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An Alkynyl-Dangling Ru(II) Polypyridine Complex for Targeted Antimicrobial Photodynamic Therapy
Authors:Yao Jian  Zhihui Jin  Shuang Qi  Xuwen Da  Zhanhua Wang  Prof Xuesong Wang  Dr Qianxiong Zhou
Institution:1. Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing, 100190 P. R. China

University of Chinese Academy of Sciences, Beijing, 100049 P. R. China;2. Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing, 100190 P. R. China

Abstract:To realize clinical application of antibacterial photodynamic therapy (aPDT), one of the most arduous challenges is how to render aPDT agents high selectivity against bacterial pathogens. In light of the fact that amino group-containing lipids are rich on the outer surfaces of Gram-positive bacteria, we herein constructed an alkynyl-dangling ruthenium(II) polypyridine complex (Ru2) to preferentially label Staphylococcus aureus (S. aureus) and methicillin-resistant Staphylococcus aureus (MRSA) over mammalian cells via the amino-yne bio-orthogonal click reaction. Thanks to the strong singlet oxygen generation ability, Ru2 could photo-inactivate S. aureus and MRSA effectively and specifically. Phosphatidylethanolamine (PE) molecules also exist in mammalian cells but are not accessible for Ru2, leading to its poor binding/uptake and negligible cytotoxicity in the dark and upon irradiation towards mammalian cells as well as low hemolysis, all favorable for aPDT application.
Keywords:amino-yne click reaction  antibacterial photodynamic therapy  methicillin-resistant Staphylococcus aureus  ruthenium(II) polypyridyl complexes  Staphylococcus aureus
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