comparison of antifungal activity and therapeutic potential
Nevena Lj. Stevanović (Author), Ivana Aleksić (Author), Jakob Kljun (Author), Sanja Skaro-Bogojevic (Author), Aleksandar Veselinovic (Author), Jasmina Nikodinović-Runić (Author), Iztok Turel (Author), Miloš I. Djuran (Author), Biljana Đ. Glišić (Author)

Abstract

Copper(II) and zinc(II) complexes with clinically used antifungal drug fluconazole (fcz), {[CuCl$_2$(fcz)$_2$]·5H$_2$O}$_n$, 1, and {[ZnCl$_2$(fcz)$_2$]·2C$_2$H$_5$OH}$_n$, 2, were prepared and characterized by spectroscopic and crystallographic methods. The polymeric structure of the complexes comprises four fluconazole molecules monodentately coordinated via the triazole nitrogen and two chlorido ligands. With respect to fluconazole, complex 2 showed significantly higher antifungal activity against Candida krusei and Candida parapsilosis. All tested compounds reduced the total amount of ergosterol at subinhibitory concentrations, indicating that the mode of activity of fluconazole was retained within the complexes, which was corroborated via molecular docking with cytochrome P450 sterol 14α-demethylase (CYP51) as a target. Electrostatic, steric and internal energy interactions between the complexes and enzyme showed that 2 has higher binding potency to this target. Both complexes showed strong inhibition of C. albicans filamentation and biofilm formation at subinhibitory concentrations, with 2 being able to reduce the adherence of C. albicans to A549 cells in vitro. Complex 2 was able to reduce pyocyanin production in Pseudomonas aeruginosa between 10% and 25% and to inhibit its biofilm formation by 20% in comparison to the untreated control. These results suggest that complex 2 may be further examined in the mixed Candida-P. aeruginosa infections.

Keywords

baker;cink;kovinski kompleksi;

Data

Language: English
Year of publishing:
Typology: 1.01 - Original Scientific Article
Organization: UL FKKT - Faculty of Chemistry and Chemical Technology
UDC: 546.47:546.562
COBISS: 45141251 Link will open in a new window
ISSN: 1424-8247
Views: 207
Downloads: 51
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Other data

Secondary language: Slovenian
Secondary keywords: baker;cink;kovinski kompleksi;
Type (COBISS): Article
Pages: str. 1-20
Volume: ǂVol. ǂ14
Issue: ǂiss. ǂ1
Chronology: Jan. 2021
DOI: 10.3390/ph14010024
ID: 14511491