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Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans an...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146627/ https://www.ncbi.nlm.nih.gov/pubmed/32213931 http://dx.doi.org/10.3390/molecules25061463 |
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author | Hamdy, Rania Fayed, Bahgat Hamoda, Alshaimaa M. Rawas-Qalaji, Mutasem Haider, Mohamed Soliman, Sameh S. M. |
author_facet | Hamdy, Rania Fayed, Bahgat Hamoda, Alshaimaa M. Rawas-Qalaji, Mutasem Haider, Mohamed Soliman, Sameh S. M. |
author_sort | Hamdy, Rania |
collection | PubMed |
description | Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans and C. auris are associated with high mortality rates, mainly because of their multidrug-resistance patterns against most available antifungal drugs. Although several compounds were designed against C. albicans, very few or none were tested on C. auris. Therefore, it is urgent to develop novel effective antifungal drugs that can accommodate not only C. albicans, but also other Candida spp., particularly newly emergent one, including C. auris. Inspired by the significant broad-spectrum antifungal activities of the essential oil cuminaldehyde and the reported wide incorporation of azoles in the antifungal drugs, a series of compounds (UoST1-11) was designed and developed. The new compounds were designed to overcome the toxicity of the aldehyde group of cuminaldehyde and benefit from the antifungal selectivity of azoles. The new developed UoST compounds showed significant anti-Candida activities against both Candida species. The best candidate compound, UoST5, was further formulated into polymeric nanoparticles (NPs). The new formula, UoST5-NPs, showed similar activities to the nanoparticles-free drug, while providing only 25% release after 24 h, maintainng prolonged activity up to 48 h and affording no toxicity. In conclusion, new azole formulations with significantly enhanced activities against C. albicans and C. auris, while maintaining prolonged action and no toxicities at lower concentrations, were developed. |
format | Online Article Text |
id | pubmed-7146627 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-71466272020-04-20 Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation Hamdy, Rania Fayed, Bahgat Hamoda, Alshaimaa M. Rawas-Qalaji, Mutasem Haider, Mohamed Soliman, Sameh S. M. Molecules Article Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans and C. auris are associated with high mortality rates, mainly because of their multidrug-resistance patterns against most available antifungal drugs. Although several compounds were designed against C. albicans, very few or none were tested on C. auris. Therefore, it is urgent to develop novel effective antifungal drugs that can accommodate not only C. albicans, but also other Candida spp., particularly newly emergent one, including C. auris. Inspired by the significant broad-spectrum antifungal activities of the essential oil cuminaldehyde and the reported wide incorporation of azoles in the antifungal drugs, a series of compounds (UoST1-11) was designed and developed. The new compounds were designed to overcome the toxicity of the aldehyde group of cuminaldehyde and benefit from the antifungal selectivity of azoles. The new developed UoST compounds showed significant anti-Candida activities against both Candida species. The best candidate compound, UoST5, was further formulated into polymeric nanoparticles (NPs). The new formula, UoST5-NPs, showed similar activities to the nanoparticles-free drug, while providing only 25% release after 24 h, maintainng prolonged activity up to 48 h and affording no toxicity. In conclusion, new azole formulations with significantly enhanced activities against C. albicans and C. auris, while maintaining prolonged action and no toxicities at lower concentrations, were developed. MDPI 2020-03-24 /pmc/articles/PMC7146627/ /pubmed/32213931 http://dx.doi.org/10.3390/molecules25061463 Text en © 2020 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Hamdy, Rania Fayed, Bahgat Hamoda, Alshaimaa M. Rawas-Qalaji, Mutasem Haider, Mohamed Soliman, Sameh S. M. Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title | Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title_full | Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title_fullStr | Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title_full_unstemmed | Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title_short | Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation |
title_sort | essential oil-based design and development of novel anti-candida azoles formulation |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146627/ https://www.ncbi.nlm.nih.gov/pubmed/32213931 http://dx.doi.org/10.3390/molecules25061463 |
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