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新型不饱和羧酸配合物与 2,2'-联吡啶的合成、结构表征、抗菌活性和体外生物相容性

Synthesis, Structural Characterization, Antimicrobial Activity, and In Vitro Biocompatibility of New Unsaturated Carboxylate Complexes with 2,2'-Bipyridine.

机构信息

Department of Soil Sciences, University of Agronomical Sciences and Veterinary Medicine, 59 Mărăşti Str., Sector 1, 011464 Bucharest, Romania.

Department of Microbiology, Faculty of Biology, University of Bucharest, 1-3 Aleea Portocalelor Str., 60101 Bucharest, Romania.

出版信息

Molecules. 2018 Jan 12;23(1):157. doi: 10.3390/molecules23010157.

Abstract

The synthesis, structural characterization, cytotoxicity, and antimicrobial properties of four new complexes formed by employing acrylate anion and 2,2'-bipyridine are reported herein. X-ray crystallography revealed the trinuclear nature of [Mn₃(2,2'-bipy)₂(C₃H₃O₂)₆] (), meanwhile complexes with general formula [M(2,2'-bipy)(C₃H₃O₂)₂(H₂O)]∙H₂O (() M: Ni, = 1, = 0; () M: Cu, = 1, = 0; () M: Zn, = 0, = 1; 2,2'-bipy: 2,2'-bipyridine; C₃H₃O₂: acrylate anion) were shown to be mononuclear. The lowest minimum inhibitory concentration (MIC) of 128 μg mL was recorded for all four tested complexes against , for complex () against , and for complex () against . Compounds () and () were also potent efflux pumps activity inhibitors (EPI), proving their potential for use in synergistic combinations with antibiotics. Complexes ()-() revealed that they were not cytotoxic to HCT-8 cells. They also proved to interfere with the cellular cycle of tumour HCT-8 cells by increasing the number of cells found in the S and G2/M phases. Taken together, these results demonstrate the potential of zinc and copper complexes for use in the development of novel antimicrobial and anti-proliferative agents.

摘要

本文报道了四种新配合物的合成、结构表征、细胞毒性和抗菌性能,这些配合物是由丙烯酸盐阴离子和 2,2'-联吡啶形成的。X 射线晶体学揭示了[Mn₃(2,2'-bipy)₂(C₃H₃O₂)₆]()的三聚体性质,同时具有通式[M(2,2'-bipy)(C₃H₃O₂)₂(H₂O)]∙H₂O 的配合物(() M: Ni, = 1, = 0; () M: Cu, = 1, = 0; () M: Zn, = 0, = 1; 2,2'-bipy: 2,2'-bipyridine; C₃H₃O₂: 丙烯酸盐阴离子)被证明为单核。所有四种测试配合物对 的最低最小抑菌浓度 (MIC) 均为 128 μg mL,对 () 对 ,对 () 对 。化合物 () 和 () 也是有效的外排泵活性抑制剂 (EPI),证明它们具有与抗生素协同组合使用的潜力。配合物 ()-() 表明它们对 HCT-8 细胞没有细胞毒性。它们还通过增加 S 和 G2/M 期细胞数量,证明它们可以干扰肿瘤 HCT-8 细胞的细胞周期。综上所述,这些结果表明锌和铜配合物在开发新型抗菌和抗增殖剂方面具有潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41d9/6017882/f2bde1c8a729/molecules-23-00157-g001.jpg

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