A new pleuromutilin candidate with potent antibacterial activity against Pasteurella multocida

Microb Pathog. 2019 Feb:127:202-207. doi: 10.1016/j.micpath.2018.12.009. Epub 2018 Dec 7.

Abstract

This study assessed the antimicrobial activity of 14-O-[(4,6-Diaminopyrimidine-2-yl) thioacetyl] mutilin (DPTM), a novel pleuromutilin candidate with a substituted pyrimidine moiety, against Pasteurella multocida. Minimum Inhibitory Concentration (MIC), Oxford Cup assay, and time-kill experiments were used to measure the activity of DPTM against P. multocida serotype A in vitro. We observed that DPTM was potent against Pasteurella multocida serotype A with the MIC value of 0.781 μg/mL. The mean inhibition-zone diameters of DPTM (50, 25, and 12.5 μg/mL) were 29.4, 24.2 and 20.1 mm, respectively. Time-kill experiments showed that the drug caused a rapid decline in the number of bacteria compared with the initial inoculum at 4 h and killed 94.6% of the bacteria during 24 h. Furthermore, DPTM activity was also assessed in a lung infection model challenged with 4.0 × 109 CFU/mL P. multocida serotype A. The results showed that DPTM significantly reduced mortality rate and bacterial load, and alleviated the pathological changes of lung. The antibacterial effect of DPTM found in this study suggested that it was useful in the prevention or control of pneumonia caused by P. multocida.

Keywords: Antibacterial activity; DPTM; Mice; Pasteurella multocida.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Colony Count, Microbial
  • Disease Models, Animal
  • Diterpenes / administration & dosage
  • Diterpenes / chemistry
  • Diterpenes / pharmacology
  • Lung / microbiology
  • Lung / pathology
  • Mice
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Pasteurella Infections / drug therapy
  • Pasteurella Infections / microbiology
  • Pasteurella Infections / pathology
  • Pasteurella multocida / drug effects*
  • Pleuromutilins
  • Pneumonia, Bacterial / drug therapy
  • Pneumonia, Bacterial / microbiology
  • Pneumonia, Bacterial / pathology
  • Polycyclic Compounds
  • Treatment Outcome

Substances

  • Anti-Bacterial Agents
  • Diterpenes
  • Polycyclic Compounds