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

Author(s)

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]

Affiliation

^[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

• Document type: Journal article
• Source: Phytotherapy Research; v. 27, n. 10, p. 1502-1507, OCT 2013.
• Web of Science Citations: 10

Abstract

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)

• FAPESP's process: 07/54762-8 - Obtaining structural analogues of pimaradienoic acid through the process of fungal biotransformation and study of the effect of these metabolites on the activity of the TcDHODH enzyme and on the contraction of the vascular smooth muscle of the aorta artery of mice
• Grantee: Sergio Ricardo Ambrosio
• Support Opportunities: BIOTA-FAPESP Program - Young Investigators Grants
• FAPESP's process: 08/07696-2 - Studies on the biotransformation of two fungal diterpene class of pimaranos by Aspergillus ochraceus and biological evaluation of the metabolites obtained.
• Grantee: Thiago Sousa Porto
• Support Opportunities: Scholarships in Brazil - Master