Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/34062
Title: Curcumin analogs as potent aldose reductase inhibitors
Authors: Du, ZY
Bao, YD
Liu, Z
Qiao, W
Ma, L
Huang, ZS
Gu, LQ
Chan, ASC
Keywords: Aldose reductase inhibitors
Curcumin analogs
Curcuminoids
Diabetic complication
Issue Date: 2006
Source: Archiv der pharmazie, 2006, v. 339, no. 3, p. 123-128 How to cite?
Journal: Archiv der Pharmazie 
Abstract: In the present study, curcuminoids isolated from curcuma longa were demonstrated to possess inhibitory activities on bovine lens aldose reductase. In order to find more potent aldose reductase inhibitor, curcumin analogs were synthesized and evaluated for their ability to inhibit bovine lens aldose reductase enzyme. The results indicated that the compounds with tetrahydroxyl groups, 2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone (A 2), 2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone (B 2), 1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one (C 2), and 3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone (D 2) showed remarkably potent inhibitory effects on aldose reductase with IC 50 of 2.9 μM, 2.6 μM, 3.4 μM, and 4.9 μM, respectively. The structure-activity relationship revealed that the curcumin analogs with ortho-dihydroxyl groups could form a more tight affinity with aldose reductase to exert more potential inhibitory activities.
URI: http://hdl.handle.net/10397/34062
ISSN: 0365-6233
DOI: 10.1002/ardp.200500205
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