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新型钴(II)配合物与咪唑衍生物:对浮游和黏附微生物的抗菌效率和体外细胞毒性特征。

New Cobalt (II) Complexes with Imidazole Derivatives: Antimicrobial Efficiency against Planktonic and Adherent Microbes and In Vitro Cytotoxicity Features.

机构信息

Stefan S. Nicolau Institute of Virology, Romanian Academy, 030304 Bucharest, Romania.

Department of Inorganic Chemistry, Faculty of Chemistry, University of Bucharest, 90-92 Panduri Str., 050663 Bucharest, Romania.

出版信息

Molecules. 2020 Dec 24;26(1):55. doi: 10.3390/molecules26010055.

Abstract

Three novel Co(II) complexes of the type [Co(CHO)L] (where CHO is methacrylate anion; L = CHN (imidazole; HIm) (), CHN (2-methylimidazole; 2-MeIm) (), CHN (2-ethylimidazole; 2-EtIm) ()) have been synthesized and characterized by elemental analysis, IR and UV-Vis spectroscopic techniques, thermal analysis and single crystal X-ray diffraction. X-ray crystallography revealed for complexes () and () distorted trigonal bipyramid stereochemistry for Co(II), meanwhile for complex () evidenced that the unit cell comprises three molecular units with interesting structural features. In each unit, both stereochemistry adopted by metallic ion and coordination modes of carboxylate anions are different. The screening of antimicrobial activity revealed that planktonic cells were the most susceptible, with minimal inhibitory concentration (MIC) values of 7.8 μg/mL for complexes () and () and 15.6 μg/mL for complex (). Complexes () and () proved to be more active than complex () against the tested bacterial strains, both in planktonic and biofilm growth state, with MIC and minimal biofilm eradication concentration (MBEC) values ranging from 15.6 to 62.5 μg/mL, the best antibacterial effects being noticed against and . Remarkably, the MBEC values obtained for the four tested bacterial strains were either identical or even lower than the MIC ones. The cytotoxicity assay indicated that the tested complexes affected the cellular cycle of HeLa, HCT-8, and MG63 cells, probably by inhibiting the expression of vimentin and transient receptor potential canonical 1 (TRPC1). The obtained biological results recommend these complexes as potential candidates for the development of novel anti-biofilm agents.

摘要

三种新型 Co(II) 配合物[Co(CHO)L](其中 CHO 是甲基丙烯酸盐阴离子;L = CHN(咪唑;HIm)(),CHN(2-甲基咪唑;2-MeIm)(),CHN(2-乙基咪唑;2-EtIm)())已被合成并通过元素分析、IR 和 UV-Vis 光谱技术、热分析和单晶 X 射线衍射进行了表征。X 射线晶体学表明,对于配合物()和(),Co(II) 具有扭曲的三角双锥立体化学,而对于配合物(),表明该单元包含三个具有有趣结构特征的分子单元。在每个单元中,金属离子采用的两种立体化学和羧酸盐阴离子的配位模式均不同。抗菌活性筛选表明,浮游细胞最易受影响,配合物()和()的最小抑菌浓度(MIC)值为 7.8 μg/mL,配合物()的 MIC 值为 15.6 μg/mL。配合物()和()对测试的细菌菌株比配合物()更具活性,无论是在浮游和生物膜生长状态下,MIC 和最小生物膜清除浓度(MBEC)值范围从 15.6 到 62.5 μg/mL,对和的抗菌效果最好。值得注意的是,对于四种测试的细菌菌株,MBEC 值要么与 MIC 值相同,要么甚至更低。细胞毒性测定表明,测试的配合物影响 HeLa、HCT-8 和 MG63 细胞的细胞周期,可能通过抑制波形蛋白和瞬时受体电位经典通道 1(TRPC1)的表达。所获得的生物学结果表明,这些配合物可作为开发新型抗生物膜剂的潜在候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/275f/7796409/cd22fd92d672/molecules-26-00055-g001.jpg

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