Bavachin and isobavachalcone, acyl-coenzyme A: Cholesterol acyltransferase inhibitors from Psoralea corylifolia

被引：0
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作者：
Jung Ho Choi
Mun-Chual Rho
Seung Woong Lee
Ji Na Choi
Koanhoi Kim
Gyu Young Song
Young Kook Kim
机构：
[1] KRIBB,Natural Medicine Research Center
[2] Pusan National University,Department of Pharmacology, School of Medicine
[3] Chungnam National University,Collage of Pharmacy
来源：
Archives of Pharmacal Research | 2008年 / 31卷
关键词：
Acyl-coenzyme A: cholesterol acyltransferase (ACAT); Enzyme assay; Prenylated flavonoids; Hypolipidemia; Atherosclerosis;
D O I：
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摘要：
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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