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In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes
The rise in the number of fungal infections is requiring the rapid development of novel antifungal agents. A new polyoxovanadate functionalized by Zn-fluconazole coordination complexes, Zn(3)(FLC)(6)V(10)O(28)·10H(2)O (ZnFLC) (FLC = fluconazole) has been synthesized and evaluated for in vitro antifu...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100367/ https://www.ncbi.nlm.nih.gov/pubmed/29747400 http://dx.doi.org/10.3390/molecules23051122 |
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author | Guo, Shuanli Yang, Wei Zhao, Mingming Tian, Rui Zhang, Boyu Qi, Yanfei |
author_facet | Guo, Shuanli Yang, Wei Zhao, Mingming Tian, Rui Zhang, Boyu Qi, Yanfei |
author_sort | Guo, Shuanli |
collection | PubMed |
description | The rise in the number of fungal infections is requiring the rapid development of novel antifungal agents. A new polyoxovanadate functionalized by Zn-fluconazole coordination complexes, Zn(3)(FLC)(6)V(10)O(28)·10H(2)O (ZnFLC) (FLC = fluconazole) has been synthesized and evaluated for in vitro antifungal against Candida species. The identity of ZnFLC were confirmed by elemental analysis, IR spectrum, and single-crystal X-ray diffraction. The antifungal activities of ZnFLC was screened in 19 Candida species strains using the microdilution checkerboard technique. The minimum inhibitory concentration (MIC(80)) value of ZnFLC is 4 μg/mL on the azole-resistant clinical isolates of C. albicans HL973, which is lower than the positive control, FLC. The mechanism of ZnFLC against C. albicans HL973 showed that ZnFLC damaged the fungal cell membrane and reduced the ergosterol content. The expression of ERG1, ERG7, ERG11 ERG27, and ERG28, which have effects on the synthesis of ergosterol, were all significantly upregulated by ZnFLC. |
format | Online Article Text |
id | pubmed-6100367 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61003672018-11-13 In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes Guo, Shuanli Yang, Wei Zhao, Mingming Tian, Rui Zhang, Boyu Qi, Yanfei Molecules Article The rise in the number of fungal infections is requiring the rapid development of novel antifungal agents. A new polyoxovanadate functionalized by Zn-fluconazole coordination complexes, Zn(3)(FLC)(6)V(10)O(28)·10H(2)O (ZnFLC) (FLC = fluconazole) has been synthesized and evaluated for in vitro antifungal against Candida species. The identity of ZnFLC were confirmed by elemental analysis, IR spectrum, and single-crystal X-ray diffraction. The antifungal activities of ZnFLC was screened in 19 Candida species strains using the microdilution checkerboard technique. The minimum inhibitory concentration (MIC(80)) value of ZnFLC is 4 μg/mL on the azole-resistant clinical isolates of C. albicans HL973, which is lower than the positive control, FLC. The mechanism of ZnFLC against C. albicans HL973 showed that ZnFLC damaged the fungal cell membrane and reduced the ergosterol content. The expression of ERG1, ERG7, ERG11 ERG27, and ERG28, which have effects on the synthesis of ergosterol, were all significantly upregulated by ZnFLC. MDPI 2018-05-09 /pmc/articles/PMC6100367/ /pubmed/29747400 http://dx.doi.org/10.3390/molecules23051122 Text en © 2018 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 Guo, Shuanli Yang, Wei Zhao, Mingming Tian, Rui Zhang, Boyu Qi, Yanfei In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title | In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title_full | In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title_fullStr | In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title_full_unstemmed | In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title_short | In Vitro Anticandidal Activity and Mechanism of a Polyoxovanadate Functionalized by Zn-Fluconazole Complexes |
title_sort | in vitro anticandidal activity and mechanism of a polyoxovanadate functionalized by zn-fluconazole complexes |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100367/ https://www.ncbi.nlm.nih.gov/pubmed/29747400 http://dx.doi.org/10.3390/molecules23051122 |
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