Department of Chemistry, Universidad de los Andes, Carrera 1 No. 18A-12, Bogotá 111711, Colombia.
Eléctrica y Electrónica, Centro de Microelectrónica, Universidad de Los Andes, Carrera 1 No. 18A-12, Bogotá 111711, Colombia.
Molecules. 2018 Feb 8;23(2):361. doi: 10.3390/molecules23020361.
Growing antimicrobial resistance is considered a potential threat for human health security by health organizations, such as the WHO, CDC and FDA, pointing to MRSA as an example. New antibacterial drugs and complex derivatives are needed to combat the development of bacterial resistance. Six new copper and cobalt complexes of azole derivatives were synthesized and isolated as air-stable solids and characterized by melting point analyses, elemental analyses, thermogravimetric analyses (TGA), and infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that the complexes had 1:1 (M:L) stoichiometries and tetrahedral geometries, the latter being supported by DFT calculations. The antibacterial activities of the metal complexes by themselves and combined with silver nanoparticles (AgNPs; 2 μg mL) were assessed in vitro by broth microdilution assays against eight bacterial strains of clinical relevance. The results showed that the complexes alone exhibited moderate antibacterial activities. However, when the metal complexes were combined with AgNPs, their antibacterial activities increased (up to 10-fold in the case of complex ), while human cell viabilities were maintained. The minimum inhibitory concentration (MIC) values were in the range of 25-500 μg mL. This study thus presents novel approaches for the design of materials for fighting bacterial resistance. The use of azole complexes combined with AgNPs provides a new alternative against bacterial infections, especially when current treatments are associated with the rapid development of antibiotic resistance.
日益增长的抗生素耐药性被世界卫生组织(WHO)、疾病控制与预防中心(CDC)和食品药品监督管理局(FDA)等健康组织视为对人类健康安全的潜在威胁,其中耐甲氧西林金黄色葡萄球菌(MRSA)就是一个例子。需要新型的抗菌药物和复杂的衍生物来对抗细菌耐药性的发展。本文合成并分离了六种新的唑类衍生物的铜钴配合物,作为稳定的固体,通过熔点分析、元素分析、热重分析(TGA)以及红外和紫外/可见光谱进行了表征。分析和光谱数据表明,这些配合物具有 1:1(M:L)的化学计量比和四面体几何形状,后者得到了密度泛函理论(DFT)计算的支持。通过肉汤微量稀释法评估了金属配合物本身以及与银纳米颗粒(AgNPs;2 μg mL)联合使用对 8 株临床相关细菌菌株的体外抗菌活性。结果表明,单独的配合物表现出中等的抗菌活性。然而,当金属配合物与 AgNPs 联合使用时,它们的抗菌活性增强(在配合物的情况下增加了 10 倍),同时保持了人类细胞的活力。最低抑菌浓度(MIC)值在 25-500 μg mL 范围内。因此,本研究为对抗细菌耐药性的材料设计提供了新的方法。唑类配合物与 AgNPs 的联合使用为细菌感染提供了新的治疗选择,特别是在当前的治疗方法与抗生素耐药性的快速发展相关联的情况下。