Polyacetylenic Compounds, ACAT Inhibitors from the Roots of Panax ginseng

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,...

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Bibliographic Details
Published in:Journal of agricultural and food chemistry 2005-02, Vol.53 (4), p.919-922
Main Authors: Rho, Mun-Chual, Lee, Hyun Sun, Lee, Seung Woong, Chang, Jong Sun, Kwon, Oh Eok, Chung, Mi Yeon, Kim, Young Kook
Format: Article
Language:English
Subjects:
Acetylene - analogs & derivatives
Acetylene - analysis
Acetylene - chemistry
Acetylene - isolation & purification
Acetylene - pharmacology
Alkynes
Animals
Biological and medical sciences
chemical structure
cholesteremic effect
cholesterol acyltransferase
Diynes
enzyme inhibitors
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - isolation & purification
Enzyme Inhibitors - pharmacology
Epoxy Compounds - chemistry
Epoxy Compounds - isolation & purification
Epoxy Compounds - pharmacology
General pharmacology
Medical sciences
medicinal properties
Microsomes, Liver - enzymology
Molecular Structure
Panax - chemistry
Panax pseudoginseng
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
plant extracts
Plant Roots - chemistry
Polyacetylenes
Polymers - analysis
Polymers - chemistry
Rats
roots
spectroscopy
Sterol O-Acyltransferase - antagonists & inhibitors
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Summary: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 μM, respectively. Keywords: Panax ginseng; Acyl-CoA:  cholesterol acyltransferase (ACAT); Polyacetylenes; atherosclerosis; cholesteryl ester
ISSN:0021-8561
1520-5118
DOI:10.1021/jf040370x