Novel synthetic polymyxins kill Gram-positive bacteria

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 a...

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Autores: Rudilla Mateo, Héctor, Pérez Guillén, Isabel, Rabanal Anglada, Francesc, Sierra Ortigosa, Josep Maria, Vinuesa Aumedes, Teresa, Viñas, Miquel
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2018
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/228138
Acceso en línea:https://hdl.handle.net/2445/228138
Access Level:acceso abierto
Palabra clave:Staphylococcus aureus
Antibiòtics pèptids
Models moleculars
Peptide antibiotics
Molecular models
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spelling Novel synthetic polymyxins kill Gram-positive bacteriaRudilla Mateo, HéctorPérez Guillén, IsabelRabanal Anglada, FrancescSierra Ortigosa, Josep MariaVinuesa Aumedes, TeresaViñas, MiquelStaphylococcus aureusAntibiòtics pèptidsModels molecularsStaphylococcus aureusPeptide antibioticsMolecular modelsBackground: 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.Oxford University Press2026202620182026info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersion32 p.application/pdfhttps://hdl.handle.net/2445/228138Articles publicats en revistes (Química Inorgànica i Orgànica)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésVersió postprint del document publicat a: https://doi.org/10.1093/jac/dky366Journal of Antimicrobial Chemotherapy, 2018, vol. 73, num.12, p. 3385-3390https://doi.org/10.1093/jac/dky366(c) Rudilla H et al., 2018info:eu-repo/semantics/openAccessoai:recercat.cat:2445/2281382026-05-29T05:05:01Z
dc.title.none.fl_str_mv Novel synthetic polymyxins kill Gram-positive bacteria
title Novel synthetic polymyxins kill Gram-positive bacteria
spellingShingle Novel synthetic polymyxins kill Gram-positive bacteria
Rudilla Mateo, Héctor
Staphylococcus aureus
Antibiòtics pèptids
Models moleculars
Staphylococcus aureus
Peptide antibiotics
Molecular models
title_short Novel synthetic polymyxins kill Gram-positive bacteria
title_full Novel synthetic polymyxins kill Gram-positive bacteria
title_fullStr Novel synthetic polymyxins kill Gram-positive bacteria
title_full_unstemmed Novel synthetic polymyxins kill Gram-positive bacteria
title_sort Novel synthetic polymyxins kill Gram-positive bacteria
dc.creator.none.fl_str_mv Rudilla Mateo, Héctor
Pérez Guillén, Isabel
Rabanal Anglada, Francesc
Sierra Ortigosa, Josep Maria
Vinuesa Aumedes, Teresa
Viñas, Miquel
author Rudilla Mateo, Héctor
author_facet Rudilla Mateo, Héctor
Pérez Guillén, Isabel
Rabanal Anglada, Francesc
Sierra Ortigosa, Josep Maria
Vinuesa Aumedes, Teresa
Viñas, Miquel
author_role author
author2 Pérez Guillén, Isabel
Rabanal Anglada, Francesc
Sierra Ortigosa, Josep Maria
Vinuesa Aumedes, Teresa
Viñas, Miquel
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Staphylococcus aureus
Antibiòtics pèptids
Models moleculars
Staphylococcus aureus
Peptide antibiotics
Molecular models
topic Staphylococcus aureus
Antibiòtics pèptids
Models moleculars
Staphylococcus aureus
Peptide antibiotics
Molecular models
description 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.
publishDate 2018
dc.date.none.fl_str_mv 2018
2026
2026
2026
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/228138
url https://hdl.handle.net/2445/228138
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1093/jac/dky366
Journal of Antimicrobial Chemotherapy, 2018, vol. 73, num.12, p. 3385-3390
https://doi.org/10.1093/jac/dky366
dc.rights.none.fl_str_mv (c) Rudilla H et al., 2018
info:eu-repo/semantics/openAccess
rights_invalid_str_mv (c) Rudilla H et al., 2018
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 32 p.
application/pdf
dc.publisher.none.fl_str_mv Oxford University Press
publisher.none.fl_str_mv Oxford University Press
dc.source.none.fl_str_mv Articles publicats en revistes (Química Inorgànica i Orgànica)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
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