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A Tale of Two Ends: Repurposing Metallic Compounds from Anti-Tumour Agents to Effective Antibacterial Activity

机译:两个目的的故事:将来自抗肿瘤剂的金属化合物重新应用于有效的抗菌活性

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摘要

The rise in antibiotic resistance coupled with the gap in the discovery of active molecules has driven the need for more effective antimicrobials while focusing the attention into the repurpose of already existing drugs. Here, we evaluated the potential antibacterial activity of one cobalt and two zinc metallic compounds previously reported as having anticancer properties. Compounds were tested against a range of Gram-positive and -negative bacteria. The determination of the minimum inhibitory and bactericidal concentrations (MIC/MBC) of the drugs were used to assess their potential antibacterial activity and their effect on bacterial growth. Motility assays were conducted by exposing the bacteria to sub-MIC of each of the compounds. The effect of sub-MIC of the compounds on the membrane permeability was measured by ethidium bromide (EtBr) accumulation assay. Cell viability assays were performed in human cells. Compound TS262 was the most active against the range of bacteria tested. No effect was observed on the motility or accumulation of EtBr for any of the bacteria tested. Cell viability assays demonstrated that the compounds showed a decrease in cell viability at the MIC. These results are promising, and further studies on these compounds can lead to the development of new effective antimicrobials.
机译:抗生素抗药性的提高以及活性分子发现的空白推动了对更有效抗菌剂的需求,同时将注意力集中在已经存在的药物的再利用上。在这里,我们评估了一种钴和两种锌金属化合物的潜在抗菌活性,先前报道它们具有抗癌特性。针对多种革兰氏阳性和阴性细菌对化合物进行了测试。测定药物的最小抑菌和杀菌浓度(MIC / MBC)用于评估其潜在的抗菌活性及其对细菌生长的影响。通过将细菌暴露于每种化合物的亚MIC下进行运动分析。通过溴化乙锭(EtBr)积累测定法测量化合物的亚MIC对膜渗透性的影响。在人细胞中进行细胞活力测定。化合物TS262对测试的细菌范围最有活性。对于任何测试的细菌,未观察到对EtBr的运动性或累积的影响。细胞活力测定表明,化合物在MIC处显示细胞活力降低。这些结果是有希望的,并且对这些化合物的进一步研究可以导致开发新的有效抗菌剂。

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