顺铂、碳铂与鸟苷、L-蛋氨酸反应动力学比较研究  

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

作　　者：丁道远[1] 胡皆汉[1] 杨志勇[1] 

机构地区：[1]中国科学院大连化学物理研究所

出　　处：《应用化学》1992年第3期114-117,共4页Chinese Journal of Applied Chemistry

摘　　要：自发现顺铂具有抗癌活性以来,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,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。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 k_2 is much greater than its first one k_1.For reactions of CDDP and CBDCA with L-Met the second rate constants are measured as 36.1×10^(-3) and 5.0×10^(-3)M^(-1)S^(-1), respectively. This may be one of the reasons that CBDCA shows less nephrotoxicity than CBDP.

关 键 词：顺铂 碳铂 鸟苷 L-蛋氨酸 

分 类 号：R914.4[医药卫生—药物化学]