Article
In vitro and in silico inhibition of Staphylococcus aureus efflux pump NorA by α‑Pinene and Limonene
Registro en:
ARAÚJO, Ana Carolina Justino de et al. In vitro and in silico inhibition of Staphylococcus aureus efflux pump NorA by α‑Pinene and Limonene. Current Microbiology, v. 78, p. 3388-3393, 16 July 2021.
0343-8651
10.1007/s00284-021-02611-9
1432-0991
Autor
Araújo, Ana Carolina Justino de
Freitas, Priscilla Ramos
Barbosa, Cristina Rodrigues dos Santos
Muniz, Débora Feitosa
Almeida, Ray Silva de
Menezes, Irwin Rose Alencar de
Ribeiro Filho, Jaime
Tintino, Saulo Relison
Coutinho, Henrique Douglas Melo
Resumen
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. 2022-07-16