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
来源：
JOURNAL OF ETHNOPHARMACOLOGY | 2007年 / 110卷 / 03期
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
相关论文
共 17 条
  • [1] ALICE FM, 2002, PLANTA MED, V68, P416
  • [2] Effect of F-1394, an acyl-CoA:cholesterol acyltransferase inhibitor, on atherosclerosis induced by high cholesterol diet in rabbits
    Aragane, K
    Kojima, K
    Fujinami, K
    Kamei, J
    Kusunoki, J
    [J]. ATHEROSCLEROSIS, 2001, 158 (01) : 139 - 145
  • [3] The ACAT inhibitor avasimibe reduces macrophages and matrix metalloproteinase expression in atherosclerotic lesions of hypercholesterolemic rabbits
    Bocan, TMA
    Krause, BR
    Rosebury, WS
    Mueller, SB
    Lu, XK
    Dagle, C
    Major, T
    Lathia, C
    Lee, H
    [J]. ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY, 2000, 20 (01) : 70 - 79
  • [4] BURNETT JR, 2000, BIOCHIM BIOPHYS ACTA, V1738, P10
  • [5] THE STRUCTURE OF ACYL-COENZYME A-CHOLESTEROL ACYLTRANSFERASE AND ITS POTENTIAL RELEVANCE TO ATHEROSCLEROSIS
    CHANG, TY
    CHANG, CCY
    CADIGAN, KM
    [J]. TRENDS IN CARDIOVASCULAR MEDICINE, 1994, 4 (05) : 223 - 230
  • [6] Acyl-coenzyme A: Cholesterol acyltransferase
    Chang, TY
    Chang, CCY
    Cheng, D
    [J]. ANNUAL REVIEW OF BIOCHEMISTRY, 1997, 66 : 613 - 638
  • [7] Antiatherosclerotic effects of licorice extract supplementation on hypercholesterolemic patients: Increased resistance of LDL to atherogenic modifications, reduced plasma lipid levels, and decreased systolic blood pressure
    Fuhrman, B
    Volkova, N
    Kaplan, M
    Presser, D
    Attias, J
    Hayek, T
    Aviram, M
    [J]. NUTRITION, 2002, 18 (03) : 268 - 273
  • [8] Licorice extract and its major polyphenol glabridin protect low-density lipoprotein against lipid peroxidation: In vitro and ex vivo studies in humans and in atherosclerotic apolipoprotein E-deficient mice
    Fuhrman, B
    Buch, S
    Vaya, J
    Belinky, PA
    Coleman, R
    Hayek, T
    Aviram, M
    [J]. AMERICAN JOURNAL OF CLINICAL NUTRITION, 1997, 66 (02) : 267 - 275
  • [9] Hexadecylphosphocholine disrupts cholesterol homeostasis and induces the accumulation of free cholesterol in HepG2 tumour cells
    Jiménez-López, JM
    Carrasco, MP
    Marco, C
    Segovia, JL
    [J]. BIOCHEMICAL PHARMACOLOGY, 2006, 71 (08) : 1114 - 1121
  • [10] Phenylpyropene A and B, new inhibitors of acyl-CoA:: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959
    Kwon, OE
    Rho, MC
    Song, HY
    Lee, SW
    Chung, MY
    Lee, JH
    Kim, YH
    Lee, HS
    Kim, YK
    [J]. JOURNAL OF ANTIBIOTICS, 2002, 55 (11) : 1004 - 1008
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