| Synthesis and α-glucosidase inhibitory activity of chrysin,diosmetin, apigenin,and luteolin derivatives |
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| 作者姓名： | Ning Cheng Wen-Bin Yi Qi-Qin Wang Sheng-Ming Peng Xiao-Qing Zou |
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| 作者单位： | a Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, College of Chemistry, Xiangtan University, Xiangtan 411105, China;
b Postdoctoral Programme of Chemical Engineering & Technology, Xiangtan University, Xiangtan 411105, China |
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| 基金项目： | This work was financially 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. 06KZI KZ08035）, and Natural Science Foundation of Xiangtan University （No. 2011XZX09）. |
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| 摘 要： | Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The α-glucosidase inhibitory activity of these compounds was evaluated. The glucosidase inhibitory activity of all derivatives （IC50 〈 24.396 μmol]L） was higher compared with that of the reference drug, acarbose （IC50=563.601 ±40.492μmol/L）, and 1- deoxynojirimycin （IC50 = 226.912± 12.573 μmol/L）. O3＇,O7-Hexyl diosmetin （IC50 = 2.406 ± 0.101μmol/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 3＇, 4＇ and 7 of the flavonoid.
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| 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 |
| 收稿时间： | 13 March 2014 |
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