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N-杂环卡宾银（I）配合物的抗菌活性及作用方式

Antimicrobial Activity and Mode of Action of N-Heterocyclic Carbene Silver(I) Complexes.

作者信息

Castagliuolo Giusy, Di Napoli Michela, Zangmo Tshering, Szpunar Joanna, Ronga Luisa, Zanfardino Anna, Varcamonti Mario, Tesauro Diego

机构信息

Department of Biology, University of Naples "Federico II", Via Cynthia 26, 80126 Naples, Italy.

IPREM (Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et les Matériaux), CNRS, E2S UPPA, Université de Pau et des Pays de l'Adour, CEDEX 9, 64012 Pau, France.

出版信息

Molecules. 2024 Dec 28;30(1):76. doi: 10.3390/molecules30010076.

DOI:10.3390/molecules30010076
PMID:39795133
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11722542/
Abstract

Silver drugs have played a vital role in human healthcare for the treatment of infections for many centuries. Currently, due to antibiotic resistance, a potential scenario or the application of silver complexes may arise as substitutes for conventional antibiotics. In this perspective, N-heterocyclic carbene (NHC) ligands have been selected as carrier molecules for silver ions. In this study, we selected two mono NHC-silver halide complexes: bromo[1,3-diethyl-4,5-bis(4-methoxyphenyl)imidazol-2-ylidene]silver(I) (Ag4MC) and chloro[2-pyridin- N-(2-ethylacetylamido)-2-yl-2-imidazol-2-ylidene]silver(I) (Ag5MC), and two cationic bis NHC silver complexes: bis[1,3-diethyl-4,5-bis(4-methoxyphenyl)imidazol-2-ylidene]silver(I) (Ag4BC) and bis[2-pyridin-N-(2-ethylacetylamido)-2-yl-2-imidazol-2-ylidene]silver(I) (Ag5BC). The inhibitory properties of the four complexes were evaluated for their antimicrobial potential against a set of Gram (+) and Gram (-) bacterial strains and the fungus . In addition, further investigations were made using fluorescence and scanning electron microscopy (SEM) in order to gain more insights into the mechanism of action. Some preliminary information on the Ag target was obtained by analyzing the cytosol of treated with Ag5MC by size-exclusion chromatography (SEC) coupled with inductively coupled plasma mass spectrometry (ICP-MS).

摘要

几个世纪以来，含银药物在人类医疗保健中治疗感染方面发挥了至关重要的作用。目前，由于抗生素耐药性问题，银配合物作为传统抗生素的替代品可能会出现潜在的应用场景。从这个角度来看，N-杂环卡宾（NHC）配体已被选作银离子的载体分子。在本研究中，我们选择了两种单NHC-卤化银配合物：溴[1,3-二乙基-4,5-双（4-甲氧基苯基）咪唑-2-亚基]银（I）（Ag4MC）和氯[2-吡啶-N-（2-乙基乙酰氨基）-2-基-2-咪唑-2-亚基]银（I）（Ag5MC），以及两种阳离子双NHC银配合物：双[1,3-二乙基-4,5-双（4-甲氧基苯基）咪唑-2-亚基]银（I）（Ag4BC）和双[2-吡啶-N-（2-乙基乙酰氨基）-2-基-2-咪唑-2-亚基]银（I）（Ag5BC）。评估了这四种配合物对一组革兰氏阳性和革兰氏阴性细菌菌株以及真菌的抗菌潜力。此外，还使用荧光和扫描电子显微镜（SEM）进行了进一步研究，以便更深入地了解其作用机制。通过尺寸排阻色谱（SEC）结合电感耦合等离子体质谱（ICP-MS）分析用Ag5MC处理后的细胞溶质，获得了一些关于银靶点的初步信息。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/11722542/ea6fbf52a60d/molecules-30-00076-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/11722542/e1cac6409bfa/molecules-30-00076-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/11722542/c585764bb3d1/molecules-30-00076-g003.jpg
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