1. Bavachin and isobavachalcone, acyl-coenzyme A: cholesterol acyltransferase inhibitors from Psoralea corylifolia.
- Author
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Choi JH, Rho MC, Lee SW, Choi JN, Kim K, Song GY, and Kim YK
- Subjects
- Animals, Cell Line, Tumor, Cholesterol Esters chemical synthesis, Dose-Response Relationship, Drug, Humans, Indicators and Reagents, Kinetics, Liver drug effects, Liver enzymology, Magnetic Resonance Spectroscopy, Microsomes, Liver drug effects, Microsomes, Liver enzymology, Rats, Seeds chemistry, Spectrometry, Mass, Electrospray Ionization, Spectrophotometry, Ultraviolet, Chalcones isolation & purification, Chalcones pharmacology, Enzyme Inhibitors isolation & purification, Enzyme Inhibitors pharmacology, Flavonoids isolation & purification, Flavonoids pharmacology, Psoralea chemistry, Sterol O-Acyltransferase antagonists & inhibitors
- Abstract
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 ((1)H-, (13)C-NMR, 2DNMR, and ESI-MS). The IC(50) values were 86.0 (1) and 48.0 (2) microM 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.
- Published
- 2008
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