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Title 

Inhibition of diacylglycerol acyltransferase by betulinic acid from Alnus hirsuta

Authors 

Mi Yeon ChungMun Chual RhoSeung Woong LeeHye Ran ParkK KimI A LeeD H KimK H JeuneHyun Sun LeeYoung Kook Kim

Publisher 

Georg Thieme Verlag

Issue Date 

2006

Citation 

Planta Medica, vol. 72, no. 3, pp. 267-269

Keywords 

alnus hirsuta extractbetulic aciddiacylglycerol acyltransferasedrug inhibitionenzyme inhibitionalnusdiacylglycerol o-acyltransferasealnus hirsuta

Abstract 

During the screening for diacylglycerol acyltransferase (DGAT) inhibitors from natural products, the lupane-type triterpenoid betulinic acid was isolated from the methanol extract of Alnus hirsuta. It potently inhibited DGAT in the rat liver microsomes with an IC50 value of 9.6 μM. Enzyme kinetic studies showed apparent Km and Ki values of 13.3 μM and 8.1 μM using [14C]oleoyl-CoA as a substrate. A decrease in the apparent Vmax was observed with betulinic acid, whereas the apparent Km remained constant. Therefore, a Lineweaver-Burk plot of DGAT inhibition by betulinic acid showed a non-competitive type of inhibition. In the cell-based assay, betulinic acid inhibited triglyceride (TG) formation by human HepG2 cells. These findings suggest that betulinic acid may be a potential lead compound in the treatment of obesity.

ISSN 

0032-0943

Link 

http://dx.doi.org/10.1055/s-2005-916178

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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