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Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase Full article

Journal Russian Journal of Bioorganic Chemistry
ISSN: 1068-1620
Output data Year: 2011, Volume: 37, Number: 5, Pages: 569-577 Pages count : DOI: 10.1134/S1068162011050050
Tags aldose reductase; N-(3 beta-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid; ursolic acid derivatives; diabetic complications
Authors Lee Eun Ha 1 , Popov S. A. 2 , Lee Joo Young 1 , Shpatov A. V. 2 , Kukina T. P. 2 , Kang Suk Woo 1 , Pan Cheol Ho 1 , Um Byung Hun 1 , Jung Sang Hoon 1
Affiliations
1 (Данные Web of science) Korea Inst Sci & Technol KIST, Gangneung Inst, Nat Prod Res Ctr, Kangnung 210340, Gangwon Do, South Korea
2 (Данные Web of science) Novosibirsk Organ Chem Inst, Novosibirsk, Russia

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-(3 beta-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid (XV) showed most potent rhAR inhibitory activity in vitro. Inhibition mode of N-(3 beta-hydroxyurs-12-en-28-oyl)-4-aminobutyric acid (XV) was tested uncompetitively by kinetic analysis using the Lineweaver-Burk plots. Ursolic acid derivative N-(3 beta-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.
Cite: Lee E.H. , Popov S.A. , Lee J.Y. , Shpatov A.V. , Kukina T.P. , Kang S.W. , Pan C.H. , Um B.H. , Jung S.H.
Inhibitory effect of ursolic acid derivatives on recombinant human aldose reductase
Russian Journal of Bioorganic Chemistry. 2011. V.37. N5. P.569-577. DOI: 10.1134/S1068162011050050 WOS Scopus РИНЦ
Dates:
Published print: Sep 1, 2011
Published online: Oct 1, 2011
Identifiers:
Web of science WOS:000295533200007
Scopus 2-s2.0-80055000521
Elibrary 18011095
OpenAlex W2077366989
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