We found a match
Your institution may have rights to this item. Sign in to continue.
- Title
In Vitro and In Silico Inhibition of Staphylococcus aureus Efflux Pump NorA by α-Pinene and Limonene.
- Authors
de Araújo, Ana Carolina Justino; Freitas, Priscilla Ramos; dos Santos Barbosa, Cristina Rodrigues; Muniz, Débora Feitosa; de Almeida, Ray Silva; Alencar de Menezes, Irwin Rose; Ribeiro-Filho, Jaime; Tintino, Saulo Relison; Coutinho, Henrique Douglas Melo
- Abstract
Since the discovery of the first antibiotics, bacteria have acquired a variety of resistance mechanisms, with efflux pump (EP) being the most prominent mechanism for intracellular targeting drugs. These proteins have become efficient mechanisms of resistance to antibiotics in species such as Staphylococcus aureus and, therefore, have been identified as promising therapeutic targets in antibacterial drug development. Accordingly, evidence suggests that monoterpenes can act as EP inhibitors and can be useful in circumventing bacterial resistance. This study aimed to evaluate the effectiveness of monoterpenes α-pinene and limonene as EP inhibitors against a strain of S. aureus expressing NorA protein. The minimum inhibitory concentration (MIC) against the 1199B strain of S. aureus, which carries genes encoding efflux proteins associated with antibiotic resistance to norfloxacin, was assessed through the broth microdilution method. The results obtained served as a subsidy for the analysis of the NorA pump inhibition with norfloxacin and ethidium bromide. Docking techniques, in silico, were used to evaluate the interaction of monoterpenes with NorA. Both monoterpenes showed no clinically effective antibacterial activity. Nevertheless, these compounds were found to decrease the MICs of ethidium bromide and norfloxacin indicating EP inhibition, which was confirmed by molecular docking analyses. In conclusion, α-pinene and limonene showed promising antibiotic-enhancing properties in S. aureus 1199B strain, indicating that monoterpenes can be used in targeted drug development to combat antibiotic resistance associated with EP expression.
- Subjects
MONOTERPENES; LIMONENE; ANTIBIOTICS; DRUG target; DRUG resistance in bacteria; NORFLOXACIN; DRUG utilization; STAPHYLOCOCCUS aureus
- Publication
Current Microbiology, 2021, Vol 78, Issue 9, p3388
- ISSN
0343-8651
- Publication type
Article
- DOI
10.1007/s00284-021-02611-9