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新型类肝素化合物及其他抗血栓药物的研发及其与血管内皮细胞的相互作用。

Development of new heparin-like compounds and other antithrombotic drugs and their interaction with vascular endothelial cells.

作者信息

Nader H B, Pinhal M A, Baú E C, Castro R A, Medeiros G F, Chavante S F, Leite E L, Trindade E S, Shinjo S K, Rocha H A, Tersariol I L, Mendes A, Dietrich C P

机构信息

Departamento de Bioquímica, Escola Paulista de Medicina, Universidade Federal de São Paulo, Rua 3 de Maio 100, 04044-020 São Paulo, SP, Brazil.

出版信息

Braz J Med Biol Res. 2001 Jun;34(6):699-709. doi: 10.1590/s0100-879x2001000600002.

DOI:10.1590/s0100-879x2001000600002
PMID:11378657
Abstract

The anticlotting and antithrombotic activities of heparin, heparan sulfate, low molecular weight heparins, heparin and heparin-like compounds from various sources used in clinical practice or under development are briefly reviewed. Heparin isolated from shrimp mimics the pharmacological activities of low molecular weight heparins. A heparan sulfate from Artemia franciscana and a dermatan sulfate from tuna fish show a potent heparin cofactor II activity. A heparan sulfate derived from bovine pancreas has a potent antithrombotic activity in an arterial and venous thrombosis model with a negligible activity upon the serine proteases of the coagulation cascade. It is suggested that the antithrombotic activity of heparin and other antithrombotic agents is due at least in part to their action on endothelial cells stimulating the synthesis of an antithrombotic heparan sulfate.

摘要

本文简要综述了肝素、硫酸乙酰肝素、低分子量肝素、临床应用或正在研发的各种来源的肝素及类肝素化合物的抗凝血和抗血栓活性。从虾中分离出的肝素模拟了低分子量肝素的药理活性。来自卤虫的硫酸乙酰肝素和来自金枪鱼的硫酸皮肤素具有较强的肝素辅因子II活性。源自牛胰腺的硫酸乙酰肝素在动静脉血栓形成模型中具有较强的抗血栓活性,而对凝血级联反应中的丝氨酸蛋白酶活性可忽略不计。有人认为,肝素和其他抗血栓药物的抗血栓活性至少部分归因于它们对内皮细胞的作用,刺激了抗血栓硫酸乙酰肝素的合成。

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Braz J Med Biol Res. 2001 Jun;34(6):699-709. doi: 10.1590/s0100-879x2001000600002.
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