Inhibitory Effect of Chalcone Derivatives on Recombinant Human Aldose Reductase

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 7.4×10^-9 M and 1.6×10^-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.