Diseño y síntesis de complejos de polirutenio dirigidos a membranas que contienen cationes de amonio cuaternario con potencial actividad antibacteriana contra Staphylococcus aureus resistente a la meticilina (SARM)

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Subcutaneous Infection of Methicillin Resistant Staphylococcus Aureus MRSA

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Published on: February 9, 2011

Runyu Xue¹, Cunhong Luo¹, Lixin Dou¹

¹School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, China.

Journal of medicinal chemistry

|February 4, 2026

Abstract:

The escalating threat of Methicillin-resistant Staphylococcus aureus (MRSA) infections seriously endangers human health, so facing the immense threat of drug-resistant bacteria, discovering new and potent antibacterial drugs less prone to inducing resistance is urgently needed. In this study, four amphiphilic ruthenium polypyridyl complexes were synthesized, namely [Ru(II)(bpy)₂(DIPPB)] (PF₆)₃ (Ru-1), [Ru(II)(dmb)₂(DIPPB)] (PF₆)₃ (Ru-2), [Ru(II)(dmob)₂(DIPPB)] (PF₆)₃ (Ru-3) and [Ru(II)(bpy)₂(DIPPB)] (PF₆)₃ (Ru-4). Among these complexes, complex Ru-4 incorporates N-methylimidazole and quaternary ammonium cations, in vitro experiments have demonstrated the presence of potent antibacterial activity against Staphylococcus aureus and MRSA, accompanied by low hemolytic activity and a diminished tendency to induce drug resistance. It acts by disrupting bacterial membranes via interaction with phosphatidylglycerol and phosphatidylethanolamine, increasing permeability, elevating ROS levels, and causing content leakage. Transcriptomics confirmed its impact on membrane-related genes. Notably, in vivo experimental results demonstrated that Ru-4 exhibits superior efficacy compared to vancomycin, thereby identifying it as a promising therapeutic candidate for MRSA infection treatment.

Palabras clave:

complejos de rutenio cationes de amonio cuaternario actividad antibacteriana SARM disrupción de membranas resistencia a los medicamentos

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