基于多芳环多吡啶配体的单功能铂配合物DNA结合研究  

Research on single function of platinum complexes of polyaromatic polypyridine ligands on DNA interactions

作　　者：陈司汉[1] 周炳荣[2] 

机构地区：[1]乐山职业技术学院,四川乐山614000 [2]南京医科大学医学科学部,江苏南京210029

出　　处：《中国生化药物杂志》2015年第2期35-38,共4页Chinese Journal of Biochemical Pharmaceutics

基　　金：国家自然科学基金(81000700)

摘　　要：目的验证配体2,4,6-三[二(2-吡啶甲基)-氨甲基苯基]-1,3,5-三嗪(L4)配合物的DNA结合能力。方法合成一个多芳环多吡啶配体2,4,6-三[二(2-吡啶甲基)-氨甲基苯基]-1,3,5-三嗪(L4)。配体(L4)与Pt(DMSO)2Cl2反应得到配合物4,表征配合物,通过紫外、荧光和凝胶电泳的方法研究了配合物4的DNA结合能力。结果紫外和荧光实验表明该配合物均可与DNA嵌入结合,结合常数分别为2.1×104M-1、2.78×107M-1。凝胶电泳实验表明配合物可使DNA超螺旋形式完全解旋,有效扰乱DNA的二级结构。结论配体2,4,6-三[二(2-吡啶甲基)-氨甲基苯基]-1,3,5-三嗪(L4)配合物与DNA具有较强的结合能力,可以缓慢结合形成DNA的加合物,并且能够有效扰乱DNA构象。Objective To verify the ability of ligand 2,4,6- three [ two （2- pyridyl methyl） - aminomethyl phenyl]-1,3,5- triazine （IA） combined with DNA. Methods Synthesis of an aromatic polypyridyl ligand 2,4,6- three [ two （2- pyridyl methyl）-aminomethyl phenyl ]-1,3,5-triazine （1.4）. Complex 4 was obtained by the reaction of ligand（IA） and Pt（ DMSO）2Cl2 ,the complex 4 was characterized, electrespray mass spectroscopy. Methods by UV, fluorescence, and gel electrephoresis study of the binding ability of complex 4 and DNA. Results UV-vis experiments showed that the complexes could be combined with the embedded DNA, the binding constant was 2. 1 × 10^4M-1, EB-DNA binding experiments also showed that the complexes could be combined with embedded DNA, the calculated Kapp was 2. 78 × 10^7M-1. Gel electrophoresis experiments showed that the complexes could make DNA from the supercoiled form to complete unwinding, and two level structure effectively disrupt DNA. Gonclusion The ligand of 2,4,6- three [ two （2- pyridyl methyl） - aminomethyl phenyl ] -1,3,5- triazine （IA） complexes combine with stronger binding ability with DNA, can combine to form DNA complexes, and can effectively disrupt the conformation of DNA.

关 键 词：铂配体 DNA结合 合成 

分 类 号：R979.1[医药卫生—药品]