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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。
Under physiological acidity (pH 7.4), fluorescence spectra, ultraviolet spectroscopy combined with ethidium bromide (EB) fluorescent probe, I-effect, ionic strength and DNA denaturation effect were used to study the effects of self- Interactions between novel antitumor prodrugs of Ti (Ⅳ) and DNA. Prodrugs can greatly quench the fluorescence of the ethidium bromide (EB) -DNA system, and the maximum absorption peak at 280 nm of the electron absorption spectrum results in significant redshift and subtractive effects after addition of DNA. It was also found that the fluorescence quenching efficiency of KI on the prodrug-DNA system was significantly lower than that of the free-form prodrugs. These experimental results indicate that prodrugs act on the nucleophilic sites of DNA by intercalation.