Héctor Rudilla, Isabel Pérez-Guillén, Francesc Rabanal, Josep María Sierra, Teresa Vinuesa, Miguel Viñas
Author Information
Héctor Rudilla: Department of Pathology and Experimental Therapeutics, Faculty of Medicine and Health Sciences, Campus Bellvitge, University of Barcelona, Barcelona, Spain.
Isabel Pérez-Guillén: Department of Pathology and Experimental Therapeutics, Faculty of Medicine and Health Sciences, Campus Bellvitge, University of Barcelona, Barcelona, Spain.
Francesc Rabanal: Department of Inorganic and Organic Chemistry, Faculty of Chemistry, University of Barcelona, 08907 Hospitalet, Barcelona, Spain.
Josep María Sierra: Department of Pathology and Experimental Therapeutics, Faculty of Medicine and Health Sciences, Campus Bellvitge, University of Barcelona, Barcelona, Spain.
Teresa Vinuesa: Department of Pathology and Experimental Therapeutics, Faculty of Medicine and Health Sciences, Campus Bellvitge, University of Barcelona, Barcelona, Spain.
Miguel Viñas: Department of Pathology and Experimental Therapeutics, Faculty of Medicine and Health Sciences, Campus Bellvitge, University of Barcelona, Barcelona, Spain.
Background: Staphylococcus aureus, including 'superbug' MRSA, is a major cause of nosocomial infections. In the European Union, up to 171 200 new nosocomial MRSA infections are acquired annually, and in the USA S. aureus causes more deaths than HIV/AIDS and tuberculosis combined. MRSA is also the first group of pathogens that infect the pulmonary tract in young patients with cystic fibrosis. Objectives: We describe two newly developed and synthesized colistin (polymyxin E)-inspired molecules. Methods: A collection of several isolates of S. aureus [including MRSA and vancomycin-resistant S. aureus (VRSA)] was tested. To check the antimicrobial activity, we performed time-kill curves, growth curves, biofilm eradication, toxicity and isothermal titration calorimetry. Results: Both peptides showed high antimicrobial activities (MIC 4 mg/L) and low relative toxicities (selectivity index close to 23). Conclusions: Successful production of polymyxin-scaffold molecules active against S. aureus, both MRSA and VRSA, opens up new approaches to the treatment of these complicated infections.
