Beeton Michael L, Aldrich-Wright Janice R, Bolhuis Albert
University of Bath, Department of Pharmacy and Pharmacology, Claverton Down, Bath BA2 7AY, United Kingdom.
University of Western Sydney, School of Biomedical and Health Sciences, South Penrith, Australia.
J Inorg Biochem. 2014 Nov;140:167-72. doi: 10.1016/j.jinorgbio.2014.07.012. Epub 2014 Jul 22.
Biofilm-related bacterial infections pose a significant problem, as they are generally more tolerant to antibiotics and the immune system. Development of novel compounds with antibiofilm activity is therefore paramount. In this study we have analysed metal complexes of the general structure M(IL)(AL) (where IL represents functionalised 1,10-phenanthrolines and AL represents 1S,2S- or 1R,2R-diaminocyclohexane) and Cu(IL)3. Antimicrobial activity was tested on a number of bacterial strains, showing that copper(II) compounds were active against both Gram-positive and Gram-negative bacteria, albeit that activity was generally higher for the former. The antibiofilm activity was then determined against a clinical isolate of meticillin-resistant Staphylococcus aureus (MRSA). Strikingly, the copper complexes tested showed significant activity against biofilms, and were better in the removal of biofilms than vancomycin, an antibiotic that is currently used in the treatment of MRSA infections.
生物膜相关的细菌感染是一个重大问题,因为它们通常对抗生素和免疫系统具有更强的耐受性。因此,开发具有抗生物膜活性的新型化合物至关重要。在本研究中,我们分析了一般结构为M(IL)(AL)(其中IL代表功能化的1,10 - 菲咯啉,AL代表1S,2S - 或1R,2R - 二氨基环己烷)和Cu(IL)3的金属配合物。对多种细菌菌株进行了抗菌活性测试,结果表明铜(II)化合物对革兰氏阳性菌和革兰氏阴性菌均有活性,尽管前者的活性通常更高。然后针对耐甲氧西林金黄色葡萄球菌(MRSA)的临床分离株测定了抗生物膜活性。令人惊讶的是,所测试的铜配合物对生物膜显示出显著活性,并且在去除生物膜方面比目前用于治疗MRSA感染的抗生素万古霉素效果更好。