title: 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 7.4x10(-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.
authors.affiliation: Research Laboratory, Minophagen Pharmaceutical Co., Ltd., Kanagawa, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Iwata
authors.forename: N
authors.initials: N
authors.lastname: Nagata
authors.forename: A
authors.initials: A
authors.lastname: Omae
authors.forename: S
authors.initials: S
authors.lastname: Yamaguchi
authors.forename: Y
authors.initials: Y
authors.lastname: Okada
authors.forename: S
authors.initials: S
authors.lastname: Shibata
authors.forename: T
authors.initials: T
authors.lastname: Okuyama
mesh_terms: 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
chemical_list: D011994:Recombinant Proteins; D002599:Chalcone; D000449:Aldehyde Reductase