中华医学超声杂志

应用化学 ›› 1992, Vol. 0 ›› Issue (3): 114-117.

• 研究简报 • 上一篇    

顺铂、碳铂与鸟苷、L-蛋氨酸反应动力学比较研究

丁道远, 胡皆汉, 杨志勇   

  1. 中国科学院大连化学物理研究所, 大连 116012
  • 收稿日期:1991-03-05 修回日期:1992-01-27 出版日期:1992-06-10 发布日期:1992-06-10

REACTION KINETICS OF CDDP,CBDCA WITH GUANOSINE AND L-Met

Ding Daoyuan, Hu Jiehan, Yang Zhiyong   

  1. Dalian Institute of Chemical Physics, Academia Sinica, Dalian 116012
  • Received:1991-03-05 Revised:1992-01-27 Published:1992-06-10 Online:1992-06-10

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摘要： 自发现顺铂具有抗癌活性以来[1],人们一直致力于它的抗癌机理研究。很多结果表明顺铂与蛋白质核苷酸(DNA)作用时主要与DNA中鸟嘌呤的N7配位[2],通过形成链内交联作用造成DNA损伤。顺铂在显示抗癌活性的同时,也表现出较强的毒副作用,有文献认为毒性可能与形成Pt—S键抑制生物体内的巯基酶有关[3-4]。

关键词: 顺铂, 碳铂, 鸟苷, L-蛋氨酸, HPLC

Abstract: The reaction kinetics of CDDP (cisplatin), CEDCA (carboplatin) with guanosine and L-Met are compared by means of HPLC.The results show that the reaction rate of CDDP with Guo is greater than that with CBDCA. However, CBDCA gave more 1:2 products with Guo than 1:1 products and its second hydrolysis rate constant k2 is much greater than its first one k1.For reactions of CDDP and CBDCA with L-Met the second rate constants are measured as 36.1?10-3 and 5.0?10-3M-1S-1, respectively. This may be one of the reasons that CBDCA shows less nephrotoxicity than CBDP.

Key words: cisplatin(CDDP), carboplatin(CBDCA), guanosine, L-Met, HPLC

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