Inhibitory effect of chalcone derivatives on recombinant human aldose reductase |
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| Authors: | Iwata S Nagata N Omae A Yamaguchi S Okada Y Shibata S Okuyama T |
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| Affiliation: | Research Laboratory, Minophagen Pharmaceutical Co., Ltd., Kanagawa, Japan. |
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| 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. |
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