8-Hydroxyquinoline derivative as a promising antifungal agent to combat ocular fungal infections

J Med Microbiol. 2025 Jan;74(1). doi: 10.1099/jmm.0.001952.

Abstract

Introduction. Ocular fungal infections are pathologies of slow progression, occurring mainly in the cornea, but can also affect the entire structure of the eyeball. The main aetiological agents are species of the genera Candida and Fusarium. Both diagnosis and treatment require speed and effectiveness. However, the currently available therapy basically consists of the use of azoles and polyenes, known for their low penetration into the ocular tissue and the associated toxicity.Hypothesis. Thus, new strategies to combat these infections are needed, such as the development of new antifungals or the use of associations.Aim. Thus, the compound PH151, derived from a promising class of 8-hydroxyquinolines, and natamycin, amphotericin B (AMB) and voriconazole (VRC), the main antifungals used in ocular antifungal therapy, were considered against Candida spp. and Fusarium spp.Methodology. The MICs of compound PH151 ranged from 1.0 to 16.0 µg ml-1, according to CLSI protocols.Results. The association of PH151 with AMB and VRC showed a synergistic effect for more than 50% of the strains tested.Conclusion. Both the compound alone and its association (VRC-AMB-PH151) demonstrated promising potential as an antifungal agent in ocular infections, since the evaluated ocular toxicity profile was positive and the compounds presented low toxicity.

Keywords: 8-hydroxyquinoline; antifungal; combination; fungal keratitis; ocular fungal infection.

MeSH terms

  • Amphotericin B / pharmacology
  • Amphotericin B / therapeutic use
  • Antifungal Agents* / pharmacology
  • Antifungal Agents* / therapeutic use
  • Candida* / drug effects
  • Candidiasis / drug therapy
  • Candidiasis / microbiology
  • Drug Synergism
  • Eye Infections, Fungal* / drug therapy
  • Eye Infections, Fungal* / microbiology
  • Fusariosis / drug therapy
  • Fusariosis / microbiology
  • Fusarium* / drug effects
  • Humans
  • Microbial Sensitivity Tests*
  • Natamycin / pharmacology
  • Natamycin / therapeutic use
  • Oxyquinoline / chemistry
  • Oxyquinoline / pharmacology
  • Voriconazole / pharmacology
  • Voriconazole / therapeutic use

Substances

  • Antifungal Agents
  • Amphotericin B
  • Oxyquinoline
  • Voriconazole
  • Natamycin