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体外评价 Zn-诺氟沙星配合物作为一种有效的细胞毒性和抗菌剂,提出的 DNA 结合模型。

In vitro evaluation of Zn-norfloxacin complex as a potent cytotoxic and antibacterial agent, proposed model for DNA binding.

机构信息

Medical Chemistry, Faculty of Medicine, Kermanshah University of Medical Sciences, Kermanshah, Iran.

出版信息

Appl Biochem Biotechnol. 2013 Jun;170(4):988-1009. doi: 10.1007/s12010-013-0255-6. Epub 2013 May 1.

Abstract

A tetrahedral Zn(II) complex with the second generation fluoroquinolone, norfloxacin, was prepared and characterized (NOR-Zn complex, NZC). The antibacterial efficiency of the NZC was tested on two Gram-positive and four Gram-negative bacteria by minimum inhibitory concentration method. The cytotoxic potential of NZC on MDA (human breast adenocarcinoma), Caco-2 (human colon adenocarcinoma), and Hela (human cervix carcinoma) cell lines was studied. The DNA interaction property of the NZC has been investigated using UV-vis, fluorescence, Fourier transform infrared, as well as cyclic voltammetry methods. Intrinsic binding constant (K(b)), thermodynamic, and other spectroscopic and voltammetric data indicate that the NZC has more affinity for DNA than for norfloxacin and interacted with DNA via two modes: electrostatic and outside hydrogen binding. The proposed DNA binding mode supports the large enhancement in the cytotoxicity and antibacterial activity of NZC.

摘要

合成并表征了一种具有第二代氟喹诺酮药物(诺氟沙星)的四面体型 Zn(II) 配合物(NOR-Zn 配合物,NZC)。采用最低抑菌浓度法研究了 NZC 对两种革兰氏阳性菌和四种革兰氏阴性菌的抗菌效率。研究了 NZC 对 MDA(人乳腺癌腺癌细胞)、Caco-2(人结肠腺癌细胞)和 Hela(人宫颈癌细胞)细胞系的细胞毒性。通过紫外可见光谱法、荧光光谱法、傅里叶变换红外光谱法以及循环伏安法研究了 NZC 的 DNA 相互作用性质。内结合常数(K(b))、热力学和其他光谱学和伏安数据表明,NZC 与 DNA 的亲和力强于诺氟沙星,通过两种模式与 DNA 相互作用:静电作用和外部氢键结合。所提出的 DNA 结合模式支持 NZC 增强细胞毒性和抗菌活性。

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