不可逆电活性药物米托蒽醌与脱氧核糖核酸的相互作用  

Interaction of an Irreversible Electroactive Drug-Mitoxantrone and Deoxyribonucleic Acid

作　　者：时巧翠[1] 彭图治[1] 王素芬[1] 

机构地区：[1]浙江大学西溪校区化学系,杭州310028

出　　处：《分析化学》2003年第10期1212-1216,共5页Chinese Journal of Analytical Chemistry

基　　金：国家自然科学基金 (No .2 9975 0 2 4;2 0 2 75 0 34);浙江省自然科学基金 (No .2 0 0 0 6 1)资助课题

摘　　要：研究了抗癌新药米托蒽醌 (MXT)的电化学行为及与脱氧核糖核酸 (DNA)的相互作用 ,推导了适用于研究不可逆电活性分子与DNA相互作用的电化学公式 ,运用该公式可以简便、快速地测定靶向分子与DNA的结合常数和结合位点数。实验发现 ,MXT与小牛胸腺DNA的结合以蒽醌母核的嵌插作用为主 ,同时 ,烃氨基侧链与骨架磷酸基团之间的静电吸引对母核起稳定作用 ,使化合物易于嵌入DNA的平面结构。MXT与DNA相互作用引起的峰电流的变化可以用于分析测定DNA。The irreversible electrochemical behavior of an antineoplastic agent-mitoxantrone (MXT) and its interaction with nature calf thymus deoxyribonucleic acid (ctDNA) were investigated by cyclic voltammetry. An electrochemical equation suitable for examining the interaction of irreversible redox compounds with DNA was established. According to the equation, diffusion coefficients of both free and binding MXT (D-f, D-b), binding constant (K) and binding site size (s) of MXT with DNA were obtained simultaneously by nonlinear fit analysis of electrochemical data. The results demonstrate that MXT binds tightly to ctDNA. The anthraquinone of MXT, a planar heterocyclic ring. intercalates between the DNA's base pairs. Two aminoethylamino side-chains of the drugs fit to the minor groove and reinforce the interaction with DNA. It is possible to detect DNA concentration by the use of the current change during the interaction of MXT and DNA.

关 键 词：不可逆电活性药物 米托蒽醌 脱氧核糖核酸 嵌插结合 电化学法 

分 类 号：O657.1[理学—分析化学]