1. Isoeugenol and Hybrid Acetamides against Candida albicans Isolated from the Oral Cavity
- Author
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Laísa Vilar Cordeiro, José Maria Barbosa-Filho, Edeltrudes de Oliveira Lima, Jefferson Nóbrega, Jeane U. G. Jardim, Daianne Medeiros, José Klidenberg de Oliveira-Júnior, Petrônio Filgueiras de Athayde-Filho, Helivaldo Diógenes da Silva Souza, Gracielle Angeline Tavares Da Silva, and Luciana Scotti
- Subjects
0301 basic medicine ,030106 microbiology ,lcsh:Medicine ,lcsh:RS1-441 ,Pharmaceutical Science ,macromolecular substances ,Article ,lcsh:Pharmacy and materia medica ,03 medical and health sciences ,Minimum inhibitory concentration ,chemistry.chemical_compound ,Drug Discovery ,Candida albicans ,medicine ,oral candidiasis ,checkerboard method ,chemistry.chemical_classification ,biology ,Chemistry ,lcsh:R ,antifungal activity ,Biological activity ,molecular docking ,biology.organism_classification ,Antimicrobial ,In vitro ,Isoeugenol ,030104 developmental biology ,Enzyme ,Nystatin ,Biochemistry ,isoeugenol ,Molecular Medicine ,medicine.drug - Abstract
Isougenol is a phytoconstituent found in several essential oils. Since many natural products are potent antimicrobials, the synthesis of hybrid molecules&mdash, combining the chemical skeleton of the phytochemical with synthetic groups&mdash, can generate substances with enhanced biological activity. Based on this, the objective of this study was to evaluate the antifungal activity of isoeugenol and hybrid acetamides against Candida albicans isolated from the oral cavity. The methodologies used were the determination of minimum inhibitory concentration (MIC), minimum fungicidal concentration (MFC), action on fungal micromorphology, interaction test with nystatin by the checkerboard method and molecular docking study with important enzymes in the maintenance of fungal viability. The synthetic molecules did not demonstrate significant antifungal activity in vitro. The isoeugenol MIC and MFC varied between 128 and 256 µ, g/mL, being the phytoconstituent able to interfere in the formation of blastoconid and chlamydoconid structures, important in the pathogenic process of the species. The molecular docking study revealed that isoeugenol is a potential inhibitor of the enzymes 14-&alpha, demethylase and delta-14-sterol reductase, interfering in the fungal cell membrane biosynthesis. Thus, this research provides clearer expectations for future pharmacological studies with isoeugenol and derived molecules, aiming at its therapeutic application against infections caused by Candida spp.
- Published
- 2020