以烟酰胺为配体的NAMI衍生物的水解性质和溶液稳定性研究  

Hydrolytic property and solution stability of NAMI derivative containing nicotinamide

作　　者：梁曜华[1,2,3] 毕葳[3] 闫寒[4] 梁国刚[1,2,3] 

机构地区：[1]中药质量研究国家重点实验室澳门科技大学中医药学院,澳门999078 [2]澳门科技大学澳门药物及健康应用研究所,澳门999078 [3]中国中医科学院中药研究所,北京100700 [4]中国中医科学院医学实验中心,北京100700

出　　处：《中国中药杂志》2012年第6期818-823,共6页China Journal of Chinese Materia Medica

基　　金：澳门科技发展基金项目(012/2009/A1);中国中医科学院基本科研业务费自主选题项目(ZZ03064;Z02089)

摘　　要：目的:研究配体结构对NAMI衍生物的水解、溶液稳定性的影响。方法:制备了化合物1 trans-[RuCl4(DMSO)(ni-ca)]Na.2DMSO(nica,nicotinamide烟酰胺);用紫外分光光度法研究了化合物1的水解机制,动力学及溶液稳定性。结果:与NAMI相似,化合物1在pH 7.40的缓冲液中发生2步脱氯水解反应(Ⅰ氯水解及Ⅱ氯水解);在pH 5.00缓冲液中二甲基亚砜(DM-SO)水解。测定了各水解反应表观速率常数、半衰期及溶液稳定性参数。结论:化合物1在酸性溶液中的稳定性明显高于中性溶液。用烟酰胺取代咪唑环能够明显减慢NAMI衍生物的脱氯水解反应速度,但对脱DMSO水解反应影响较小。Objective： To study the influence of ligand structure on hydrolysis and solution stability of NAMI derivatives. Method ： NAMI type compound 1, trans- [ RuC14 （DMSO） （nica） ] Na . 2DMSO （ nica, nicotinamide） were prepared. Their hydrolytic mechanism, kinetics and stability were investigated by UV-Vis spectrophotometer. Result： Similar to NAMI, compound 1 undergoes two well-separated steps chloro-hydrolysis （I chloro-hydrolysis and II chloro-hydrolysis） （step reaction） in pH 7.4 buffer solution; while dimethyl sulfoxide （DMSO） hydrolyze in pH 5.00 acetic buffer solution. The kabs and t1/2 for each hydrolytic reaction were determined. Conclusion ： The stability of compound 1 in acidic solution is much more stable than that of in neutral solution. Nicotinamide in place of imidazole can decrease chloro hydrolytic rate of NAMI derivatives obviously, while the influence on the DMSO hydrolytic process is not so remarkable.

关 键 词：钌化合物 烟酰胺 抗转移 水解动力学 稳定性 

分 类 号：R284[医药卫生—中药学]