Glabrol, an acyl-coenzyme A: cholesterol acyltransferase inhibitor from licorice roots.
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.
Choi
Jung Ho
JH
Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yusong-gu, Daejeon 305-333, Republic of Korea.
Rho
Mun-Chual
MC
Lee
Seung Woong
SW
Kwon
Oh Eok
OE
Park
Hye Ran
HR
Kang
Ji Yun
JY
Lee
Seung Ho
SH
Lee
Hyun Sun
HS
Bae
Ki Hwan
KH
Kim
Young Kook
YK
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
D000924:Anticholesteremic Agents; D002788:Cholesterol Esters; D005419:Flavonoids; C420863:glabrol; D002785:Sterol O-Acyltransferase