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姜黄素类似物的合成及其生物活性的测定
引用本文:李俊海,孙纲春,谢晶曦.姜黄素类似物的合成及其生物活性的测定[J].化学研究与应用,2009,21(7).
作者姓名:李俊海  孙纲春  谢晶曦
作者单位:1. 河南工业大学化学化工学院,河南,郑州,450001
2. 中国医学科学院,协和医科大学药物研究所,北京,100050
基金项目:河南工业大学引进人才资助项目 
摘    要:实验合成了姜黄素的Knoevenagel缩合物4-(2-呋喃次甲基)姜黄素C1,氨基硫脲Schiff 碱配体E1,及其Schiff 碱配体的Zn(Ⅱ)配合物D1.采用DPPH法测定了产品清除自由基的能力,结果表明产品C1对DPPH自由基清除率为82.0%.在pH7.2的Tris-Hcl缓冲溶液中,采用紫外光谱和荧光光谱研究了C1与鲱鱼精DNA的相互作用,结果表明,C1与DNA是通过嵌插模式发生相互作用的,其键合常数为Kq =9.31×103.

关 键 词:姜黄素类似物  合成  DPPH·自由基  DNA相互作用  DPPH·radical

Synthesis and bioactivities of the movel curcumin analogues
LI Jun-hai,SUN Gang-chun,XI Jing-xi.Synthesis and bioactivities of the movel curcumin analogues[J].Chemical Research and Application,2009,21(7).
Authors:LI Jun-hai  SUN Gang-chun  XI Jing-xi
Institution:1.Henan University of Technology;Zhengzhou 450001;China;2.Institute of Materia Medica;Chinese Academy of Medical Sciences and Peking Union Medical College;Beijing 100050;China
Abstract:Knoevenagel condensate 4-(2-furanmethylidyne)curcumin of curcumin C1,thiosemicarbazide Schiff base E1 and Zn(Ⅱ) complexes D1 were synthesized.The scavenging capacity of the products is studied against the DPPH radical, the results indicat that the scavenging rate of the C1 is 82.0%.The mechanism of interaction between C1 and DNA was studied by ultraviolet absorption and fluorescence spectroscopy in pH7.2 Tris-Hcl buffer.It was found that the major mode of recognition is intercalation binding between C1 and Herring Sperm DNA and the binding constant was Kq =9.31×103.
Keywords:curcumin analogues  synthesis  DNA interaction
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