用生物质谱方法研究抗肿瘤双β-咔啉与DNA及核苷酸的非共价结合  

Bio-MS Studies of Non-covalent Interaction of Bis-β-carbolines Towards DNA and Nucleotides

作　　者：董肖椿[1] 胥颖[1,2] Carlos AFONSO 蒋为群[1] Jean-Claude TABET 闻韧[1] 

机构地区：[1]复旦大学药学院药物化学教研室,上海200032 [2]法国巴黎第六大学生物活性分子合成、结构和功能实验室,UMR7613,巴黎75252

出　　处：《高等学校化学学报》2008年第8期1578-1582,共5页Chemical Journal of Chinese Universities

基　　金：上海市卫生局青年科研基金(批准号:2006Y14)资助

摘　　要：利用电喷雾傅里叶变换离子回旋共振质谱研究一系列双β-咔啉化合物与DNA的非共价结合。发现化合物1—5与5种不同序列的12-mer双链DNA均有明显的非共价结合，并且有两个β-咔啉环之间连接碳链的长度对此类化合物与双链DNA的非共价结合活性有明显影响．同时对此类化合物对于DNA非共价结合的序列选择性进行了讨论．另外还利用电喷雾离子阱质谱研究了双β-咔啉化合物2和4与4种单核苷酸的非共价结合．The non-covalent complexes of five bis-β-carbolines alkaloids with five different double-stranded oligodeoxynucleotides were investigated via electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry. These five antitumor compounds all showed DNA binding abilities. The binding affinities in the order of 2 〉 3,4 〉 5,1 were obtained, which mean that the length of the linkage chain between two β- carbolines has a remarkable effect on the formation of the non-covalent complexes. The competition binding experiments results were almost the same as that determined by relative ion abundances. The structure-activity relationships and sequence selectivity were discussed. The non-covalent bindings between the bis-β-carbolines 2, 4 and the nucleotide were then investigated by ESI-MS.

关 键 词：双β-咔啉 DNA 核苷酸 非共价结合 电喷雾傅里叶变换离子回旋共振质谱 

分 类 号：O629[理学—有机化学] R914[理学—化学]