Sun Weize, Boerhan Rena, Tian Na, Feng Yang, Lu Jian, Wang Xuesong, Zhou Qianxiong
Key Laboratory of Photochemical Conversion and Optoelectronic Materials, 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.
RSC Adv. 2020 Jul 3;10(42):25364-25369. doi: 10.1039/d0ra01806f. eCollection 2020 Jun 29.
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-:2',3'-]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 (MRSA), vancomycin-resistant (VRE), and () 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.
研究了氟化作用对含光不稳定配体的钌(II)配合物光活化抗菌活性的增强作用。发现含有二氟化二吡啶并[3,2 - a:2',3'- c]吩嗪(dppz)或单三氟甲基化dppz二齿配体以及四个吡啶单齿配体的钌(II)多吡啶配合物(配合物3和4)在常氧和低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)均表现出有效的光活化抗菌活性。配合物3和4在低氧条件下的杀菌作用可能源于光诱导吡啶解离后含氟的钌(II)水合物种,并且DNA可能是潜在的抗菌靶点。单线态氧敏化也可能解释了它们在常氧条件下的抗菌活性。此外,还观察到这两种配合物对人正常肝细胞(L - O2)的溶血率可忽略不计,以及低的暗毒性和光毒性。我们的工作可能为开发新型高效的基于钌(II)配合物的光活化抗菌剂以对抗耐药细菌提供新的见解。