| Author | Muniz, Débora Feitosa | |
| Author | Barbosa, Cristina Rodrigues dos Santos | |
| Author | Menezes, Irwin Rose Alencar de | |
| Author | Sousa, Erlânio Oliveira de | |
| Author | Pereira, Raimundo Luiz Silva | |
| Author | Calixto Júnior, João Tavares | |
| Author | Pereira, Pedro Silvino | |
| Author | Matos, Yedda M.L.S. de | |
| Author | Costa, Roger H.S. da | |
| Author | Tintino, Cícera Datiane de Morais Oliveira | |
| Author | Coutinho, Henrique Douglas Melo | |
| Author | Barbosa Filho, José Maria | |
| Author | Sousa, Gabriela Ribeiro de | |
| Author | Ribeiro Filho, Jaime | |
| Author | Siqueira Junior, José Pinto | |
| Author | Tintino, Saulo Relison | |
| Access date | 2020-09-25T12:21:28Z | |
| Available date | 2020-09-25T12:21:28Z | |
| Document date | 2020 | |
| Citation | MUNIZ, Débora Feitosa et al. In vitro and in silico inhibitory effects of synthetic and natural eugenol derivatives against the NorA efflux pump in Staphylococcus aureus. Food Chemistry, v. 337, p. 1-7, 2020. | pt_BR |
| ISSN | 0308-8146 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/43616 | |
| Sponsorship | Coordination for the Improvement of
Higher Education Personnel (CAPES, Finance Code 001), the Cearense
Foundation for Scientific and Technological Development Support
(FUNCAP, Finance Code BPI), the National Council of Scientific and
Technological Development (CNPq. Processes 150456/2018-2 and
406685/2018-5) and the Financier of Studies and Projects – Brazil
(FINEP). | pt_BR |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | pt_BR |
| Subject in Portuguese | Staphylococcus aureus | pt_BR |
| Subject in Portuguese | Inibidores da bomba | pt_BR |
| Subject in Portuguese | Resistência a antibióticos | pt_BR |
| Subject in Portuguese | Eugenol | pt_BR |
| Title | In vitro and in silico inhibitory effects of synthetic and natural eugenol derivatives against the NorA efflux pump in Staphylococcus aureus | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.foodchem.2020.127776 | pt_BR |
| Abstract | Staphylococcus aureus is a Gram-positive bacterium responsible for a number of diseases and has demonstrated
resistance to conventional antibiotics. This study aimed to evaluate the antibacterial activity of eugenol and its
derivatives allylbenzene, 4-allylanisole, isoeugenol and 4-allyl-2,6-dimethoxyphenol against the S. aureus NorA
efflux pump (EP) in association with norfloxacin and ethidium bromide. The antibacterial activity of the compounds
was assessed using the broth microdilution method to determine the minimum inhibitory concentration
(MIC). A reduction in the MIC of ethidium bromide (a substrate for several efflux pumps) or norfloxacin was used
as a parameter of EP inhibition. Molecular modeling studies were used to predict the 3D structure and analyze
the interaction of selected compounds with the binding pocket of the NorA efflux pump. Except for 4-allylanisole
and allylbenzene, the compounds presented clinically effective antibacterial activity. When associated with
norfloxacin against the SA 1199B strain, 4-allyl-2,6-dimethoxyphenol eugenol and isoeugenol caused significant
reduction in the MIC of the antibiotic, demonstrating synergistic effects. Similar effects were observed when 4-
allyl-2,6-dimethoxyphenol, allylbenzene and isoeugenol were associated with ethidium bromide. Together, these
findings indicate a potential inhibition of the NorA pump by eugenol and its derivatives. This in vitro evidence
was corroborated by docking results demonstrating favorable interactions between 4-allyl-2,6-dimetoxypheno
and the NorA pump mediated by hydrogen bonds and hydrophobic interactions. In conclusion, eugenol derivatives
have the potential to be used in antibacterial drug development in strains carrying the NorA efflux pump. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Pharmacology and Molecular Chemistry. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Regional University of Cariri. Laboratory of Studies of the Regional Flora of the Cariri. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Pharmacology and Molecular Chemistry. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Pharmacology and Molecular Chemistry. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Pharmacology and Molecular Chemistry. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Affilliation | University of João Pessoa. Laboratory of Phamaceutical Tecnology Federal. João Pessoa, PB, Brazil. | pt_BR |
| Affilliation | University of João Pessoa. Laboratory of Phamaceutical Tecnology Federal. João Pessoa, PB, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | pt_BR |
| Affilliation | Universidade Regional do Cariri. Laboratory of Microbiology and Molecular Biolog y. Department of Biological Chemistry. Cariri, CE, Brazil. | pt_BR |
| Subject | Staphylococcus aureus | pt_BR |
| Subject | Efflux pump inhibitors | pt_BR |
| Subject | Antibiotic resistance | pt_BR |
| Subject | Eugenol derivatives | pt_BR |
