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7-羟基香豆素及6,7-二羟基香豆素与DNA的作用机理及构效关系研究
引用本文:张爱平,杨锦艳,郑茂东,郝娟,黄茜. 7-羟基香豆素及6,7-二羟基香豆素与DNA的作用机理及构效关系研究[J]. 中国新药杂志, 2011, 0(1)
作者姓名:张爱平  杨锦艳  郑茂东  郝娟  黄茜
作者单位:山西医科大学药学院;
基金项目:山西高校科技研究开发项目(2007122,2007125)
摘    要:目的:研究7-羟基香豆素(umbelliferone,UMB)和6,7-二羟基香豆素(aesculetin,AES)与小牛胸腺DNA的作用机制,探讨其构效关系。方法:采用荧光光谱法研究UMB和AES与DNA的结合作用,并计算相关结合参数,利用紫外光谱、盐效应、I-猝灭、与单双链DNA作用、DNA热变性温度及黏度测定等方法确定UMB和AES与DNA的作用模式。结果:DNA对UMB和AES的荧光猝灭机制均为静态猝灭;UMB和AES与DNA的结合常数分别为2.13×104和5.27×102L.mol-1,作用力主要是氢键和范德华力。结论:UMB和AES与DNA的作用方式均为沟槽作用。

关 键 词:7-羟基香豆素  6  7-二羟基香豆素  小牛胸腺DNA  紫外光谱法  荧光光谱法  黏度法  

Mechanism and the structure-activity relationship of umbelliferone and aesculetin with DNA
ZHANG Ai-ping,YANG Jin-yan,ZHENG Mao-dong,HAO Juan,HUANG Qian. Mechanism and the structure-activity relationship of umbelliferone and aesculetin with DNA[J]. Chinese Journal of New Drugs, 2011, 0(1)
Authors:ZHANG Ai-ping  YANG Jin-yan  ZHENG Mao-dong  HAO Juan  HUANG Qian
Affiliation:ZHANG Ai-ping,YANG Jin-yan,ZHENG Mao-dong,HAO Juan,HUANG Qian(School of Pharmaceutical Science,Shanxi Medical University,Taiyuan 030001,China)
Abstract:Objective: To investigate the mechanism and the structure-activity relationship of umbelliferone(UMB) and aesculetin(AES) with calf thymus DNA.Methods: Fluorescence spectroscopy was used to determine the interaction of UMB and AES with DNA and to calculate the binding parameters.The binding mode of UMB and AES with DNA were determined by UV-Vis spectra,salt effect,I-quenching effect,the comparison of single and double stranded DNA bound to UMB and AES,DNA denaturation temperature and DNA viscosity measureme...
Keywords:umbelliferone  aesculetin  calf thymus DNA  ultraviolet spectroscopy  fluorescence spectroscopy  viscosimetry  
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