Terpinen-4-ol as an Antibacterial and Antibiofilm Agent against Staphylococcus aureus

Int J Mol Sci. 2020 Jun 25;21(12):4531. doi: 10.3390/ijms21124531.

Abstract

Staphylococcus aureus is able to rapidly develop mechanisms of resistance to various drugs and to form strong biofilms, which makes it necessary to develop new antibacterial drugs. The essential oil of Melaleuca alternifolia is used as an antibacterial, a property believed to be mainly due to the presence of terpinen-4-ol. Based on this, the objective of this study was to evaluate the antibacterial and antibiofilm potential of terpinen-4-ol against S. aureus. The Minimal Inhibitory and Minimal Bactericidal Concentrations (MIC and MBC) of terpinen-4-ol were determined, and the effect of its combination with antibacterial drugs as well as its activity against S. aureus biofilms were evaluated. In addition, an in silico analysis of its pharmacokinetic parameters and a molecular docking analysis were performed. Terpinen-4-ol presented a MIC of 0.25% (v/v) and an MBC of 0.5% (v/v) (bactericidal action); its association with antibacterials was also effective. Terpinen-4-ol has good antibiofilm activity, and the in silico results indicated adequate absorption and distribution of the molecule in vivo. Molecular docking indicated that penicillin-binding protein 2a is a possible target of terpinen-4-ol in S. aureus. This work highlights the good potential of terpinen-4-ol as an antibacterial product and provides support for future pharmacological studies of this molecule, aiming at its therapeutic application.

Keywords: Staphylococcus aureus; antibacterial; antibiofilm; checkerboard method; molecular docking; terpinen-4-ol.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Biofilms / drug effects
  • Melaleuca / chemistry
  • Microbial Sensitivity Tests
  • Molecular Docking Simulation
  • Oils, Volatile / pharmacology
  • Staphylococcal Infections / drug therapy
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / metabolism
  • Terpenes / metabolism
  • Terpenes / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Oils, Volatile
  • Terpenes
  • terpinenol-4