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5α-胆甾-8(14)-烯-3β-醇-15-酮。酰基辅酶A:胆固醇酰基转移酶的竞争性底物。

5 alpha-cholest-8(14)-en-3 beta-ol-15-one. A competitive substrate for acyl coenzyme A:cholesterol acyl transferase.

作者信息

Miller L R, Needleman D H, Brabson J S, Wang K S, Schroepfer G J

机构信息

Department of Biochemistry, Rice University, Houston, TX 77251.

出版信息

Biochem Biophys Res Commun. 1987 Nov 13;148(3):934-40. doi: 10.1016/s0006-291x(87)80222-x.

Abstract

5 alpha-Cholest-8(14)-en-3 beta-ol-15-one, a potent inhibitor of cholesterol biosynthesis with hypocholesterolemic activity, has been found to serve as an efficient substrate for acyl CoA:cholesterol acyl transferase of rat hepatic and jejunal microsomes and to inhibit the esterification of cholesterol. Concentrations required to give 50% inhibition of cholesterol ester formation in liver and jejunal microsomes were approximately 10 microM and approximately 3 microM, respectively.

摘要

5α-胆甾-8(14)-烯-3β-醇-15-酮是一种具有降胆固醇活性的强效胆固醇生物合成抑制剂,已被发现可作为大鼠肝脏和空肠微粒体中酰基辅酶A:胆固醇酰基转移酶的有效底物,并抑制胆固醇的酯化。在肝脏和空肠微粒体中产生50%胆固醇酯形成抑制所需的浓度分别约为10微摩尔和约3微摩尔。

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