Inhibitory effect of chalcone derivatives on recombinant human aldose reductase.
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.
Iwata
S
S
Research Laboratory, Minophagen Pharmaceutical Co., Ltd., Kanagawa, Japan.
Nagata
N
N
Omae
A
A
Yamaguchi
S
S
Okada
Y
Y
Shibata
S
S
Okuyama
T
T
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D002599:Chalcone / Q000031:analogs & derivatives / Q000494:pharmacology*; D006801:Humans; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D011994:Recombinant Proteins; D002599:Chalcone; D000449:Aldehyde Reductase