樟脑亚胺金（I）配合物的合成与表征及其对……具有显著高抗菌活性

Synthesis and Characterization of Camphorimine Au(I) Complexes with a Remarkably High Antibacterial Activity towards and .

作者信息

Costa Joana P, Sousa Sílvia A, Soeiro Catarina, Leitão Jorge H, Galvão Adelino M, Marques Fernanda, Carvalho M Fernanda N N

机构信息

Centro de Química Estrutural e Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal.

Department of Bioengineering, iBB-Institute of Bioengineering and Biosciences, Instituto Superior Técnico, University of Lisbon, 1049-001 Lisbon, Portugal.

出版信息

Antibiotics (Basel). 2021 Oct 19;10(10):1272. doi: 10.3390/antibiotics10101272.

DOI:10.3390/antibiotics10101272

PMID:34680852

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8532832/

Abstract

Fourteen new camphorimine Au(I) complexes were synthesized and characterized by spectroscopic (NMR, FTIR) and elemental analysis. The structural arrangement of three selected examples were computed by Density Functional Theory (DFT) showing that the complexes essentially keep the {Au-CN} unit. The Minimum Inhibition Concentrations (MIC) were assessed for all complexes showing that they are active towards the Gram-negative strains ATCC25922, 477, and IST408 and the Gram-positive strain Newman. The complexes display very high activity towards 477 and IST408 with selectivity towards . An inverse correlation between the MIC values and the gold content was found for and . However, plots of MIC values and Au content for 477 and IST408 follow distinct trends. No clear relationship could be established between the MIC values and the redox potentials of the complexes measured by cyclic voltammetry. The MIC values are essentially independent of the redox potentials either cathodic or anodic. The complexes K[{Au(CN)}(L)] (, Y = m-OHCH) and K[{Au(CN)}(L)]·3HO (, Z = p-CH) display the lower MIC values for the two strains. In normal fibroblast cells, the IC values for the complexes are ca. one order of magnitude lower than their MIC values, although higher than that of the precursor KAu(CN).

摘要

合成了14种新型樟脑亚胺金（I）配合物，并通过光谱（NMR、FTIR）和元素分析对其进行了表征。通过密度泛函理论（DFT）计算了三个选定实例的结构排列，结果表明这些配合物基本上保留了{Au-CN}单元。评估了所有配合物的最低抑菌浓度（MIC），结果表明它们对革兰氏阴性菌株ATCC25922、477和IST408以及革兰氏阳性菌株纽曼具有活性。这些配合物对477和IST408显示出非常高的活性，并对……具有选择性。发现……和……的MIC值与金含量之间呈负相关。然而，477和IST408的MIC值与金含量的关系图呈现出不同的趋势。通过循环伏安法测量的配合物的MIC值与氧化还原电位之间无法建立明确的关系。MIC值基本上与阴极或阳极的氧化还原电位无关。配合物K[{Au(CN)}(L)]（……，Y = 间位-OHCH）和K[{Au(CN)}(L)]·3H₂O（……，Z = 对位-CH₃）对这两种菌株显示出较低的MIC值。在正常成纤维细胞中，这些配合物的IC值比其MIC值低约一个数量级，尽管高于前体KAu(CN)的IC值。