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Synthesis and a-glucosidase inhibitory activity of chrysin, diosmetin,apigenin, and luteolin derivatives

查看全文 作  者:Ning [1]Cheng;Wen-Bin [1]Yi;Qi-Qin [1]Wang;Sheng-Ming [1,2]Peng;Xiao-Qing [2]Zou 高影响力作者 机构地区:[1]Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education,College of Chemistry,Xiangtan University;[2]Postdoctoral Programme of Chemical Engineering & Technology,Xiangtan University高影响力机构 出  处:《Chinese Chemical Letters》索引2014年第25卷第7期,共5页高影响力期刊 基  金:supported by the Research Fund for the Doctoral Program of Higher Education of China(No.20114301120004);Hunan Provincial Natural Science Foundation of China(No.12JJ6081);Dr.’s Start-up Foundation of Xiangtan University(No.06KZjKZ08035);Natural Science Foundation of Xiangtan University(No.2011XZX09) 摘  要:Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The a-glucosidase inhibitory activity of these compounds was evaluated. The glucosidase inhibitory activity of all derivatives(IC50< 24.396 mmol/L) was higher compared with that of the reference drug, acarbose(IC50= 563.601 40.492 mmol/L), and 1-deoxynojirimycin(IC50= 226.912 12.573 mmol/L). O30,O7-Hexyl diosmetin(IC50= 2.406 0.101 mmol/L)was the most potent inhibitor identified. These compounds showed a higher inhibitory ability compared with their precursors except the luteolin derivatives. In general, the inhibitory activity of the synthetic derivatives was enhanced with long alkyl chains at positions 30, 40 and 7 of the flavonoid. 关 键 词:葡萄糖苷酶 抑制活性 木犀草素 衍生物 白杨素 芹菜素 合成 木素
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