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Title 

Sesquiterpenoids isolated from the flower buds of Tussilago farfara L. inhibit diacylglycerol acyltransferase

 

관동화유래 세스퀴테르펜계 물질의 지방생합성 저해효과

Authors 

H R ParkM Y YooJee Hee SeoIl Sun KimNam Yue KimJ Y KangL CuiC S LeeChul Ho LeeHyun Sun Lee

Publisher 

American Chemical Society

Issue Date 

2008

Citation 

Journal of Agricultural and Food Chemistry, vol. 56, no. 22, pp. 10493-10497

Keywords 

diacylglycerol acyltansferase (DGAT)obesitysesquiterpenoidtriglyceride synthesistussilago farfaratype II diabetesdiacylglycerol acyltransferaseenzyme inhibitortriacylglycerolanimal

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.

ISSN 

0021-8561

Link 

http://dx.doi.org/10.1021/jf801978r

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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