[某些氯乙基甲基芳胺对DNA的烷基化动力学特征及DNA中烷基化碱基的消除]

[Kinetic characteristics of DNA alkylation with some chloroethylmethylarylamines and elimination of alkylated bases from DNA].

作者信息

Grineva N I, Myzina S D

出版信息

Mol Biol (Mosk). 1975 Jul-Aug;9(4):502-8.

Abstract

Kinetics of DNA alkylation with 2',3'-o-[N-2-chloroethyl-N-methylamino)benzylidene]uridine (UCHRCL), uridine-5'-methylphosphate (MepUCHRCL) and 4-(N-2-chloroethyl-N-methylamino)benzylamine (NH2CH2RCl) and kinetics of elimination of alkylated bases have been studied. Efficiency of DNA alkylation (p/s-ratio of rate constant of alkylation to the sum of rate constants of by-reactions of an active intermediate formed from the reagent) increases with an increase of the positive charge of the reagents as well as efficiency of tRNA alkylation. Alkylated bases are eliminated from DNA; rate of elimination depends on the structure of the reagent; it decreases in the series NH2CH2R- greater than greater than UCHR-greater than MepUCHR-. Bases alkylated by NH2CH2RCl and UCHRCl are eliminated from DNA during alkylation; therefore plots of DNA alkylation by NH2CH2RCl have a maximum. DNA alkylated by MepUCHRCl is rather stable; alkylated bases are not eliminated during alkylation. Effect of temperature and pH on elimination has been studied.

摘要

研究了用2',3'-O-[(N-2-氯乙基-N-甲氨基)亚苄基]尿苷（UCHRCL）、尿苷-5'-甲基磷酸酯（MepUCHRCL）和4-(N-2-氯乙基-N-甲氨基)苄胺（NH2CH2RCl）进行DNA烷基化的动力学以及烷基化碱基的消除动力学。DNA烷基化效率（烷基化速率常数与由试剂形成的活性中间体副反应速率常数之和的p/s比）随着试剂正电荷的增加以及tRNA烷基化效率的增加而提高。烷基化碱基从DNA中消除；消除速率取决于试剂的结构；在NH2CH2R- >> UCHR- >> MepUCHR-系列中降低。被NH2CH2RCl和UCHRCl烷基化的碱基在烷基化过程中从DNA中消除；因此，NH2CH2RCl对DNA烷基化的曲线有一个最大值。被MepUCHRCl烷基化的DNA相当稳定；烷基化碱基在烷基化过程中不被消除。研究了温度和pH对消除的影响。