Objective:To evaluate inhibitoy potential of seven Korean thistles against the advanced glyeatinn endproducts(AGE) formation as well as to identify responsible compounds from the most active species.Methods:We used an...Objective:To evaluate inhibitoy potential of seven Korean thistles against the advanced glyeatinn endproducts(AGE) formation as well as to identify responsible compounds from the most active species.Methods:We used an in vitro AGE inhibition assay to evaluate the antidiabetic complication potential of the methanol extracts of the selected Korean thistles.Results:Among the seven Korean thistles,the leaves of Cirsium maackii(C.maackii) exhibited the most significant inhibitory activity against AGE formation.By means of bioassay-directed fractionation,a lignan.chlorogenic acid and 14 flavonoids were isolated from the active ethyl acetate soluble fraction of a methanol extract from C.maackii leaves.Luteolin and its 5-O-glueoside have been previously isolated:however,a lignan and 13 known compounds were isolated for the first lime from C maackii leaves in this study.Most of the isolated compounds exhibited inhibitory activities against potential AGE formation.Among them,cernuoside was shown to be the most potent AGE inhibitor with an IC_(50) value of 21.21 μ mol/L.Most importantly,two major flavonoids,luteolin and ils 5-O-glucoside,also significantly inhibited AGE formation,with IC_(50) values of36.33 and 37.47 μmol/L,respectively.Structure activity relationship revealed that the presence of free 3'and 4' dihydroxyl group in flavonoids skeleton played an important role in AGE inhibition.Conclusions:These results indicate that C.maackii and C maackii-derived flavonoids might be explored further to develop therapeutic agents for the prevention of diabetic eoniplicalions due to their significant inhibitory activity against AGE formation.展开更多
基金supported by the Pukyoug National University Research Fund in 2011(C-D-2011-0766)
文摘Objective:To evaluate inhibitoy potential of seven Korean thistles against the advanced glyeatinn endproducts(AGE) formation as well as to identify responsible compounds from the most active species.Methods:We used an in vitro AGE inhibition assay to evaluate the antidiabetic complication potential of the methanol extracts of the selected Korean thistles.Results:Among the seven Korean thistles,the leaves of Cirsium maackii(C.maackii) exhibited the most significant inhibitory activity against AGE formation.By means of bioassay-directed fractionation,a lignan.chlorogenic acid and 14 flavonoids were isolated from the active ethyl acetate soluble fraction of a methanol extract from C.maackii leaves.Luteolin and its 5-O-glueoside have been previously isolated:however,a lignan and 13 known compounds were isolated for the first lime from C maackii leaves in this study.Most of the isolated compounds exhibited inhibitory activities against potential AGE formation.Among them,cernuoside was shown to be the most potent AGE inhibitor with an IC_(50) value of 21.21 μ mol/L.Most importantly,two major flavonoids,luteolin and ils 5-O-glucoside,also significantly inhibited AGE formation,with IC_(50) values of36.33 and 37.47 μmol/L,respectively.Structure activity relationship revealed that the presence of free 3'and 4' dihydroxyl group in flavonoids skeleton played an important role in AGE inhibition.Conclusions:These results indicate that C.maackii and C maackii-derived flavonoids might be explored further to develop therapeutic agents for the prevention of diabetic eoniplicalions due to their significant inhibitory activity against AGE formation.
