Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase

Title
Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase
Authors
이은하Popov S.A.이주영Shpatov A.V.Kukina T.P.강석우판철호엄병헌정상훈
Keywords
aldose reductase; ursolic acid derivatives; diabetic complications
Issue Date
2011-09
Publisher
Russian journal of bioorganic chemistry
Citation
VOL 37, NO 5, 637-644
Abstract
Aldose reductase (AR) is the first enzyme in the polyol pathway. AR has been reported to play an important role in the pathogenesis of diabetic complications. Ursolic acid and fourteen synthetic derivatives with ursane skeleton were tested for recombinant human aldose reductase (rhAR) inhibitory activity for development of diabetic complications. Among them, N-(3β-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid (XV) showed most potent rhAR inhibitory activity in vitro. Inhibition mode of N-(3β-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid (XV) was tested uncompetitively by kinetic analysis using the Lineweaver Burk plots. Ursolic acid derivative N-(3β-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid is able to inhibit rhAR uncompetitively and could be offered as a lead compound for AR inhibition.
URI
http://pubs.kist.re.kr/handle/201004/40248
ISSN
1068-1620
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