; Thrombosis; 凝血酶抑制剂; 心血管疾病; 抗血栓; 苯并呋喃; 血栓性疾病; 衍生物; thrombin inhibitor; bromophenol derivative; antithrombotic effect
• ISSN: 0254-4059; 2096-5508; 1993-5005; 2523-3521
• DOI: 10.1007/s00343-010-9213-0

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.