: Quinolone alkaloid as inhibitors of acyl CoA:diacylglycerol acyltransferase the method for preparing thereof and pharmaceutical compositions containing the same

摘要

PURPOSE: Quinolone alkaloid as an inhibitor of acyl CoA:diacylglycerol acyltransferase, a method for preparing the same and pharmaceutical compositions containing the same are provided. The compounds inhibit absorption of neutral fat and biosynthesis of neutral fat in liver, fat cell and muscle cell to reduce neutral fat in blood and inhibit accumulation of neutral fat in organs, so that they can be useful for prevention and treatment of disease caused by disorder of neutral fat. CONSTITUTION: Quinolone alkaloid as an inhibitor of acyl CoA:diacylglycerol acyltransferase is represented by the formula(1), the formula(2), the formula(3), the formula(4) or the formula(5), wherein R is C5 to C20 aliphatic compound. A method for preparing the quinolone alkaloid represented by the formula(1) comprises the steps of: (1) extracting Evodiae Fructus with lower alcohol such as 10 to 100% methanol or ethanol; (2) extracting the alcohol extract with acetic acid ester such as ethylacetate; (3) subjecting the acetic acid ester extract to silica gel column chromatography; (4) subjecting the active fraction to reverse phase low pressure column chromatography; and (5) subjecting the active fraction to high pressure liquid chromatography(HPLC).