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KMID : 0043320080310111419
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Archives of Pharmacal Research
2008 Volume.31 No. 11 p.1419 ~ p.1423
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Bavachin and Isobavachalcone, Acyl-coenzyme A: Cholesterol Acyltransferase Inhibitors from Psoralea corylifolia
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Kim Young-Kook
Song Gyu-Yong
Rho Mun-Chual
Choi Jung-Ho
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Abstract
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Acyl-coenzyme A: cholesterol acyltransferase (ACAT) catalyzes cholesterol esterification and plays important roles in intestinal absorption of cholesterol, hepatic production of lipoproteins and accumulation of cholesteryl ester within macrophages and smooth muscle cells. Ethanol extract of Psoralea corylifolia showed a significant inhibition of ACAT enzyme. Via bioactivity-guided fractionation of the ethanol extract of Psoralea corylifolia, two prenylated flavonoids were isolated. Their structures were determined as bavachin (1) and isobavachalcone (2) by spectroscopic analysis (1H-, 13C-NMR, 2DNMR, and ESI-MS). The IC50 values were 86.0 (1) and 48.0 (2) μM in the ACAT assay system using rat liver microsome. Compound 2 also decreased cholesteryl ester formations in HepG2 cells. In addition, this compound showed a noncompetitive type of inhibition of ACAT.
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KEYWORD
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Acyl-coenzyme A: cholesterol acyltransferase (ACAT), Enzyme assay, Psoralea corylifolia, Prenylated flavonoids, Hypolipidemia, Atherosclerosis
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