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化学学报
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化学学报 ›› 2010, Vol. 68 ›› Issue (18): 1864-1870. 上一篇    下一篇

研究论文

表柔比星-铁体系与DNA作用的光谱和电化学法研究

席小莉1，杨曼曼2，杨频*,1   

  1. (1山西大学分子科学研究所 化学生物学与分子工程教育部重点实验室 太原 030006)
    (2山西大学化学化工学院 太原 030006)
  • 投稿日期:2010-04-12 修回日期:2010-05-13 发布日期:2010-05-24
  • 通讯作者: 杨频 E-mail:yangpin@sxu.edu.cn
  • 基金资助:

    金属－Aβ肽均一分布聚集体与神经细胞膜的相互作用及机理研究

Study on the Interaction between Epirubicin-Fe2＋ System and DNA by Spectroscopic and Electrochemical Methods

Xi Xiaoli1 Yang Manman2 Yang Pin*,1   

  1. (1 Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education of China at College of Chemistry and Chemical Engineering, Institute of Molecular Science, Shanxi University, Taiyuan 030006)
    (2 College of Chemistry and Chemical Engeneering, Shanxi University, Taiyuan 030006)
  • Received:2010-04-12 Revised:2010-05-13 Published:2010-05-24

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被引次数

15 | 3

表柔比星是临床上广泛用于治疗增殖很快肿瘤的药物. 应用紫外、荧光、园二色、黏度、循环伏安等方法研究了表柔比星及表柔比星-Fe2＋体系与DNA的作用. 结果发现, 在pH＝7.4时表柔比星可与Fe2＋形成稳定体系, 加入DNA后表柔比星-Fe2＋体系的紫外吸收明显降低. Scatchard图表明, 表柔比星-Fe2＋体系对溴化乙锭(EB)与DNA的结合为竞争性抑制, 同时此体系可使DNA-EB体系荧光偏振度增大, 使DNA的热变性温度(tm)上升, 黏度增大. 循环伏安法表明, DNA的加入使得表柔比星及表柔比星-Fe2＋体系的式量电位正移. 园二色谱法表明, 随着表柔比星-Fe2＋体系的加入, DNA碱基间作用能迅速减弱. 综合以上结果得出: 表柔比星及表柔比星-Fe2＋体系与DNA之间均为嵌插作用, 而且表柔比星-Fe2＋体系具有比单纯表柔比星更好的嵌插效果. 这些结果可为合理改善药效、降低抗癌药物毒性和设计新药提供依据.

关键词: 表柔比星-Fe2＋体系, 小牛胸腺DNA, Scatchard图

Epirubicin is used to treat the fast multiplication cancer. The interaction of Epirubicin-Fe2＋ system with calf thymus DNA has been investigated using UV spectra, fluorescent spectra, CD, viscosity and cyclic voltammetry etc. The results show that Epirubicin can form constant system with Fe2＋ in pH＝7.4 solution. Hypochromism was observed in the UV spectra of the system in the presence of the DNA. The Scatchard plots showed competitive inhibition aganist EB binding to DNA. The relative viscosity and thermal deformation temperature of DNA increased with addition of the Epirubicin-Fe2＋ system. The fluorescence polarization of the DNA-EB system increased with addition of the Epirubicin-Fe2＋ system. Determination of cyclic voltammetry showed that the DNA made the Epirubicin-Fe2＋ formal potential positively shift. The energy of base pair has been weakened with addition of the Epirubicin-Fe2＋ system. So it can be concluded that the binding mode of the Epirubicin-Fe2＋ system with CT DNA belongs to intercalation action. This work may be usefully applied to elucidating the mechanisms of natural nucleases and drug design.

Key words: Epirubicin-Fe2＋ system, calf thymus DNA, Scatchard plot