Glycosidase Inhibitory Flavonoids from Sophora flavescens(Medicinal Chemistry)

概要

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The methanol extract of Sophora flavescens showed a potent glycosidase inhibitory activity. Active components were identified as well-known flavonoid antioxidants: kushenol A (1), (-)-kurarinone (2), sophoraflavanone G (3), 2'-methoxykurarinone (4), kurarinol (5), 8-prenylkaempferol (6), isoxanthohumol (7), kuraridin (8) and maackian (9). All flavonoids were effective inhibitors of α-glucosidase and β-amylase. Interestingly, lavandulylated flavanones 1-5 had strong α-glucosidase inhibitory activities, with IC_<50> values of 45μM, 68μM, 37μM, 155μM and 179μM, respectively. Kushenol A (1) which does not bear a 4'-hydroxy group showed selective α-glucosidase inhibitory activity. Lavandulylated chalcone, kuraridine (8), exhibited IC_<50> value of 57μM against β-glucosidase, which is the first report of a chalcone displaying glycosidase inhibition. Results showed that 8-lavandulyl group in B-ring was a key factor of the glycosidase inhibitory activities. The inhibition pattern was noncompetitive for α-glucosidase, whereas mixed inhibition was observed for β-amylase.
公益社団法人日本薬学会の論文
2006-02-01