Pimarane-type Diterpenes Obtained by Biotransformation: Antimicrobial Properties Against Clinically Isolated Gram-positive Multidrug-resistant Bacteria

Autor(es)

Porto, Thiago S. ^[1] ; Simao, Marilia R. ^[1] ; Carlos, Lucas Z. ^[1] ; Martins, Carlos H. G. ^[1] ; Furtado, Niege A. J. C. ^[2] ; Said, Suraia ^[2] ; Arakawa, Nilton S. ^[3] ; dos Santos, Raquel A. ^[1] ; Veneziani, Rodrigo C. S. ^[1] ; Ambrosio, Sergio R. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Franca, Nucleo Pesquisa Ciencias Exatas & Tecnol, Franca, SP - Brazil

^[2] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Dept Ciencias Farmaceut, Ribeirao Preto, SP - Brazil

^[3] Univ Estadual Londrina, Dept Ciencias Farmaceut, Ctr Ciencias Saude, Londrina, PR - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Phytotherapy Research; v. 27, n. 10, p. 1502-1507, OCT 2013.
• Citações Web of Science: 10

Resumo

The present study describes the antimicrobial activity of five pimarane-type diterpenes obtained by fungal biotransformation against several nosocomial multidrug-resistant bacteria. Among the investigated metabolites, ent-8(14),15-pimaradien-3-ol was the most active compound, with very promising minimal inhibitory concentration values (between 8.0 and 25.0 mu g mL(-1)). Time-kill assays using this metabolite against Staphylococcus aureus (HCRP180) revealed that this compound exerted its bactericidal effect within 24 h at all the evaluated concentrations (8.0, 16.0, and 24.0 mu g mL(-1)). When this metabolite was associated with vancomycin at their minimal bactericidal concentration values, the resulting combination was able to drastically reduce the number of viable strains of S. aureus within the first 6 h, compared with these chemicals alone. The checkerboard assays conducted against this microorganism did not evidence any synergistic effects when this same combination was employed. In conclusion, our results point out that ent-8(14),15-pimaradien-3-ol is an important metabolite in the search for new effective antimicrobial agents. Copyright (c) 2012 John Wiley \& Sons, Ltd. (AU)

• Processo FAPESP: 07/54762-8 - Obtenção de análogos estruturais do ácido pimaradienóico através do processo de biotransformação fúngica e estudo do efeito destes metabólitos sobre a atividade da enzima TcDHODH e sobre a contração da musculatura lisa vascular de artéria aorta de ratos
• Beneficiário: Sergio Ricardo Ambrosio
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Jovens Pesquisadores
• Processo FAPESP: 08/07696-2 - Estudos sobre a biotransformação fúngica de dois diterpenos da classe dos pimaranos por Aspergillus ochraceus e avaliação biológica dos metabólitos obtidos.
• Beneficiário: Thiago Sousa Porto
• Modalidade de apoio: Bolsas no Brasil - Mestrado