Web Release Date: January 28,
Polyacetylenic Compounds, ACAT Inhibitors from the Roots of Panax ginseng
Laboratory of Lipid Metabolism, Korea Research Institute of Bioscience and Biotechnology, 52 Eoundong, Yusong-gu, Taejon 305-333, Korea
Received for review August 18, 2004. Revised manuscript received November 7, 2004. Accepted November 11, 2004.
Abstract:
Acyl-CoA: cholesterol acyltransferase (ACAT), which plays a role in the absorption, storage, and
production of cholesterol, has been explored as a potential target for pharmacological intervention of
hyperlipidemia and atherosclerotic disease. In our search for ACAT inhibitors from natural sources,
the petroleum ether extract of Panax ginseng showed moderate inhibition of ACAT enzyme from rat
liver microsomes. Bioactivity-guided fractionations led to the isolation of one new polyacetylenic
compound, (9R,10S)-epoxy-16-heptadecene-4, 6-diyne-3-one (1), in addition to the previously reported
polyacetylenic compounds 2 and 3. Their chemical structures were elucidated on the basis of
spectroscopic evidence (UV, IR, NMR, and MS). The compounds 1, 2, and 3 showed significant
ACAT inhibition with IC50 values of 35, 47, and 21 
M, respectively.
Keywords: Panax ginseng; Acyl-CoA: cholesterol acyltransferase (ACAT); Polyacetylenes; atherosclerosis; cholesteryl ester
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