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首页> 外文期刊>Journal of Pharmaceutical Analysis >DNA-binding studies of valrubicin as a chemotherapy drug using spectroscopy and electrochemical techniques
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DNA-binding studies of valrubicin as a chemotherapy drug using spectroscopy and electrochemical techniques

机译:使用光谱学和电化学技术研究缬沙星作为化疗药物的DNA结合

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In this study, the molecular interactions between valrubicin, an anticancer drug, and fish sperm DNA have been studied in phosphate buffer solution (pH 7.4) using UV–Vis spectrophotometry and cyclic voltammetry techniques. Valrubicin intercalated into double stranded DNA under a weak displacement reaction with methylene blue (MB) molecule in a competitive reaction. The binding constant ( k b ) of valrubicin-DNA was determined as 1.75×10 3 L/mol by spectrophotometric titration. The value of non-electrostatic binding constant ( k t 0 ) was almost constant at different ionic strengths while the ratio of k t 0 / k b increased from 4.51% to 23.77%. These results indicate that valrubicin binds to ds-DNA via electrostatic and intercalation modes. Thermodynamic parameters including ΔH 0 , ΔS 0 and ΔG 0 for valrubicin-DNA interaction were determined as ?25.21×10 3 kJ/mol, 1.55×10 2 kJ/mol K and ?22.03 kJ/mol, respectively. Cyclic voltammetry study shows a pair of redox peaks for valrubicin at 0.45 V and 0.36 V (vs. Ag/AgCl). The peak currents decreased and peak positions shifted to positive direction in the presence of DNA, showing intercalation mechanism due to the variation in formal potential. Graphical abstract Display Omitted.
机译:在这项研究中,已使用紫外可见分光光度法和循环伏安法研究了磷酸盐缓冲溶液(pH 7.4)中抗癌药缬沙星与鱼精DNA的分子相互作用。在竞争性反应中,在与亚甲基蓝(MB)分子的弱置换反应下,Valrubicin插入双链DNA。通过分光光度滴定法测定的Valrubicin-DNA的结合常数(k b)为1.75×10 3 L / mol。在不同离子强度下,非静电结合常数(k t 0)的值几乎恒定,而k t 0 / k b的比率从4.51%增加到23.77%。这些结果表明,Valrubicin通过静电和嵌入模式与ds-DNA结合。测定缬草霉素-DNA相互作用的热力学参数包括ΔH0,ΔS0和ΔG0,分别为Δ25.21×10 3 kJ / mol,1.55×10 2 kJ / mol K和Δ22.03kJ / mol。循环伏安法研究显示,在0.45 V和0.36 V下(相对于Ag / AgCl),有一对valrubicin的氧化还原峰。在存在DNA的情况下,峰值电流降低,并且峰位置向正方向移动,这表明由于形式势的变化而引起的嵌入机制。图形抽象显示被忽略。

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