Antithrombotic effects of bromophenol,an alga-derived thrombin inhibitor

IOCAS-IR

	Antithrombotic effects of bromophenol,an alga-derived thrombin inhibitor
	Shi DY(史大永); Li XH(李晓红); Li J(李敬); Guo SJ(郭书举); Su H(苏华); Fan X(范晓)
发表期刊	Chinese Journal of Oceanology and Limnology
ISSN	0254-4059
	2010-02-15
出版年	2010
卷号	v.28 期号:01 页码:98-100
文献类型	CNKI期刊论文
摘要	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.
关键词	thrombin inhibitor antithrombotic effect bromophenol derivative
CNKI专辑号	A;E;
CNKI专辑名称	基础科学;医药卫生科技;
CNKI专题号	E079;
CNKI专题名称	药学;
分类号	R972
收录类别	中科院核心
语种	英文;
资助项目(基金）	Supported by the National High Technology Research and Development Program of China (863 Program) (No. 2007AA09Z410) ; the National Major Research Program of China “The Creation for Significant Innovative Drugs” (No. 2009ZX09103-148)
文献类型	CNKI期刊论文
条目标识符	http://ir.qdio.ac.cn/handle/337002/192265
专题	中国科学院海洋研究所
作者单位	1.InstituteofOceanology,ChineseAcademyofSciences 2.QingdaoMunicipalHospital
推荐引用方式 GB/T 7714	Shi DY,Li XH,Li J,et al. Antithrombotic effects of bromophenol,an alga-derived thrombin inhibitor. 2010.