1. Ex vivo potential of a quinoline-derivative nail lacquer as a new alternative for dermatophytic onychomycosis treatment
- Author
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Marilene Henning Vainstein, Pierre van de Weghe, Denise Diedrich, Simone Jacobus Berlitz, Alexandre Meneghello Fuentefria, Simone Cristina Baggio Gnoatto, Bruna Pippi, Mickael Jean, Diego Defferrari, Gabriella da Rosa Monte Machado, Irene Clemes Külkamp-Guerreiro, William Lopes, Saulo Fernandes de Andrade, Universidade Federal do Rio Grande do Sul [Porto Alegre] (UFRGS), Institut des Sciences Chimiques de Rennes (ISCR), Université de Rennes (UR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), AlexandreMeneghello Fuentefria , FAPERGS , (Award 16/2551-0000517-6), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), and Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)
- Subjects
0301 basic medicine ,Microbiology (medical) ,dermatophytes ,030106 microbiology ,Nail lacquer ,Trichophyton rubrum ,Pharmacology ,Microbiology ,03 medical and health sciences ,chemistry.chemical_compound ,medicine ,onychomycosis ,[CHIM]Chemical Sciences ,Inhibitory effect ,Ergosterol ,biology ,Quinoline ,General Medicine ,biology.organism_classification ,3. Good health ,030104 developmental biology ,medicine.anatomical_structure ,chemistry ,fungicidal effect ,Nail (anatomy) ,ex vivomodel ,quinoline derivative ,Ex vivo ,Derivative (chemistry) - Abstract
Introduction. Onychomycosis infections currently show a significant increase, affecting about 10 % of the world population. Trichophyton rubrum is the main agent responsible for about 80 % of the reported infections. The clinical cure for onychomycosis is extremely difficult and effective new antifungal therapy is needed. Hypothesis/Gap Statement. Ex vivo onychomycosis models using porcine hooves can be an excellent alternative for evaluating the efficacy of new anti-dermatophytic agents in a nail lacquer. Aim. Evaluation of the effectiveness of a nail lacquer containing a quinoline derivative on an ex vivo onychomycosis model using porcine hooves, as well as the proposal of a plausible antifungal mechanism of this derivative against dermatophytic strains. Methodology. The action mechanism of a quinoline derivative was evaluated through the sorbitol protection assay, exogenous ergosterol binding, and the determination of the dose-response curves by time-kill assay. Scanning electron microscopy evaluated the effect of the derivative in the fungal cells. The efficacy of a quinoline-derivative nail lacquer on an ex vivo onychomycosis model using porcine hooves was evaluated as well. Results. The quinoline derivative showed a time-dependent fungicidal effect, demonstrating reduction and damage in the morphology of dermatophytic hyphae. In addition, the ex vivo onychomycosis model was effective in the establishment of infection by T. rubrum. Conclusion. Treatment with the quinoline-derivative lacquer showed a significant inhibitory effect on T. rubrum strain in this infection model. Finally, the compound presents high potential for application in a formulation such as nail lacquer as a possible treatment for dermatophytic onychomycosis.
- Published
- 2021
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