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Effect of α-Bisabolol and Its β-Cyclodextrin Complex as TetK and NorA Efflux Pump Inhibitors in Staphylococcus aureus Strains

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Department of Biological Sciences, Regional University of Cariri, Crato, Ceará 63105-000, Brazil
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Department of Physiology, Federal University of Sergipe, São Cristóvão, Sergipe 49100-000, Brazil
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Department of Molecular Biology, Federal University of Paraíba, João Pessoa, Paraíba 58051-900, Brazil
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Department of Agricultural and Environmental Sciences, Milan State University, 20133 Milan, Italy
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Department of Biomedical, Surgical and Dental Sciences, Milan State University, 20142 Milan, Italy
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Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará 63105-000, Brazil
*
Author to whom correspondence should be addressed.
Received: 9 December 2019 / Revised: 8 January 2020 / Accepted: 10 January 2020 / Published: 14 January 2020
(This article belongs to the Special Issue Antimicrobial Plant Extracts and Phytochemicals)
Efflux pumps are proteins present in the plasma membrane of bacteria, which transport antibiotics and other compounds into the extracellular medium, conferring resistance. The discovery of natural efflux pump inhibitors is a promising alternative. α-Bisabolol is a sesquiterpene isolated from several plants such as Matricaria chamomilla L. and has important properties such as antibacterial and anti-inflammatory activity. Currently, the formation of inclusion complexes with β-Cyclodextrin has been used for improving the physicochemical characteristics of the host molecule. This study evaluated the effect of α-Bisabolol, in isolation and in complexation with β-Cyclodextrin, as TetK and NorA efflux pump inhibitors in Staphylococcus aureus strains. The minimum inhibitory concentration (MIC) was determined. Subsequently, inhibitory activity over the pumps was observed by an MIC reduction for the antibiotics, by using subinhibitory concentrations (MIC/8) in combination with tetracycline and norfloxacin. The MIC of the compounds was ≥1024 μg/mL. α-Bisabolol potentiated the action of tetracycline and reduced the MIC of norfloxacin to a clinically relevant concentration. The complexed substance showed synergism however, the effect of the isolated α-Bisabolol was superior to the complex. These results indicate α-Bisabolol is a potential substance to be used as an efflux pump inhibitor. View Full-Text
Keywords: resistance; antibiotics; sesquiterpene; bacteria resistance; antibiotics; sesquiterpene; bacteria
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MDPI and ACS Style

Pereira da Cruz, R.; Sampaio de Freitas, T.; do Socorro Costa, M.; Lucas dos Santos, A.T.; Ferreira Campina, F.; Pereira, R.L.S.; Bezerra, J.W.A.; Quintans-Júnior, L.J.; De Souza Araújo, A.A.; De Siqueira Júnior, J.P.; Iriti, M.; Varoni, E.M.; De Menezes, I.R.A.; Melo Coutinho, H.D.; Bezerra Morais-Braga, M.F. Effect of α-Bisabolol and Its β-Cyclodextrin Complex as TetK and NorA Efflux Pump Inhibitors in Staphylococcus aureus Strains. Antibiotics 2020, 9, 28. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010028

AMA Style

Pereira da Cruz R, Sampaio de Freitas T, do Socorro Costa M, Lucas dos Santos AT, Ferreira Campina F, Pereira RLS, Bezerra JWA, Quintans-Júnior LJ, De Souza Araújo AA, De Siqueira Júnior JP, Iriti M, Varoni EM, De Menezes IRA, Melo Coutinho HD, Bezerra Morais-Braga MF. Effect of α-Bisabolol and Its β-Cyclodextrin Complex as TetK and NorA Efflux Pump Inhibitors in Staphylococcus aureus Strains. Antibiotics. 2020; 9(1):28. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010028

Chicago/Turabian Style

Pereira da Cruz, Rafael, Thiago Sampaio de Freitas, Maria do Socorro Costa, Antonia T. Lucas dos Santos, Fábia Ferreira Campina, Raimundo L.S. Pereira, José W.A. Bezerra, Lucindo J. Quintans-Júnior, Adriano A. De Souza Araújo, José P. De Siqueira Júnior, Marcello Iriti, Elena M. Varoni, Irwin R.A. De Menezes, Henrique D. Melo Coutinho, and Maria F. Bezerra Morais-Braga 2020. "Effect of α-Bisabolol and Its β-Cyclodextrin Complex as TetK and NorA Efflux Pump Inhibitors in Staphylococcus aureus Strains" Antibiotics 9, no. 1: 28. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010028

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