Modulation of drug resistance in Staphylococcus aureus by 132-hydroxy-(132-R/S)-pheophytin isolated from Sargassum polyceratium

Microb Pathog. 2020 Apr:141:104034. doi: 10.1016/j.micpath.2020.104034. Epub 2020 Jan 30.

Abstract

Efflux pumps are integral parts of the bacterial plasma membrane that are responsible for many cases of antibiotic resistance. Modulators of drug resistance are regarded as the most suitable new antibacterial therapies. We evaluated the extracts of Sargassum polyceratium and the isolated compound pheophytin (Sp-1) for antibiotic modifying activity in strains of Staphylococcus aureus with efflux pump. The minimum inhibitory concentrations (MICs) for norfloxacin, tetracycline and erythromycin were determined by the microdilution broth method, in the absence and presence of the extract at a sub-inhibitory concentration (MIC/4). The extracts and isolated compounds showed no significant antimicrobial activity, but they changed the antibiotic activity, decreasing bacterial resistance by 2 to 4x. Using a checkerboard method, it was also possible to observe the synergistic effect (ΣFIC ≤ 0.5) between Sp-1 and the antibiotics erythromycin and norfloxacin. The results indicate that the seaweed Sargassum polyceratium and pheophytin are potential sources of an antibiotic adjuvant that modulates bacterial resistance, acting as a putative efflux pump inhibitor.

Keywords: Efflux pump inhibition; Modulation of drug resistance; Pheophytin; Sargassum polyceratium.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Bacterial Proteins / antagonists & inhibitors
  • Bacterial Proteins / metabolism
  • Drug Resistance, Bacterial / drug effects
  • Drug Synergism
  • Erythromycin / pharmacology
  • Membrane Transport Proteins / metabolism
  • Microbial Sensitivity Tests
  • Multidrug Resistance-Associated Proteins / antagonists & inhibitors*
  • Multidrug Resistance-Associated Proteins / metabolism
  • Norfloxacin / pharmacology
  • Pheophytins / metabolism
  • Pheophytins / pharmacology*
  • Plant Extracts / pharmacology
  • Sargassum / metabolism*
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / metabolism
  • Tetracycline / pharmacology

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Membrane Transport Proteins
  • Multidrug Resistance-Associated Proteins
  • Pheophytins
  • Plant Extracts
  • Erythromycin
  • Tetracycline
  • Norfloxacin