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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.

Citation

Jung Ho Choi, Mun-Chual Rho, Seung Woong Lee, Oh Eok Kwon, Hye Ran Park, Ji Yun Kang, Seung Ho Lee, Hyun Sun Lee, Ki Hwan Bae, Young Kook Kim. Glabrol, an acyl-coenzyme A: cholesterol acyltransferase inhibitor from licorice roots. Journal of ethnopharmacology. 2007 Apr 4;110(3):563-6

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PMID: 17123760

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