Inhibition of diacylglycerol acyltransferase by betulinic acid from Alnus hirsuta

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Title
Inhibition of diacylglycerol acyltransferase by betulinic acid from Alnus hirsuta
Author(s)
Mi Yeon Chung; Mun Chual RhoSeung Woong Lee; Hye Ran Park; K Kim; I A Lee; D H Kim; K H Jeune; Hyun Sun Lee; Young Kook Kim
Bibliographic Citation
Planta Medica, vol. 72, no. 3, pp. 267-269
Publication Year
2006
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
Publisher
Georg Thieme Verlag Kg
DOI
http://dx.doi.org/10.1055/s-2005-916178
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Immunoregulatory materials Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Medicine Research Center > 1. Journal Articles
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