The presence of polyamines in living cells is crucial for survival. Due to their high net charge at physiological pH, polyamines effectively charge neutralize the phosphodiester backbone of DNA in an interaction that also may protect the DNA from external damage. We here present a study illustrating the influence of spermidine and spermine on the platination reactions of the model oligonucleotides d(T(6)GT(6)), d(T(12)GT(12)), and d(T(24)GT(24)), and the pUC18 DNA plasmid. The aquated forms of the anticancer active compounds cisplatin (cis-[Pt(NH(3))(2)Cl(2)]) and the major Pt(II) metabolite of JM216 (cis-[PtCl(2)(NH(3))(c-C(6)H(11)NH(2))], JM118) were used as platination reagents. The study shows that the kinetics for formation of the coordinative Pt-DNA adduct are strongly influenced by the presence of sub-millimolar polyamine concentrations. At polyamine concentrations in the muM-range, the reactions remain salt-dependent. In contrast, platination of pUC18 is effectively prevented at mM concentrations of both spermidine and spermine with the latter as the more potent inhibitor. The results suggest that variations of intracellular polyamine concentrations may have a profound influence on the efficacy by which cationically charged reagents interfere with DNA function in vivo by modulation of the preassociation conditions.

译文

:活细胞中多胺的存在对生存至关重要。由于它们在生理pH值下具有高净电荷,因此多胺在相互作用中有效地中和了DNA的磷酸二酯主链,这也可以保护DNA免受外部损害。我们在这里进行了一项研究,阐明了亚精胺和亚精胺对模型寡核苷酸d(T(6)GT(6)),d(T(12)GT(12))和d(T(24)的电镀反应的影响)GT(24))和pUC18 DNA质粒。 JM216的抗癌活性化合物顺铂(cis- [Pt(NH(3))(2)Cl(2)])和主要Pt(II)代谢产物的水合形式(cis- [PtCl(2)(NH( 3))(cC(6)H(11)NH(2)),JM118)用作电镀试剂。研究表明,亚毫摩尔多胺浓度的存在强烈影响形成配位的Pt-DNA加合物的动力学。在muM范围内的多胺浓度下,反应仍然依赖于盐。相反,在mM浓度的亚精胺和精胺中,有效抑制pUC18的电镀反应,后者是更有效的抑制剂。结果表明,细胞内多胺浓度的变化可能会对阳离子带电试剂通过调节预缔合条件在体内干扰DNA功能的功效产生深远影响。

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