Fluorination in enhancing photoactivated antibacterial activity of Ru(ii) complexes with photo-labile ligands.
Fluorination in enhancing photoactivated antibacterial activity of Ru(ii) complexes with photo-labile ligands.
复制标题
氟化增强光不稳定配体 Ru(ii) 配合物的光活化抗菌活性
作者：
研究了氟化对具有光不稳定配体的Ru（ii）配合物光激活抗菌活性的增强作用。含有二氟化dppz（二吡啶[3,2-a:2 ',3 ' -c]非那嗪）或单三氟甲基化dppz双齿配体和四个吡啶单齿配体（配合物3和4）的Ru（ii）多吡啶配合物被发现在常氧和缺氧条件下对耐甲氧西林金黄色葡萄球菌（MRSA）、耐万古霉素肠球菌（VRE）和大肠杆菌（E. coli）都具有强效的光激活抗菌活性。配合物3和4在缺氧条件下的杀菌作用可能源于光诱导吡啶解离后含氟的Ru（ii）水族，DNA可能是潜在的抗菌靶点。光敏单线态氧也可以解释它们在常氧条件下的抗菌活性。此外，还观察到这两种复合物的溶血率可以忽略不计，对人类正常肝细胞（L-O2）的暗毒性和光毒性也很低。我们的工作可能为开发新型高效的Ru（ii）配合物光活化抗菌剂对抗耐药细菌提供新的见解。dppz配体中的氟化有效地增强了具有光不稳定配体的Ru（ii）配合物在常氧和缺氧条件下对耐药细菌的光激活抗菌活性。
Fluorination in enhancing photoactivated antibacterial activity of Ru(ii) complexes with photo-labile ligands was studied. Ru(ii) polypyridine complexes containing a di-fluorinated dppz (dipyrido[3,2-a:2′,3′-c]phenazine) or mono-trifluoromethylated dppz bidentate ligand and four pyridine monodentate ligands (complexes 3 and 4) were found to show potent photoactivated antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), and Escherichia coli (E. coli) in both normoxic and hypoxic conditions. The bactericidal effect of complexes 3 and 4 under hypoxic conditions may stem from the fluorine-containing Ru(ii) aqua species after photo-induced pyridine dissociation, and DNA may be the potential antibacterial target. Photosensitized singlet oxygen may also account for their antibacterial activity under normoxic conditions. Moreover, negligible hemolysis rates as well as low dark- and photo-cytotoxicity toward human normal liver cells (L-O2) were also observed for both complexes. Our work may provide new insights into the development of novel and efficient Ru(ii) complex based photoactivatable antibacterial agents against antibiotic-resistant bacteria. Fluorination in the dppz ligand efficiently enhanced the photoactivated antibacterial activity of Ru(ii) complexes with photo-labile ligands against antibiotic-resistant bacteria both under normoxic and hypoxic conditions.
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影响因子：
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