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降血脂药物维塞尔(Vessel)的糖胺聚糖成分及生物活性研究。

Studies of glycosaminoglycan composition and biologic activity of Vessel, a hypolipidemic agent.

作者信息

Radhakrishnamurthy B, Ruiz H A, Srinivasan S R, Preau W, Dalferes E R, Berenson G S

出版信息

Atherosclerosis. 1978 Oct;31(2):217-29. doi: 10.1016/0021-9150(78)90167-3.

Abstract

Heparin-like glycosaminoglycans (GAG) were isolated from commerical Vessel and their biologic properties studied. Vessel was found to be a mixture of chondroitin sulfates, dermatan sulfate and heparin-like GAG. Chondroitin sulfates and dermatan sulfate in Vessel were hydrolyzed by chondroitinase ABC and the residual Vessel was fractionated on a Dowex-1 Cl- column eluting with a stepwise-increasing concentration of NaCl (1.2--4.0 M). The major fractions eluted at 1.6 M and 1.8 M NaCl were tentatively identified by chemical analysis as heparin-like GAG with somewhat lower sulfate content than standard heparin. Both fractions had lipoprotein lipase-releasing activity and anticoagulant activity similar to heparin, but 1.6 M NaCl fraction had a third of the anticoagulant activity of standard heparin. The 1.8 M NaCl fraction complexed with serum lipoproteins similarly to heparin. In preliminary studies cholesterol-fed rabbits treated with Vessel exhibited somewhat less atherosclerosis than controls.

摘要

从商用血管中分离出类肝素糖胺聚糖(GAG)并研究其生物学特性。发现血管是硫酸软骨素、硫酸皮肤素和类肝素GAG的混合物。用软骨素酶ABC水解血管中的硫酸软骨素和硫酸皮肤素,剩余的血管在Dowex-1 Cl-柱上进行分级分离,用逐步增加浓度的NaCl(1.2 - 4.0 M)洗脱。在1.6 M和1.8 M NaCl处洗脱的主要级分通过化学分析初步鉴定为类肝素GAG,其硫酸含量略低于标准肝素。两个级分都具有与肝素相似的脂蛋白脂肪酶释放活性和抗凝血活性,但1.6 M NaCl级分的抗凝血活性是标准肝素的三分之一。1.8 M NaCl级分与血清脂蛋白的结合方式与肝素相似。在初步研究中,用血管处理的高胆固醇喂养兔子的动脉粥样硬化程度比对照组略轻。

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