Terpinen-4-ol as an Antibacterial and Antibiofilm Agent against <i>Staphylococcus aureus</i>

• Main Authors: Laísa Cordeiro, Pedro Figueiredo, Helivaldo Souza, Aleson Sousa, Francisco Andrade-Júnior, Daianne Medeiros, Jefferson Nóbrega, Daniele Silva, Evandro Martins, José Barbosa-Filho, Edeltrudes Lima
• Format: Article
• Language: English
• Published: MDPI AG 2020-06-01
• Series: International Journal of Molecular Sciences
• Subjects: terpinen-4-ol; <i>Staphylococcus aureus</i>; antibacterial; antibiofilm; molecular docking; checkerboard method
• Online Access: https://www.mdpi.com/1422-0067/21/12/4531
• ISSN: 1661-6596; 1422-0067

<i>Staphylococcus aureus</i> 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 <i>Melaleuca alternifolia</i> 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 <i>S. aureus</i>. 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 <i>S. aureus</i> 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% (<i>v/v</i>) and an MBC of 0.5% (<i>v/v</i>) (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 <i>S. aureus</i>. 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.