New Polyacetylenes, DGAT Inhibitors from the Roots of Panax ginseng
Seung Woong Lee1
, Koanhoi Kim1
, Mun-Chual Rho1
, Mi Yeon Chung1
, Young Ho Kim2
, Sangku Lee1
, Hyun Sun Lee1
, Young Kook Kim1
1Laboratory of Lipid Metabolism, Korea Research Institute of Bioscience and Biotechnology, Taejon, Korea
2College of Pharmacy, Chungnam National University, Taejon, Korea
This research was supported by grants from Plant Diversity Research Center of 21st Century Frontier Research Program and KRIBB Research Initiative Program funded by the Ministry of Science and Technology of the Korean government
The petroleum ether extract of Panax ginseng showed a significant inhibition of the diacylglycerol acyltransferase (DGAT) enzyme from rat liver microsomes. Bioactivity-guided fractionation led to the isolation of two new polyacetylenic compounds, (9R,10S)-epoxyheptadecan-4,6-diyn-3-one (1) and 1-methoxy-(9R,10S)-epoxyheptadecan-4,6-diyn-3-one (2). Their chemical structures were elucidated on the basis of spectroscopic evidence and asymmetric synthesis. IC50 values of 9 μg/mL (1) and 32 μg/mL (2) were obtained.
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