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喹吖因与DNA相互作用的伏安法研究。

Voltammetric studies of the interaction of quinacrine with DNA.

作者信息

Aslanoglu Mehmet, Ayne Gulay

机构信息

Department of Chemistry, Harran University, 63100 Sanliurfa, Turkey.

出版信息

Anal Bioanal Chem. 2004 Oct;380(4):658-63. doi: 10.1007/s00216-004-2797-5. Epub 2004 Aug 14.

Abstract

The binding interaction of the antimalarial drug quinacrine with herring sperm deoxyribonucleic acid (DNA) has been studied by square wave voltammetry. The binding parameters, the binding constant K and the binding site size s, were obtained simultaneously by the analysis of bound and free quinacrine concentration corresponding to the limits of slow and fast binding kinetics compared to the experimental timescale. The binding constant and the binding site size for the interaction of quinacrine with DNA were K = 1.59 (+/-0.18)x10(5) M(-1) and s = 7.1 (+/-0.15) base pairs and K = 7.35 (+/-0.83)x10(5) M(-1), s = 6.2 (+/-0.02) base pairs for the limiting conditions of static and mobile binding equilibrium respectively. The standard Gibbs free energy change (Delta G0 = - RT ln K) is approximately -29.67 kJ/mol at 25 degrees C, which highlights the spontaneity of the binding of quinacrine with DNA. The binding of quinacrine to herring sperm DNA results in peak potential shifts in voltammetric and a red shift in UV-absorption measurements. The ionic strength dependence of the binding constant is not large. Furthermore, the relative viscosity of DNA increases in the presence of quinacrine. These characteristics strongly support the intercalation of quinacrine into DNA. The results also show that the intercalation of quinacrine into DNA may occur at approximately every seventh base pair.

摘要

已通过方波伏安法研究了抗疟药物奎纳克林与鲱鱼精脱氧核糖核酸(DNA)的结合相互作用。通过分析与实验时间尺度相比的慢速和快速结合动力学极限相对应的结合态和游离奎纳克林浓度,同时获得了结合参数、结合常数K和结合位点大小s。奎纳克林与DNA相互作用的结合常数和结合位点大小,在静态和动态结合平衡的极限条件下,分别为K = 1.59(±0.18)×10⁵ M⁻¹,s = 7.1(±0.15)个碱基对和K = 7.35(±0.83)×10⁵ M⁻¹,s = 6.2(±0.02)个碱基对。在25℃时,标准吉布斯自由能变化(ΔG⁰ = -RT ln K)约为 -29.67 kJ/mol,这突出了奎纳克林与DNA结合的自发性。奎纳克林与鲱鱼精DNA的结合导致伏安法中的峰电位偏移和紫外吸收测量中的红移。结合常数对离子强度的依赖性不大。此外,在奎纳克林存在下,DNA的相对粘度增加。这些特性有力地支持了奎纳克林插入DNA。结果还表明,奎纳克林插入DNA可能大约每隔七个碱基对发生一次。

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