Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Guo, Shuanli, Yang, Wei, Zhao, Mingming, Tian, Rui, Zhang, Boyu, Qi, Yanfei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
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
_version_ 1783348856999641088
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
work_keys_str_mv AT guoshuanli invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes
AT yangwei invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes
AT zhaomingming invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes
AT tianrui invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes
AT zhangboyu invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes
AT qiyanfei invitroanticandidalactivityandmechanismofapolyoxovanadatefunctionalizedbyznfluconazolecomplexes