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Sythesis, Characterisation, Anticancer and Antimicrobial Activity of Ag-N-heterocyclic Carbene Complexes Containing Benzimidazole Derivatives

Inorganica Chimica Acta(2024)

Inonu Univ | Quaid I Azam Univ | King Saud Univ | Univ Carthage

Cited 2|Views15
Abstract
To prepare a novel series of silver(I) complexes, the interaction of benzimidazolium salts having their two nitrogen atoms substituted by bulky groups with Ag2O in DCM has been carried out. Their structures were characterized by elemental analyses, 1H NMR, 13C NMR, elemental analysis, and IR spectroscopy techniques. Further, the antimicrobial and antifungal activities properties of both the salts and their silver(I)-NHC complexes were tested against positive and negative bacteria using the Clinical and Laboratory Standards Institute (CLSI) and the European Committee for Antimicrobial Susceptibility Testing (EUCAST) respectively. The results show that silver complexes are effective against E. coli, P. aeruginosa and S. aureus bacterial species with moderate to high activity, and their minimum inhibitory concentrations ranging from 25 to 400 mu g/Ml. It was also observed that 3b compound, which has the best antifungal properties among the synthesized compounds, showed high antimicrobial activity when all bacterial species were taken into account. In addition, the salts and complexes were then evaluated for their ability to inhibit the proliferation of four different cancer cell lines (A549, MCF-7, HCT116, SH-SY5Y and BEAS-2B cells lines). AlamarBlue assay demonstrated that the salts and complexes exhibited potent cytotoxicity towards all cancer lines. 2c compound showed the highest cytotoxic activity against BEAS-2B, A549 and MCF-7 cell lines. Except for 2c, compounds 3d, 3e and 3f showed cytotoxic activity at the lowest concentrations against MCF7 cell line.The study highlights the importance of N-heterocyclic carbene ligands in the development of silver-based drugs with anticancer properties.
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N -Heterocyclic carbene,Silver(I) -NHC complexes,Antimicrobial activity,Anticancer activity
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要点】:该论文合成了含有苯并咪唑衍生物的银-N-杂环卡宾配合物,并研究了其抗肿瘤和抗微生物活性。创新点在于通过有机银化合物和银氧化物在有机溶剂中的反应,成功合成了这些配合物,并证实了它们对多种癌症细胞和细菌、真菌具有显著的抑制作用。

方法】:采用苯并咪唑ium盐与Ag2O在DCM中反应的方法制备银-N-杂环卡宾配合物,并用元素分析、1H NMR、13C NMR、IR光谱等技术对其结构进行表征。

实验】:使用临床与实验室标准研究所(CLSI)和欧洲抗微生物敏感性测试委员会(EUCAST)的方法,测试了盐及其银(I)-NHC配合物对阳性及阴性细菌的抗微生物活性。结果显示,这些配合物对E. coli、P. aeruginosa和S. aureus等细菌具有中到高的活性,最小抑制浓度范围从25到400微克/毫升。此外,通过AlamarBlue试验发现这些盐和配合物对四种不同的癌症细胞系(A549、MCF-7、HCT116、SH-SY5Y和BEAS-2B细胞系)具有显著的细胞毒性,其中2c化合物对BEAS-2B、A549和MCF-7细胞系表现出最高的细胞毒性,而3d、3e和3f化合物在较低浓度下对MCF7细胞系也显示出细胞毒性。该研究突显了N-杂环卡宾配体在银基药物抗肿瘤属性开发中的重要性。