New Polyacetylenes, DGAT inhibitors from the roots of Panax ginseng.
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, (9 R,10 S)-epoxyheptadecan-4,6-diyn-3-one ( 1) and 1-methoxy-(9 R,10 S)-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 microg/mL ( 1) and 32 microg/mL ( 2) were obtained.
Lee
Seung Woong
SW
Korea Research Institute of Bioscience and Biotechnology, Taejon, Korea.
Kim
Koanhoi
K
Rho
Mun-Chual
MC
Chung
Mi Yeon
MY
Kim
Young Ho
YH
Lee
Sangku
S
Lee
Hyun Sun
HS
Kim
Young Kook
YK
D000114:Acetylene / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use; D000217:Acyltransferases / Q000037:antagonists & inhibitors* / Q000187:drug effects*; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D020128:Inhibitory Concentration 50; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D005894:Panax; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots; D011108:Polymers / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D053279:Polyynes; D051381:Rats
D004791:Enzyme Inhibitors; D010936:Plant Extracts; D011108:Polymers; D053279:Polyynes; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase; D000114:Acetylene