水溶性不对称卟啉及其金属配合物合成及与DNA的作用  

The Synthesis of Water-soluble Asymmetric Porphyrins, Their Metal Complexes and Their Interaction with CT DNA

作　　者：韩高义[1] 杨频[2] 

机构地区：[1]南京大学化学系配位化学国家重点实验室，南京210093 [2]山西大学分子科学研究所，太原030006

出　　处：《化学学报》2001年第6期925-930,共6页Acta Chimica Sinica

基　　金：国家自然科学基金，山西省自然科学基金

摘　　要：合成并表征了以三(4-N-甲基吡啶基)卟啉为母体,带有乙氧羰基甲氧基或羧基甲氧基侧链的水溶正电性卟啉及其金属配合物(M=Cu,Ni),并研究了它们与DNA的相互作用.卟啉对EB-DNA荧光猝灭研究表明:卟啉与DNA作用存在单一结合模式.EB荧光竞争法测得它们与DNA作用的结合常数介于3×105～3×106L@mol-1.电子吸收研究谱表明:DNA引起卟啉Soret带的不同程度的红移(≤9 nm)和减色(≤35%).卟啉及其金属配合物都引起DNA的熔点升高(≤2.5℃)和DNA粘度的略微下降.所有这些研究表明:这些带较长侧链的水溶性卟啉及其金属配合物与DNA作用不存在插入作用模式,只是在DNA的外部结合.(Ethoxycarbonyl)methoxy - or carboxylmethoxy - tris(methylpyridinyl) porphyrins and their metal complexes have been synthesized and characterized. AU. of them were sufficiently water - soluble for DNA binding studies. Their apparent affinity binding constant for CT DNA varied from 3 x 10(5) to 3 x 10(6) L.mol(-1) as measured by competition with EB. The porphyrins as well as their Cut II) and Nit II) derivatives decrease the viscocity of CT DNA slightly and increase the melting point of DNA by only up to 2.5 degreesC at DNA base pair/ ligand ratios of 60. The fact that DNA causes a red shift(less than or equal to9 nm) and weak hypochromic effect(less than or equal to 35%) on the soret band of porphyrins shows that all these porphyrins interact with DNA without intercalation.

关 键 词：DNA 相互作用 金属配合物 合成 抗癌药物 水溶性不对称卟啉 抗癌机理 

分 类 号：R979.1[医药卫生—药品] R963[医药卫生—药学]