Abstract

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, Zn3(FLC)6V10O28·10H2O (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 (MIC80) 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.

Highlights

  • The Candida species including C. albicans, C. glabrata, C. parapsilosis, C. tropicalis, and C. krusei are posing serious nosocomial threats to patient populations [1,2,3]

  • Ergosterol is an important component throughout the fungal cell membranes, which pathway is a significant target of most existing antifungals and new antifungals under development, distinguishes fungi from bacteria, plant, and animal cells

  • ZnFLC, the ergosterol contents were determined synthesized a new compound, Zn3(FLC)6V10O28·10H2O (ZnFLC) which consists of the decavanadate, by high liquid (HPLC),effect and real-time

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Summary

Introduction

The Candida species including C. albicans, C. glabrata, C. parapsilosis, C. tropicalis, and C. krusei are posing serious nosocomial threats to patient populations [1,2,3]. Knowledge, antifungal evaluation decavanadate remains fungiinside from yeast bacteria, and animal It plays a vital role in manyofbiological functions such as scarcely reported by far. Ergosterol is an important component throughout the fungal cell membranes, which pathway is a significant target of most existing antifungals and new antifungals under development, distinguishes fungi from bacteria, plant, and animal cells. It plays a vital role in many biological for instance, itraconazole, amphotericin. ZnFLC, the ergosterol contents were determined synthesized a new compound, Zn3(FLC)6V10O28·10H2O (ZnFLC) which consists of the decavanadate, by high liquid (HPLC),effect and real-time Results and Discussion demonstrates that ZnFLC is a potential antifungal candidate against the Candida species

ResultsDescription and Discussion
FT-IR of ZnFLC
Antifungal Susceptibility Testing
Inhibitory
Growth
Assessment
Methods
F12 N36were
Determination of MIC of ZnFLC
MTS-Reduction Assay
Growth Inhibition Curves
Assessment of Ergosterol Content
3.10. Real-Time PCR
Conclusions
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