High hypolipidemic activity of saturated side-chain α-asarone analogs

With the aim of evaluating the pharmacophore potential of the side chain of α-asarone (1) regarding its high hypolipidemic activity, the series of derivatives 7a-7e, and 11-13 were evaluated pharmacologically. For the hydrocarbon compounds 7a-7e, with a variable-size side chain, significant decreases in serum cholesterol, LDL-cholesterol, and triglyceride levels and significant increases in HDL-cholesterol levels were observed in mice. The small-size side-chain derivatives were even more active than 1 in reducing cholesterol. The results suggested that the length and saturated character of the side chain seem to be a key feature in improving hypolipidemic activity of α-asarone (1) analogs.