Rationally designed curcumin based ruthenium(ii) antimicrobials effective against drug-resistant Staphylococcus aureus†

IF 3.3 3区化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR

Dalton Transactions Pub Date : 2019-06-19 DOI:10.1039/C9DT01650C

Payal Srivastava, Manjulika Shukla, Grace Kaul, Sidharth Chopra and Ashis K. Patra

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引用次数: 27

Abstract

Two new curcumin containing octahedral ruthenium(II) polypyridyl complexes, viz. [Ru(NN)₂(cur)](PF₆) [NN = bpy (1), phen (2)], were designed to explore the antimicrobial activity against ESKAPE pathogens, especially with the Gram-positive drug resistant S. aureus. Solid-state structural characterization by single-crystal X-ray crystallography shows the Ru^II-center in a distorted octahedral {RuN₄O₂} geometry. The tested compounds showed significant inhibitory activity and high selectivity (MIC = 1 μg mL^?1, SI = 80) against a wide variety of methicillin and vancomycin-resistant S. aureus strains. Compound 1 exhibited strong anti-biofilm activity (48% reduction of biofilm) at 10× MIC compared to the other approved drugs. The murine model of Staphylococcus infection significantly reduced the mean bacterial counts when treated with complex 1 compared to vancomycin, demonstrating its antimicrobial potential in vivo.

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合理设计姜黄素钌(ii)抗菌药物对耐药金黄色葡萄球菌†有效

设计了两种新的含八面体钌(II)多吡啶配合物[Ru(NN)2(cur)](PF6) [NN = bpy (1)， phen(2)]姜黄素，研究其对ESKAPE病原菌，特别是革兰氏阳性耐药金黄色葡萄球菌的抑菌活性。单晶x射线晶体学的固态结构表征表明，rui -中心呈畸变八面体{RuN4O2}几何形状。所测化合物具有显著的抑制活性和高选择性(MIC = 1 μg mL?1, SI = 80)对抗多种耐甲氧西林和万古霉素金黄色葡萄球菌菌株。与其他获批药物相比，化合物1在10倍MIC下表现出较强的抗生物膜活性(生物膜减少48%)。与万古霉素相比，在葡萄球菌感染的小鼠模型中，复合物1显著降低了平均细菌计数，证明了其在体内的抗菌潜力。

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来源期刊

Dalton Transactions 化学-无机化学与核化学

CiteScore

6.60

自引率

7.50%

发文量

1832

审稿时长

1.5 months

期刊介绍： Dalton Transactions is a journal for all areas of inorganic chemistry, which encompasses the organometallic, bioinorganic and materials chemistry of the elements, with applications including synthesis, catalysis, energy conversion/storage, electrical devices and medicine. Dalton Transactions welcomes high-quality, original submissions in all of these areas and more, where the advancement of knowledge in inorganic chemistry is significant.