抗肿瘤前药物β-二酮Ti(Ⅳ)与DNA相互作用研究  

Studies on interaction of a novel anti-tumor prodrug β-diketonate Ti(Ⅳ) complex with DNA

作　　者：袁泽利[1] 杨名惠[2] 易颜丹[1] 肖苹英[1] 吴庆[1] 胡庆红[1] 张铭钦[1] 

机构地区：[1]遵义医学院药学院,遵义563003 [2]遵义医学院第一附属医院检验科,遵义563003

出　　处：《分析试验室》2012年第10期50-54,共5页Chinese Journal of Analysis Laboratory

基　　金：贵州省科学技术基金资助项目(黔科合J字[2011]2032、[2010]2223);贵州省国际合作项目(黔科合外G字[2012]7036)资助

摘　　要：在生理酸度(pH 7.4)下,采用荧光光谱、紫外光谱法并结合溴化乙锭(EB)荧光探针、I-效应、离子强度及DNA热变性效应等实验手段研究了自制的β-二酮Ti(Ⅳ)新型抗肿瘤前药与DNA之间的相互作用。前药能极大地猝灭溴化乙锭(EB)-DNA体系的荧光,其电子吸收光谱在280 nm处的最大吸收峰在加入DNA后产生明显红移和减色效应。实验还发现KI对前药-DNA体系的荧光猝灭效率明显小于自由形式存在的前药的荧光猝灭效率;这些实验结果说明前药以嵌插方式作用于DNA的亲核位点。The interaction betweend novel anti-tumor prodrug β-diketonateTi （IV） （10） ：50 -54 Complex （P-Ti） and mih DNA in physiological buffer （pH 7.4 ） was investigated by UV absorption and fluorescence spectroscopies combined with melting point effect of DNA, anion quencher KI, salt effect and using ethidium bromide （EB） as a fluorescence probe. The results showed that the prodrug could remarkably quench the fluorecence intensity of ethidium bromide （EB） - DNA system. And the red shift and hypochromie effect were observed for the absorption peak of prodrug at 280 nm, with the addition of DNA. It was also found that different ionic strength had little or no effect on the fluorescence intensity of prodrug - DNA system. At the same time, the fluorescence intensity of prodrug - DNA quenched by anionic quencher KI was much less than that of free prodrug. And the value of melting temperature of DNA increased in the presence of prodrug. Based on the above experimental results, it can be inferred that the binding mode between prodrug and milt- DNA is intercalation binding.

关 键 词：钛配合物 鱼精DNA 抗肿瘤前药 键合模式 

分 类 号：O657.3[理学—分析化学]