Sesquiterpenoids isolated from the flower buds of Tussilago farfara L. inhibit diacylglycerol acyltransferase = 관동화유래 세스퀴테르펜계 물질의 지방생합성 저해효과

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Title
Sesquiterpenoids isolated from the flower buds of Tussilago farfara L. inhibit diacylglycerol acyltransferase = 관동화유래 세스퀴테르펜계 물질의 지방생합성 저해효과
Author(s)
H R Park; M Y Yoo; Jee Hee Seo; Il Sun Kim; Nam Yue Kim; J Y Kang; L Cui; C S Lee; Chul Ho Lee; Hyun Sun Lee
Bibliographic Citation
Journal of Agricultural and Food Chemistry, vol. 56, no. 22, pp. 10493-10497
Publication Year
2008
Abstract
Inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT), which is a key enzyme in triglyceride synthesis in eukaryotic organisms, has been proposed as one of the drug targets for treating obesity, type II diabetes mellitus, and metabolic syndrome. Bioassay-guided fractionation of EtOH extract of the flower buds of Tussilago farfara, using an in vitro DGAT enzyme assay, resulted in the isolation of four known sesquiterpenoids, tussilagonone (1), tussilagone (2), 7β-(3-ethyl-cis-crotonoyloxy)-1α-(2-methylbutyryloxy)-3, 14-dehydro-Z-notonipetranone (3), and 8-angeloylxy-3,4-epoxy-bisabola-7(14),10- dien-2-one (4). DGAT1 inhibitory activity was studied by in vitro DGAT assay using rat liver microsomes and HepG2 cell microsomes. They showed DGAT1 inhibition with IC50 values of 99.2 (1), 18.8 (2), 47.0 (3), and 211.1 (4) μM (for rat liver microsomes) and >1 mM(1), 49.1 (2), 160.7 (3), and 294.4 (4) μM (for HepG2 cell microsomes), respectively. Compound 2 showed the most potent inhibition against microsomal DGAT1 derived from rat liver and human hepatocellular carcinoma HepG2 cells and also significantly inhibited triglyceride synthesis by suppressing incorporation of [ 14C]acetate or [14C]glycerol into triglycerides in HepG2 cells. These findings suggest that tussilagone is a potential lead compound in the treatment of obesity and type 2 diabetes.
Keyword
diacylglycerol acyltansferase (DGAT)obesitysesquiterpenoidtriglyceride synthesistussilago farfaratype II diabetes
ISSN
0021-8561
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/jf801978r
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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