Cargando…

The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors

Given the increased antimicrobial resistance, global effort is currently focused on the identification of novel compounds, both of natural and chemical origin. The present study reports on the antifungal potential of 1-(1H-indol-3-yl) derivatives, previously known as tyrosinase inhibitors. The effec...

Descripción completa

Detalles Bibliográficos
Autores principales: Gervasi, Teresa, Ginestra, Giovanna, Mancuso, Francesca, Barreca, Davide, De Luca, Laura, Mandalari, Giuseppina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8538185/
https://www.ncbi.nlm.nih.gov/pubmed/34683392
http://dx.doi.org/10.3390/microorganisms9102070
_version_ 1784588444947709952
author Gervasi, Teresa
Ginestra, Giovanna
Mancuso, Francesca
Barreca, Davide
De Luca, Laura
Mandalari, Giuseppina
author_facet Gervasi, Teresa
Ginestra, Giovanna
Mancuso, Francesca
Barreca, Davide
De Luca, Laura
Mandalari, Giuseppina
author_sort Gervasi, Teresa
collection PubMed
description Given the increased antimicrobial resistance, global effort is currently focused on the identification of novel compounds, both of natural and chemical origin. The present study reports on the antifungal potential of 1-(1H-indol-3-yl) derivatives, previously known as tyrosinase inhibitors. The effect of seven compounds (indicated as 3a–g) was determined against Candida albicans ATCC 10531, three clinical isolates of Candida albicans, two clinical isolates of Candida glabrata, two clinical isolates of Candida parapsilosis and Aspergillus niger ATCC 16404. The effect of these derivatives on tyrosinase enzymatic activity was also evaluated. Results showed a fungicidal activity of compounds 3b, 3c and 3e against all tested strains at concentrations ranging between 0.250 and 1 mg/mL. Furthermore, the association between 3c and fluconazole and between 3b and caspofungin showed a trend of indifference tending toward synergism. Compound 3c was also able to inhibit microbial tyrosinase up to ~28% at the concentration of 0.250 mg/mL. These data could help provide novel therapeutics for topical use to treat fungal infections and increase the potential effectiveness of the association between novel compounds and commercial antifungals in order to combat drug resistance.
format Online
Article
Text
id pubmed-8538185
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-85381852021-10-24 The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors Gervasi, Teresa Ginestra, Giovanna Mancuso, Francesca Barreca, Davide De Luca, Laura Mandalari, Giuseppina Microorganisms Article Given the increased antimicrobial resistance, global effort is currently focused on the identification of novel compounds, both of natural and chemical origin. The present study reports on the antifungal potential of 1-(1H-indol-3-yl) derivatives, previously known as tyrosinase inhibitors. The effect of seven compounds (indicated as 3a–g) was determined against Candida albicans ATCC 10531, three clinical isolates of Candida albicans, two clinical isolates of Candida glabrata, two clinical isolates of Candida parapsilosis and Aspergillus niger ATCC 16404. The effect of these derivatives on tyrosinase enzymatic activity was also evaluated. Results showed a fungicidal activity of compounds 3b, 3c and 3e against all tested strains at concentrations ranging between 0.250 and 1 mg/mL. Furthermore, the association between 3c and fluconazole and between 3b and caspofungin showed a trend of indifference tending toward synergism. Compound 3c was also able to inhibit microbial tyrosinase up to ~28% at the concentration of 0.250 mg/mL. These data could help provide novel therapeutics for topical use to treat fungal infections and increase the potential effectiveness of the association between novel compounds and commercial antifungals in order to combat drug resistance. MDPI 2021-10-01 /pmc/articles/PMC8538185/ /pubmed/34683392 http://dx.doi.org/10.3390/microorganisms9102070 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Gervasi, Teresa
Ginestra, Giovanna
Mancuso, Francesca
Barreca, Davide
De Luca, Laura
Mandalari, Giuseppina
The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title_full The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title_fullStr The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title_full_unstemmed The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title_short The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors
title_sort in vitro potential of 1-(1h-indol-3-yl) derivatives against candida spp. and aspergillus niger as tyrosinase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8538185/
https://www.ncbi.nlm.nih.gov/pubmed/34683392
http://dx.doi.org/10.3390/microorganisms9102070
work_keys_str_mv AT gervasiteresa theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT ginestragiovanna theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT mancusofrancesca theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT barrecadavide theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT delucalaura theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT mandalarigiuseppina theinvitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT gervasiteresa invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT ginestragiovanna invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT mancusofrancesca invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT barrecadavide invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT delucalaura invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors
AT mandalarigiuseppina invitropotentialof11hindol3ylderivativesagainstcandidasppandaspergillusnigerastyrosinaseinhibitors