New antifungal 4-chloro-3-nitrophenyldifluoroiodomethyl sulfone reduces the Candida albicans pathogenicity in the Galleria mellonella model organism

Braz J Microbiol. 2020 Mar;51(1):5-14. doi: 10.1007/s42770-019-00140-z. Epub 2019 Sep 4.

Abstract

Candida albicans represents an interesting microorganism to study complex host-pathogen interactions and for the development of effective antifungals. Our goal was to assess the efficacy of 4-chloro-3-nitrophenyldifluoroiodomethyl sulfone (named Sulfone) against the C. albicans infections in the Galleria mellonella host model. We assessed invasiveness of CAI4 parental strain and mutants: kex2Δ/KEX2 and kex2Δ/kex2Δ in G. mellonella treated with Sulfone. We determined that KEX2 expression was altered following Sulfone treatment in G. mellonella-C. albicans infection model. Infection with kex2Δ/kex2Δ induced decreased inflammation and minimal fault in fitness of larvae vs CAI4. Fifty percent of larvae died within 4-5 days (P value < 0.0001) when infected with CAI4 and kex2Δ/KEX2 at 109 CFU/mL; survival reached 100% in those injected with kex2Δ/kex2Δ. Larvae treated with Sulfone at 0.01 mg/kg 30 min before infection with all C. albicans tested survived infection at 90-100% vs C. albicans infected-PBS-treated larvae. Hypersensitive to Sulfone, kex2Δ/kex2Δ reduced virulence in survival. KEX2 was down-regulated when larvae were treated with Sulfone: 30 min before and 2 h post-SC5314-wild-type infection respectively. kex2Δ/kex2Δ was able to infect larvae, but failed to kill host when treated with Sulfone. Sulfone can be used to prevent or treat candidiasis. G. mellonella facilitates studding of host-pathogen interactions, i.e., testing host vs panel of C. albicans mutants when antifungal is dosed.

Keywords: Antifungal agent; C. albicans; Candidiasis; G. mellonella; Gene expression; Virulence.

MeSH terms

  • Animals
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology*
  • Candida albicans / drug effects*
  • Candida albicans / genetics
  • Candida albicans / pathogenicity
  • Candidiasis / drug therapy*
  • Colony Count, Microbial
  • Fungal Proteins / genetics
  • Host-Pathogen Interactions
  • Larva / drug effects
  • Larva / microbiology
  • Moths / drug effects*
  • Moths / microbiology
  • Sulfones / chemical synthesis
  • Sulfones / pharmacology*
  • Virulence

Substances

  • Antifungal Agents
  • Fungal Proteins
  • Sulfones