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In-depth characterization of antibacterial activity of melittin against Staphylococcus aureus and use in a model of non-surgical MRSA-infected skin wounds.
Lima, William Gustavo; de Brito, Júlio César Moreira; Cardoso, Valbert Nascimento; Fernandes, Simone Odília Antunes.
Afiliação
  • Lima WG; Laboratório de Radioisótopos, Departamento de Análises Clinicas e Toxicológicas, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
  • de Brito JCM; Fundação Ezequiel Dias (FUNED), Belo Horizonte, MG, Brazil.
  • Cardoso VN; Laboratório de Radioisótopos, Departamento de Análises Clinicas e Toxicológicas, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
  • Fernandes SOA; Laboratório de Radioisótopos, Departamento de Análises Clinicas e Toxicológicas, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil. Electronic address: simoneodilia@yahoo.com.br.
Eur J Pharm Sci ; 156: 105592, 2021 Jan 01.
Article em En | MEDLINE | ID: mdl-33049305
Skin infections caused by methicillin-resistant Staphylococcus aureus (MRSA) require the development of new and effective topical antibiotics. In this context, melittin, the main component of apitoxin, has a potent antibacterial effect. However, little is known regarding the anti-inflammatory potential this peptide in infection models, or its ability to induce clinically important resistance. Here, we aimed to conduct an in-depth characterization of the antibacterial potential of melittin in vitro and evaluate the pharmaceutical potential of an ointment containing melittin for the treatment of non-surgical infections induced by MRSA. The minimum inhibitory concentration of melittin varied from 0.12 to 4 µM. The antibacterial effect was mainly bactericidal and fast (approximately 0.5 h after incubation) and was maintained even in stationary cells and mature MRSA biofilms. Melittin interacts synergistically with beta-lactams and aminoglycosides, and its ability to form pores in the membrane reverses the resistance of vancomycin-intermediate Staphylococcus aureus (VISA) to amoxicillin, and vancomycin. Its ability to induce resistance in vitro was absent, and melittin was stable in several conditions often associated with infected wounds. In vivo, aointment containing melittin reduced bacterial load and the content of pro-inflammatory cytokines, such as tumor necrosis factor-α, interleukin-6 (IL-6), and IL-1 beta. Collectively, these data point to melittin as a potential candidate for topical formulations aimed at the treatment of non-surgical infections caused by MRSA.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Infecções Estafilocócicas / Staphylococcus aureus Resistente à Meticilina Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Eur J Pharm Sci Assunto da revista: FARMACIA / FARMACOLOGIA / QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Infecções Estafilocócicas / Staphylococcus aureus Resistente à Meticilina Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Eur J Pharm Sci Assunto da revista: FARMACIA / FARMACOLOGIA / QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda