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 antiatherosclero...

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Bibliographic Details
Published in:Journal of ethnopharmacology 2007-04, Vol.110 (3), p.563-566
Main Authors: 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
Format: Article
Language:English
Subjects:
acetyl coenzyme A
Acyl-CoA: cholesterol acyltransferase
Animals
antiatherosclerotic agents
anticholesteremic agents
Anticholesteremic Agents - isolation & purification
Anticholesteremic Agents - pharmacology
Atherosclerosis
Atherosclerosis - drug therapy
bioassays
Biological and medical sciences
Cell Line, Tumor
chemical constituents of plants
cholesterol acyltransferase
Cholesterol Esters - metabolism
Dose-Response Relationship, Drug
enzyme inhibitors
flavonoids
Flavonoids - isolation & purification
Flavonoids - pharmacology
General pharmacology
Glycyrrhiza - chemistry
Glycyrrhiza glabra
Hypocholesterolemia
Licorice
liver
Medical sciences
medicinal plants
medicinal properties
Microsomes, Liver - drug effects
Microsomes, Liver - metabolism
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Phytotherapy
plant extracts
Plant Roots
Plants, Medicinal - chemistry
Rats
roots
Sterol O-Acyltransferase - drug effects
Sterol O-Acyltransferase - metabolism
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Summary: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 μM and decreased cholesteryl ester formation with an IC 50 value of 26.0 μM in HepG2 cells. In addition, 1 showed a non-competitive type of inhibition against ACAT.
ISSN:0378-8741
1872-7573
DOI:10.1016/j.jep.2006.10.012