物理化学学报 >> 1999, Vol. 15 >> Issue (05): 413-419.doi: 10.3866/PKU.WHXB19990506

研究论文 上一篇    下一篇

环斑铂立体异构体与DNA的作用

李册, 王保怀, 李芝芬, 杨铭, 王夔   

  1. 北京联合大学应用文理学院，北京 100083|北京大学物理化学研究所，北京 100871|北京医科大学天然及仿生药物国家重点实验室，北京 100083
  • 收稿日期:1998-08-06 修回日期:1998-10-08 发布日期:1999-05-15
  • 通讯作者: 王保怀

The Interction between Stereoisomer of Cntharidato 1,2-cyclohexane Diamine Platinim(II)and Calf Thymus DNA

Li Ce, Wang Bao-Huai, Li Zhi-Fen, Yang Ming, Wang Kui   

  1. College of Applied Sciences and Humnities of Beijing United University,Beijing 100083|Research Lboratory of Natural and Bilmimetic Drugs,Beijing Medical University,Beijing 100083
  • Received:1998-08-06 Revised:1998-10-08 Published:1999-05-15
  • Contact: Wang Bao-Huai

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摘要：

研究了环斑铂的三种立体异构体（RSRR和SS）与小牛胸腺DNA的作用．用等温滴定量热法（ITC）测得三种化合物与DNA在298.15K时相互作用的摩尔烙变分别为-1．1，－7．2和16KJ•mol－1；差示扫描量热法（DSC）结果证实三种化合物与DNA作用使得其解链温度分别升高3.56, 7.66和8.53K；而圆二色性波谱研究（CD）则显示出在室温时三种化合物与DNA间的作用使得其摩尔椭圆度发生了不等的微弱变化；核磁共振波谱法（NMR）结果告诉我们在室温时DNA的加入未使SS-环斑铂1H谱的化学位移及峰型出现明显的改变．综合热力学及波谱实验结果，对环斑钥立体异构体与DNA作用及结合的方式进行了讨论．

关键词: 环斑铂, 小牛胸腺DNA, 嵌插作用, 沟区结合

Abstract:

 The binding of three stereoisomers of cyclocantharidatoplatin, RS, RR and SS, with calf thymus DNA was investigated by ITC, DSC, CD and NMR methods. The enthalpy changes for the binding of three stereoisomers of cyclocantharidatoplatin with DNA are - 1. 1 (RS ), - 7.2 (RR) and 16 (SS) kJ•mol - 1 at 298. 15K, respectively. In the presence of three stereoisomers of cyclocantharidatoplatin, the melting temperatures of DNA are 346. 72(RS),350. 82(RR) and 351. 69 K(SS), respectively, compared with the melting temperature 343. 16 K of DNA. The CD spectra of the DNA binding with three stereoisomers of cyclocantharidatoplatin at room temperature show a small difference of molar ellipticity between them and that of DNA. Comparing the 1H-NMR spectra of SS -cyclocantharidatoplatin in the presence of DNA with that in the absence of DNA at room temperature, there is no distinct difference between them. On the basis of the above experimental results, the binding model of cyclocantharatoplatin with DNA has been discussed.

Key words: Cyclocantharatoplatin, Calf thymus DNA, Interclation, Groove combination