| Literature DB >> 34159523 |
Cristina Rodrigues Dos Santos Barbosa1, Jackelyne Roberta Scherf2, Thiago Sampaio de Freitas3, Irwin Rose Alencar de Menezes4, Raimundo Luiz Silva Pereira3, Joycy Francely Sampaio Dos Santos2, Sarah Silva Patrício de Jesus2, Thais Pereira Lopes2, Zildene de Sousa Silveira2, Cícera Datiane de Morais Oliveira-Tintino5, José Pinto Siqueira Júnior6, Henrique Douglas Melo Coutinho7, Saulo Relison Tintino8, Francisco Assis Bezerra da Cunha9.
Abstract
Undue exposure to antimicrobials has led to the acquisition and development of sophisticated bacterial resistance mechanisms, such as efflux pumps, which are able to expel or reduce the intracellular concentration of various antibiotics, making them ineffective. Therefore, inhibiting this mechanism is a promising way to minimize the phenomenon of resistance in bacteria. In this sense, the present study sought to evaluate the activity of the Carvacrol (CAR) and Thymol (THY) terpenes as possible Efflux Pump Inhibitors (EPIs), by determining the Minimum Inhibitory Concentration (MIC) and the association of these compounds in subinhibitory concentrations with the antibiotic Norfloxacin and with Ethidium Bromide (EtBr) against strains SA-1199 (wild-type) and SA-1199B (overexpresses NorA) of Staphylococcus aureus. In order to verify the interaction of the terpenes with the NorA efflux protein, an in silico molecular modeling study was carried out. The assays used to obtain the MIC of CAR and THY were performed by broth microdilution, while the Efflux Pump inhibitory test was performed by the MIC modification method of the antibiotic Norfloxacin and EtBr. docking was performed using the Molegro Virtual Docker (MVD) program. The results of the study revealed that CAR and THY have moderate bacterial activity and are capable of reducing the MIC of Norfloxacin antibiotic and EtBr in strains of S. aureus carrying the NorA efflux pump. The docking results showed that these terpenes act as possible competitive NorA inhibitors and can be investigated as adjuvants in combined therapies aimed at reducing antibiotic resistance.Entities:
Keywords: Antibiotic resistance; Efflux pump inhibitors; Fluoroquinolone; NorA; Terpenes
Mesh:
Substances:
Year: 2021 PMID: 34159523 DOI: 10.1007/s10863-021-09906-3
Source DB: PubMed Journal: J Bioenerg Biomembr ISSN: 0145-479X Impact factor: 2.945