Search for Naturally Occuring Substances to Prevent the Complications of Diabetes. Part III. Inhibitory Effect of Chalcone Derivatives on Recombinant Human Aldose Reductase.
- 1 January 1999
- journal article
- Published by Pharmaceutical Society of Japan in Biological & Pharmaceutical Bulletin
- Vol. 22 (3) , 323-325
- https://doi.org/10.1248/bpb.22.323
Abstract
More than fifty chalcone derivatives were synthesized to examine structure-activity relationships against human aldose reductase. Certain 2',4'-dihydroxychalcone derivatives inhibited human aldose reductase activities, and 2',4',2, 4-tetrahydroxychalcone and 2',4',2-trihydroxychalcone showed potent inhibitory activity with IC50 values of 7.4x10(-9) M and 1.6x10(-7) M, respectively. On the other hand, cis-form chalcones, which were isomerized from the original trans-forms by irradiation of daylight in methanol solution, promoted the activity of human aldose reductase.Keywords
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