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杂双核配合物的合成:体外 DNA 结合、切割及抗菌研究。

Synthesis of heterobimetallic complexes: in vitro DNA binding, cleavage and antimicrobial studies.

机构信息

Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India.

出版信息

J Photochem Photobiol B. 2012 Sep 3;114:108-18. doi: 10.1016/j.jphotobiol.2012.05.017. Epub 2012 Jun 13.

DOI:10.1016/j.jphotobiol.2012.05.017
PMID:22762922
Abstract

The monometallic (1-3) and heterobimetallic (4-6) complexes, containing 1,10-phenanthroline and indole-3-acetic acid were synthesized and characterized by spectroscopic (IR, UV-vis, NMR, ESI-MS) and analytical methods. The in vitro DNA binding studies of 5 and 6 with CT DNA were carried out by employing various biophysical methods which reveal strong electrostatic binding via phosphate backbone of DNA helix. The binding constant (K) value as determined from fluorescence experiments of complexes 5 and 6 were calculated to be 4.09×10(4) and 2.51×10(4) M(-1), respectively revealing that complex 5 has greater binding propensity for DNA. To gain further insight into the molecular recognition at the target site, interaction studies of 5 with 5'-GMP were carried out by employing (1)H and (31)P NMR spectroscopy. Complex 5 exhibited preferential selectively towards the minor groove of pBR322 DNA and efficient cleavage activity via hydrolytic pathway. Furthermore complexes 4-6 exhibited significant antimicrobial activity.

摘要

合成并通过光谱(IR、UV-vis、NMR、ESI-MS)和分析方法表征了单核(1-3)和杂双核(4-6)配合物,这些配合物含有 1,10-菲啰啉和吲哚-3-乙酸。采用各种物理方法研究了 5 和 6 与 CT DNA 的体外 DNA 结合情况,结果表明它们通过 DNA 螺旋的磷酸骨架进行强静电结合。荧光实验测定配合物 5 和 6 的结合常数(K)值分别为 4.09×10(4)和 2.51×10(4)M(-1),表明配合物 5 对 DNA 具有更大的结合倾向。为了更深入地了解靶位点的分子识别,通过(1)H 和(31)P NMR 光谱研究了 5 与 5'-GMP 的相互作用。配合物 5 对 pBR322 DNA 的小沟表现出优先选择性和通过水解途径的有效切割活性。此外,配合物 4-6 表现出显著的抗菌活性。

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