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Ruthenium polypyridine complexes containing prenyl groups as antibacterial agents against Staphylococcus aureus through a membrane-disruption mechanism
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2023-07-08 , DOI: 10.1002/ardp.202300175 Runbin Wang 1 , Xiaomin Zhou 2 , Jingjing Chen 1 , Yushou Chen 1 , Yanshi Xiong 1 , Xuemin Duan 1 , Xiangwen Liao 1 , Jintao Wang 1
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2023-07-08 , DOI: 10.1002/ardp.202300175 Runbin Wang 1 , Xiaomin Zhou 2 , Jingjing Chen 1 , Yushou Chen 1 , Yanshi Xiong 1 , Xuemin Duan 1 , Xiangwen Liao 1 , Jintao Wang 1
Affiliation
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Four new ruthenium polypyridyl complexes with prenyl groups, [Ru(bpy)2(MHIP)](PF6)2 (Ru(II)-1), [Ru(dtb)2(MHIP)](PF6)2 (Ru(II)-2), [Ru(dmb)2(MHIP)](PF6)2 (Ru(II)-3), and [Ru(dmob)2(MHIP)](PF6)2 (Ru(II)-4) (bpy = 2,2′-bipyridine, dtb = 4,4′-di-tert-butyl-2,2′-bipyridine, dmb = 4,4′-dimethyl-2,2′-bipyridine, dmob = 4,4′-dimethoxy-2,2′-bipyridine, and MHIP = 2-(2,6-dimethylhepta-1,5-dien-1-yl)−1H-imidazo[4,f][1,10]phenanthroline), were synthesized and characterized. Their antibacterial activities against Staphylococcus aureus were assessed, and the minimum inhibition concentration (MIC) value of Ru(II)-2 against S. aureus was only 0.5 µg/mL, showing the best antibacterial activity among them. S. aureus could be quickly killed by Ru(II)-2 in 30 min and Ru(II)-2 displayed an obvious inhibitive effect on the formation of a biofilm, which was essential to avoid the development of drug-resistance. Meanwhile, Ru(II)-2 exhibited a stable MIC value against antibiotic-resistant bacteria. The antibacterial mechanism of Ru(II)-2 was probably related to depolarization of the cell membrane, and a change of permeability was associated with the formation of reactive oxygen species, leading to leakage of nucleic acid and bacterial death. Furthermore, Ru(II)-2 hardly showed toxicity to mammalian cells and the Galleria mellonella worm. Finally, murine infection studies also illustrated that Ru(II)-2 was highly effective against S. aureus in vivo.
中文翻译：
含有异戊二烯基团的钌聚吡啶复合物通过膜破坏机制作为抗菌剂对抗金黄色葡萄球菌
四种新的异戊烯基钌聚吡啶配合物，[Ru(bpy) 2 (MHIP)](PF 6 ) 2 (Ru(II)- 1 )、[Ru(dtb) 2 (MHIP)](PF 6 ) 2 (Ru (II)- 2 )、[Ru(dmb) 2 (MHIP)](PF 6 ) 2 (Ru(II)- 3 ) 和 [Ru(dmob) 2 (MHIP)](PF 6 ) 2 (Ru( II)- 4 ) (bpy = 2,2′-联吡啶，dtb = 4,4′-二叔丁基-2,2′-联吡啶，dmb = 4,4′-二甲基-2,2′-联吡啶, dmob = 4,4′-二甲氧基-2,2′-联吡啶，MHIP = 2-(2,6-二甲基庚-1,5-二烯-1-基)−1 H-咪唑并[4, f ][ 1,10]菲咯啉），进行了合成和表征。评估其对金黄色葡萄球菌的抗菌活性，Ru(II) -2对金黄色葡萄球菌的最低抑制浓度(MIC)仅为0.5 µg/mL，抗菌活性最好。Ru(II) -2可在30分钟内快速杀死金黄色葡萄球菌，且Ru(II)-2对生物膜的形成具有明显的抑制作用，这对于避免耐药性的产生至关重要。同时，Ru(II)-2对抗生素耐药菌表现出稳定的MIC值。Ru(II) -2的抗菌机制可能与细胞膜的去极化有关，通透性的变化与活性氧的形成有关，导致核酸泄漏和细菌死亡。此外，Ru(II)-2对哺乳动物细胞和大蜡螟几乎没有表现出毒性。最后，小鼠感染研究还表明，Ru(II) -2在体内对金黄色葡萄球菌非常有效。
更新日期：2023-07-08
中文翻译：
含有异戊二烯基团的钌聚吡啶复合物通过膜破坏机制作为抗菌剂对抗金黄色葡萄球菌
四种新的异戊烯基钌聚吡啶配合物，[Ru(bpy) 2 (MHIP)](PF 6 ) 2 (Ru(II)- 1 )、[Ru(dtb) 2 (MHIP)](PF 6 ) 2 (Ru (II)- 2 )、[Ru(dmb) 2 (MHIP)](PF 6 ) 2 (Ru(II)- 3 ) 和 [Ru(dmob) 2 (MHIP)](PF 6 ) 2 (Ru( II)- 4 ) (bpy = 2,2′-联吡啶，dtb = 4,4′-二叔丁基-2,2′-联吡啶，dmb = 4,4′-二甲基-2,2′-联吡啶, dmob = 4,4′-二甲氧基-2,2′-联吡啶，MHIP = 2-(2,6-二甲基庚-1,5-二烯-1-基)−1 H-咪唑并[4, f ][ 1,10]菲咯啉），进行了合成和表征。评估其对金黄色葡萄球菌的抗菌活性，Ru(II) -2对金黄色葡萄球菌的最低抑制浓度(MIC)仅为0.5 µg/mL，抗菌活性最好。Ru(II) -2可在30分钟内快速杀死金黄色葡萄球菌，且Ru(II)-2对生物膜的形成具有明显的抑制作用，这对于避免耐药性的产生至关重要。同时，Ru(II)-2对抗生素耐药菌表现出稳定的MIC值。Ru(II) -2的抗菌机制可能与细胞膜的去极化有关，通透性的变化与活性氧的形成有关，导致核酸泄漏和细菌死亡。此外，Ru(II)-2对哺乳动物细胞和大蜡螟几乎没有表现出毒性。最后，小鼠感染研究还表明，Ru(II) -2在体内对金黄色葡萄球菌非常有效。
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