Antimicrobial activity of enacyloxin IIa and gladiolin against the urogenital pathogens Neisseria gonorrhoeae and Ureaplasma spp

J Appl Microbiol. 2021 May;130(5):1546-1551. doi: 10.1111/jam.14858. Epub 2020 Oct 21.

Abstract

Aims: To determine the antimicrobial activity of enacyloxin IIa and gladiolin against Neisseria gonorrhoeae and Ureaplasma spp.

Methods and results: The Burkholderia polyketide antibiotics enacyloxin IIa and gladiolin were tested against 14 N. gonorrhoeae and 10 Ureaplasma spp. isolates including multidrug-resistant N. gonorrhoeae isolates WHO V, WHO X and WHO Z as well as macrolide, tetracycline and ciprofloxacin-resistant ureaplasmas. Susceptibility testing of N. gonorrhoeae was carried out by agar dilution, whereas broth micro-dilution and growth kinetic assays were used for Ureaplasma spp. The MIC range for enacyloxin IIa and gladiolin against N. gonorrhoeae was 0·015-0·06 mg l-1 and 1-2 mg l-1 respectively. The presence of resistance to front line antibiotics had no effect on MIC values. The MIC range for enacyloxin IIa against Ureaplasma spp. was 4-32 mg l-1 with a clear dose-dependent effect when observed using a growth kinetic assay. Gladiolin had no antimicrobial activity on Ureaplasma spp. at 32 mg l-1 and limited impact on growth kinetics.

Conclusions: Enacyloxin IIa and gladiolin antibiotics have antimicrobial activity against a range of antibiotic susceptible and resistant N. gonorrhoeae and Ureaplasma isolates.

Significance and impact of the study: This study highlights the potential for a new class of antimicrobial against pathogens in which limited antibiotics are available. Development of these compounds warrants further investigation in the face of emerging extensively drug-resistant strains.

Keywords: Neisseria gonorrhoeae; Ureaplasma parvum; Ureaplasma urealyticum; Enacyloxin IIa; gladiolin; novel antimicrobials.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Drug Resistance, Bacterial / drug effects
  • Humans
  • Macrolides / pharmacology*
  • Microbial Sensitivity Tests
  • Neisseria gonorrhoeae / drug effects*
  • Neisseria gonorrhoeae / growth & development
  • Neisseria gonorrhoeae / isolation & purification
  • Polyenes / pharmacology*
  • Ureaplasma / drug effects*
  • Ureaplasma / growth & development
  • Ureaplasma / isolation & purification

Substances

  • Anti-Bacterial Agents
  • Macrolides
  • Polyenes
  • gladiolin
  • enacyloxin IIa