title: Pimarane-type diterpenes obtained by biotransformation: antimicrobial properties against clinically isolated Gram-positive multidrug-resistant bacteria.
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-3β-ol was the most active compound, with very promising minimal inhibitory concentration values (between 8.0 and 25.0 µg 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 µg 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-3β-ol is an important metabolite in the search for new effective antimicrobial agents.
authors.affiliation: Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.
authors.forename: Thiago S
authors.initials: TS
authors.lastname: Porto
authors.forename: Marília R
authors.initials: MR
authors.lastname: Simão
authors.forename: Lucas Z
authors.initials: LZ
authors.lastname: Carlos
authors.forename: Carlos H G
authors.initials: CH
authors.lastname: Martins
authors.forename: Niege A J C
authors.initials: NA
authors.lastname: Furtado
authors.forename: Suraia
authors.initials: S
authors.lastname: Said
authors.forename: Nilton S
authors.initials: NS
authors.lastname: Arakawa
authors.forename: Raquel A
authors.initials: RA
authors.lastname: dos Santos
authors.forename: Rodrigo C S
authors.initials: RC
authors.lastname: Veneziani
authors.forename: Sérgio R
authors.initials: SR
authors.lastname: Ambrósio
mesh_terms: D045784:Abietanes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001235:Aspergillus ochraceus / Q000378:metabolism; D019659:Asteraceae / Q000737:chemistry; D001711:Biotransformation; D024901:Drug Resistance, Multiple, Bacterial; D008826:Microbial Sensitivity Tests; D018517:Plant Roots / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects*; D014640:Vancomycin / Q000494:pharmacology
chemical_list: C544314:8(14),15-pimaradien-3-bol; D045784:Abietanes; D000900:Anti-Bacterial Agents; D014640:Vancomycin