Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase
- Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase
- 이은하; Popov S.A.; 이주영; Shpatov A.V.; Kukina T.P.; 강석우; 판철호; 엄병헌; 정상훈
- aldose reductase; ursolic acid derivatives; diabetic complications
- Issue Date
- Russian journal of bioorganic chemistry
- VOL 37, NO 5, 637-644
- 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.
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