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标题：Glycosidase Inhibitory Flavonoids from Sophora flavescens
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作者：Jin Hyo Kim ; Young Bae Ryu ; Nam Suk Kang 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2006
卷号：29
期号：2
页码：302-305
DOI：10.1248/bpb.29.302
出版社：The Pharmaceutical Society of Japan
摘要：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 IC₅₀ values of 45 μ M , 68 μ M , 37 μ M , 155 μ M and 179 μ M , respectively. Kushenol A (1) which does not bear a 4′-hydroxy group showed selective α-glucosidase inhibitory activity. Lavandulylated chalcone, kuraridine (8), exhibited IC₅₀ value of 57 μ M 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.
关键词：lavandulylated flavonoid;glycosidase inhibitor;Sophora flavescens;mixed-type inhibitor;noncompetitive inhibitor