Glabrol, an acyl-coenzyme A: Cholesterol acyltransferase inhibitor from licorice roots

被引:12
|
作者
Choi, Jung Ho
Rho, Mun-Chual
Lee, Seung Woong
Kwon, Oh Eok
Park, Hye Ran
Kang, Ji Yun
Lee, Seung Ho
Lee, Hyun Sun
Bae, Ki Hwan
Kim, Young Kook
机构
[1] Korea Res Inst Biosci & Biotechnol, Nat Med Res Ctr, Taejon 305333, South Korea
[2] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
[3] Chungnam Natl Univ, Coll Pharm, Taejon, South Korea
关键词
acyl-CoA; cholesterol acyltransferase; licorice; hypocholesterolemia; atherosclerosis;
D O I
10.1016/j.jep.2006.10.012
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Acyl-coenzyme A: cholesterol acyltransferase (ACAT) esterifies free cholesterol in the liver and the intestine. It has relations with production of lipoproteins and accumulation of cholesteryl esters of the atheroma. Therefore, ACAT inhibitors may act as antihypercholesterolemic and antiatherosclerotic agents. One isoprenyl flavonoid was isolated from ethanol extract of licorice roots. On the basis of spectral evidences, the compound was identified as glabrol (1). Compound 1 inhibited rat liver microsomal ACAT activity with an IC50 value of 24.6 mu M and decreased cholesteryl ester formation with an IC50 value of 26.0 mu M in HepG2 cells. In addition, 1 showed a non-competitive type of inhibition against ACAT. (c) 2006 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码:563 / 566
页数:4
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