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

作　　者：Ning Cheng Wen-Bin Yi Qi-Qin Wang Sheng-Ming Peng Xiao-Qing Zou 

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

出　　处：《Chinese Chemical Letters》2014年第7期1094-1098,共5页中国化学快报（英文版）

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 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.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.

关 键 词：DERIVATIVES Flavonoid Α-GLUCOSIDASE INHIBITION 

分 类 号：TQ463[化学工程—制药化工]