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Ent-hardwickiic acid from C. pubiflora and its microbial metabolites are more potent than fluconazole in vitro against Candida glabrata

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Sousa Teixeira, M., V ; Fernandes, L. M. ; de Paula, V. Stefanelli ; Ferreira, A. G. ; Jacometti Cardoso Furtado, N. A.
Total Authors: 5
Document type: Journal article
Source: Letters in Applied Microbiology; v. 74, n. 4, p. 8-pg., 2022-01-17.

The incidence of Candida glabrata infections has rapidly grown and this species is among those responsible for causing invasive candidiasis with a high mortality rate. The diterpene ent-hardwickiic acid is a major constituent in Copaifera pubiflora oleoresin and the ethnopharmacological uses of this oleoresin by people from Brazilian Amazonian region point to a potential use of this major constituent as an antimicrobial. Therefore, the goal of this study was to evaluate the antifungal activity of ent-hardwickiic acid against Candida species and to produce derivatives of this diterpene by using microbial models for simulating the mammalian metabolism. The microbial transformations of ent-hardwickiic acid were carried out by Aspergillus brasiliensis and Cunninghamella elegans and hydroxylated metabolites were isolated and their chemical structures were determined. The antifungal activity of ent-hardwickiic acid and its metabolites was assessed by using the microdilution broth method in 96-well microplates and compared with that of fluconazole. All the diterpenes showed fungistatic effects (ranging from 19 center dot 7 to 75 center dot 2 mu mol l(-1)) against C. glabrata at lower concentrations than fluconazole (163 center dot 2 mu mol l(-1)) and were more potent fungicides (ranging from 39 center dot 5 to 150 center dot 4 mu mol l(-1)) than fluconazole, which showed fungicidal effect at the concentration of 326 center dot 5 mu mol l(-1). (AU)

FAPESP's process: 11/13630-7 - Chemical and pharmacological validation of extracts and active compounds of Copaifera species
Grantee:Jairo Kenupp Bastos
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 16/25201-7 - In vitro studies of bioaccessibility, intestinal transportation and biotransformation of ent-hardwickiic and ent-polyalthic acids from Copaifera pubiflora and Copaifera duckei oil resins
Grantee:Niege Araçari Jacometti Cardoso Furtado
Support Opportunities: Regular Research Grants
FAPESP's process: 17/20397-3 - Investigation of the potential of filamentous fungi to biotransform the ent-polyalthic acid
Grantee:Lívia Maria Fernandes
Support Opportunities: Scholarships in Brazil - Scientific Initiation
FAPESP's process: 17/20071-0 - Investigation of the potential of filamentous fungi to biotransform the ent-hardwickiic acid
Grantee:Vinicius Stefanelli de Paula
Support Opportunities: Scholarships in Brazil - Scientific Initiation