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  

Mechanism and the structure-activity relationship of umbelliferone and aesculetin with DNA

作　　者：张爱平[1] 杨锦艳[1] 郑茂东[1] 郝娟[1] 黄茜[1] 

机构地区：[1]山西医科大学药学院,太原030001

出　　处：《中国新药杂志》2011年第1期68-74,共7页Chinese Journal of New Drugs

基　　金：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。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 measurement.Results： The mechanism of fluorescence quenching of UMB and AES with DNA were static quenching.The binding constants of UMB and AES with DNA were 2.34×104 and 5.27×102 L·mol-1,respectively.The main binding forces were hydrogen bond and van der Waals.Conclusion： Both UMB and AES interacted with calf thymus DNA in groove bindings.

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 

分 类 号：R962[医药卫生—药理学]