title: Glabrol, an acyl-coenzyme A: cholesterol acyltransferase inhibitor from licorice roots.
abstract: 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 IC(50) value of 24.6 microM and decreased cholesteryl ester formation with an IC(50) value of 26.0 microM in HepG2 cells. In addition, 1 showed a non-competitive type of inhibition against ACAT.
authors.affiliation: Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yusong-gu, Daejeon 305-333, Republic of Korea.
authors.forename: Jung Ho
authors.initials: JH
authors.lastname: Choi
authors.forename: Mun-Chual
authors.initials: MC
authors.lastname: Rho
authors.forename: Seung Woong
authors.initials: SW
authors.lastname: Lee
authors.forename: Oh Eok
authors.initials: OE
authors.lastname: Kwon
authors.forename: Hye Ran
authors.initials: HR
authors.lastname: Park
authors.forename: Ji Yun
authors.initials: JY
authors.lastname: Kang
authors.forename: Seung Ho
authors.initials: SH
authors.lastname: Lee
authors.forename: Hyun Sun
authors.initials: HS
authors.lastname: Lee
authors.forename: Ki Hwan
authors.initials: KH
authors.lastname: Bae
authors.forename: Young Kook
authors.initials: YK
authors.lastname: Kim
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D050197:Atherosclerosis / Q000188:drug therapy; D045744:Cell Line, Tumor; D002788:Cholesterol Esters / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D006035:Glycyrrhiza / Q000737:chemistry*; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D008517:Phytotherapy; D018517:Plant Roots; D010946:Plants, Medicinal / Q000737:chemistry; D051381:Rats; D002785:Sterol O-Acyltransferase / Q000187:drug effects* / Q000378:metabolism
chemical_list: D000924:Anticholesteremic Agents; D002788:Cholesterol Esters; D005419:Flavonoids; C420863:glabrol; D002785:Sterol O-Acyltransferase