1. Terpinen-4-ol, tyrosol, and β-lapachone as potential antifungals against dimorphic fungi.
- Author
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Brilhante RS, Caetano ÉP, Lima RA, Marques FJ, Castelo-Branco DS, Melo CV, Guedes GM, Oliveira JS, Camargo ZP, Moreira JL, Monteiro AJ, Bandeira TJ, Cordeiro RA, Rocha MF, and Sidrim JJ
- Subjects
- Cell Membrane Permeability drug effects, Ergosterol metabolism, Fungi classification, Fungi metabolism, Microbial Sensitivity Tests, Osmotic Pressure, Phenylethyl Alcohol pharmacology, Antifungal Agents pharmacology, Fungi drug effects, Naphthoquinones pharmacology, Phenylethyl Alcohol analogs & derivatives, Terpenes pharmacology
- Abstract
This study aimed to evaluate the in vitro antifungal activity of terpinen-4-ol, tyrosol, and β-lapachone against strains of Coccidioides posadasii in filamentous phase (n=22) and Histoplasma capsulatum in both filamentous (n=40) and yeast phases (n=13), using the broth dilution methods as described by the Clinical and Laboratory Standards Institute, to determine the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of these compounds. The mechanisms of action of these compounds were also investigated by analyzing their effect on cell membrane permeability and ergosterol synthesis. The MIC and MFCf these compounds against C. posadasii, mycelial H. capsulatum, and yeast-like H. capsulatum, were in the following ranges: 350-5720μg/mL, 20-2860μg/mL, and 40-1420μg/mL, respectively for terpinen-4-ol; 250-4000μg/mL, 30-2000μg/mL, and 10-1000μg/mL, respectively, for tyrosol; and 0.48-7.8μg/mL, 0.25-16μg/mL, and 0.125-4μg/mL, respectively for β-lapachone. These compounds showed a decrease in MIC when the samples were subjected to osmotic stress, suggesting that the compounds acted on the fungal membrane. All the compounds were able to reduce the ergosterol content of the fungal strains. Finally, tyrosol was able to cause a leakage of intracellular molecules., (Copyright © 2016 Sociedade Brasileira de Microbiologia. Published by Elsevier Editora Ltda. All rights reserved.)
- Published
- 2016
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