高等学校化学学报 ›› 1995, Vol. 16 ›› Issue (7): 1075.

• 研究简报 • 上一篇    下一篇

米托蒽醌与生物大分子DNA结合平衡的研究

杨频1, 杨斌盛2, 王宏飞1   

  1. 1. 山西大学分子科学研究所, 太原, 030006;
    2. 南京大学化学系
  • 收稿日期:1994-07-20 修回日期:1994-12-07 出版日期:1995-07-24 发布日期:1995-07-24
  • 通讯作者: 杨频,男,60岁,教授.
  • 作者简介:杨频,男,60岁,教授.
  • 基金资助:

    国家自然科学基金

The Binding Equilibrium of Mitoxantrone and Deoxyribonuleic Acids

YANG Pin1, WANG Hong-Fei2, YANG Bin-Sheng1   

  1. 1. Molecular Science Institute of Shanxi University, Taiyuan, 030006;
    2. Dept. of Chem. Nanjing Univ.
  • Received:1994-07-20 Revised:1994-12-07 Online:1995-07-24 Published:1995-07-24

摘要: 米托蒽醌(MX)是一个广谱高效的葸醌类抗癌新药(下式),核酸是该类药物的主要细胞作用靶位,它通过与DNA结合,影响DNA的转译和复制,从而起到抗癌作用。研究这类药物与核酸的作用对于阐明抗癌机理具有重要意义,为此,广泛地开展了这方面的研究。

关键词: 米托蒽醌, DNA, 结合平衡, McGhee和VonHippel方程

Abstract: Interaction of mitoxantrone and deoxyribonuleic acids was studied at different phosphate/drug ratios(P/D), and it was found that there are two types of binding processes and interaction models. In a certain range of P/D, one type of model is dominant. At P/D <3, MX leads to condensation of DNA. At higher P/Dratio, MX intercalate into DNA, leading to red-shift of absorption spectra. At P/D>6, MX and DNA are in the binding e-qulibrium, the equilibrium binding constant of MX and calf thymus DNA is 9. 0×105(mol/L)-1at 20℃, and the binding site size n is 5. The results indicate that major groove and minor groove may be the most favorable binding sites in the structures of double stranded nucleic acids. There existed anticooperative effects between the binding sites.

Key words: Mitoxantrone, DNA, Binding equilibrium, McGhee and Von Hippel equation

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