Abstract

The presence and fate of antifungal agents in the environment have hardly been investigated. This is despite the increased usage of antifungal agents and higher prevalence of antifungal resistance. Stereochemistry of antifungal agents has been largely overlooked due to lack of analytical methods enabling studies at the enantiomeric level. This paper introduces a new analytical method for combined separation of achiral and chiral antifungal agents and their metabolites with the utilization of chiral chromatography coupled with triple quadrupole tandem mass spectrometry to enable comprehensive profiling of wide-ranging antifungal agents and their metabolites in environmental matrices. The method showed very good linearity and range (r2 > 0.997), method accuracy (61-143%) and precision (3-31%) as well as low (ng L-1) MQLs for most analytes. The method was applied in selected environmental samples. The following analytes were quantified: fluconazole, terbinafine, N-desmethyl-carboxyterbinafine, tebuconazole, epoxiconazole, propiconazole and N-deacetyl ketoconazole. They were predominantly present in the aqueous environment (as opposed to wastewater) with sources linked with animal and plant protection rather than usage in humans. Interestingly, chiral fungicides quantified in river water were enriched with one enantiomer. This might have consequences in terms of their ecological effects which warrants further study.

Highlights

  • Antifungal agents are widely used as pharmaceuticals, in household products and in agriculture, which has an impact on the environment

  • The results of this study indicate predominance of antifungal agents in the aqueous environment with sources linked with animal and plant protection rather than usage in humans

  • Chiral fungicides quanti ed in the river water were enriched with one enantiomer

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Summary

Introduction

Antifungal agents are widely used as pharmaceuticals, in household products and in agriculture, which has an impact on the environment. The global reporting of fungal diseases has increased signi cantly in recent years because of an increasing population leading to a rise in the use of antifungal drugs.[1] Generally, there are 3 classes of antifungal agents used in medicines These are azoles, polyenes, and allylamines.[2] Azole antifungal agents can be used in an anti-dandruff shampoo[3] and for material preservation in paints, plastics, sealants, wall adhesives, binders, papers, or polymerised materials, such as leather, rubber, and paper.[4] As a result, antifungal agents, especially azoles, have emerged as a new group of pollutants in the environment and a risk to human health due to unintentional (non-clinical) exposure.[5,6] fungicides are commonly used on fruits and vegetables because fungal diseases are a major threat to crop production. The growth rates of plants and mortality of sh were the result of contamination with antifungal agents.[8,9] azole agents were linked with the decrease in the formation of estradiol and testosterone in humans.[10]

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