金黄色葡萄球菌
细胞内
化学
光毒性
细胞毒性
万古霉素
抗药性
配体(生物化学)
微生物学
耐甲氧西林金黄色葡萄球菌
抗生素
细菌
生物化学
生物
受体
体外
遗传学
作者
Weize Sun,Jian Yao,Mengxue Zhou,Yishan Yao,Na Tian,Chao Li,Jun Chen,Xuesong Wang,Qianxiong Zhou
标识
DOI:10.1021/acs.jmedchem.0c02257
摘要
Novel antibacterial agents capable of efficiently sterilizing intracellular Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) but with low cytotoxicity and low resistance development are quite appealing. In this work, three Ru(II) complexes with photolabile ligands were explored to realize such a goal. Complex 3 (5 μM) can inhibit more than 90% growth of S. aureus/MRSA that has invaded in J774A.1 cells upon visible light irradiation, being much more efficient than vancomycin. In similar conditions, negligible dark- and phototoxicity were found toward the host cells. The bactericidal activity is highly correlated with DNA covalent binding by the Ru(II) fractions generated after ligand photodissociation. Moreover, S. aureus quickly developed resistance toward vancomycin, while negligible resistance toward complex 3 even after 700 generations was obtained. These appealing results may pave a new way for fighting against intracellular antibiotic-resistant pathogens.
科研通智能强力驱动
Strongly Powered by AbleSci AI