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A Flavone from<i>Manilkara indica</i>as a Specific Inhibitor against Aldose Reductase<i>In Vitro</i>
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2003
Year
Specific InhibitorBioorganic ChemistryAldo-keto ReductaseRedox BiologyOxidative StressMolecular PharmacologyMedicinal ChemistryPhytopharmacologyPhytochemicalGlycosylationLens Aldose ReductaseBiochemistryAldose Reductase InhibitionPharmacologyNadh OxidaseNatural SciencesPhytochemistryMedicineDrug Discovery
Isoaffinetin (5,7,3',4',5'-pentahydroxyflavone-6-C-glucoside) was isolated from Manilkara indica as a potent inhibitor of lens aldose reductase by bioassay-directed fractionation. This C-glucosyl flavone showed specific inhibition against aldose reductases (rat lens, porcine lens and recombinant human) with no inhibition against aldehyde reductase and NADH oxidase. Kinetic analysis showed that isoaffinetin exhibited uncompetitive inhibition against both dl-glyceraldehyde and NADPH. A structure-activity relationship study revealed that the increasing number of hydroxy groups in the B-ring contributes to the increase in aldose reductase inhibition by C-glucosyl flavones.