Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives
Semisynthetic and commercial coumarins were investigated for their antibacterial and adjuvant properties with antibiotic agents against norfloxacin, erythromycin, and tetracycline resistant Staphylococcus aureus as based on efflux mechanisms. The coumarins and certain commercial antibiotics had thei...
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| Format: | Article |
| Language: | English |
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Wiley
2016-01-01
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| Series: | Scientifica |
| Online Access: | http://dx.doi.org/10.1155/2016/6894758 |
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| author | Rodrigo Santos Aquino de Araújo José Maria Barbosa-Filho Marcus Tullius Scotti Luciana Scotti Ryldene Marques Duarte da Cruz Vivyanne dos Santos Falcão-Silva José Pinto de Siqueira-Júnior Francisco Jaime Bezerra Mendonça-Junior |
| author_facet | Rodrigo Santos Aquino de Araújo José Maria Barbosa-Filho Marcus Tullius Scotti Luciana Scotti Ryldene Marques Duarte da Cruz Vivyanne dos Santos Falcão-Silva José Pinto de Siqueira-Júnior Francisco Jaime Bezerra Mendonça-Junior |
| author_sort | Rodrigo Santos Aquino de Araújo |
| collection | DOAJ |
| description | Semisynthetic and commercial coumarins were investigated for their antibacterial and adjuvant properties with antibiotic agents against norfloxacin, erythromycin, and tetracycline resistant Staphylococcus aureus as based on efflux mechanisms. The coumarins and certain commercial antibiotics had their Minimum Inhibitory Concentrations determined by broth microdilution assay against resistant S. aureus strains which overexpress efflux pump proteins. For evaluation of the modulatory activity, the antibiotics MICs were determined in the presence of the coumarin derivatives at subinhibitory concentration. Although the coumarins did not display relevant antibacterial activity (MIC ≥ 128 µg/mL), they did modulate the antibiotics activities. Various coumarins, especially the alkylated derivatives in combination with antibiotics at subinhibitory concentrations, modulated antibiotic activity, reducing the MIC for tetracycline and norfloxacin by 2 to 8 times. Polar Surface Area (PSA) studies were performed and the fact that the presence of apolar groups is an important factor for the modulatory activity of coumarins was corroborated. Docking on the Penicillin-Binding Protein from MRSA identified that 18 is a potential ligand presenting low Ebinding. The results indicate that coumarin derivatives modulated antibiotic resistance and may be used as potential antibiotic adjuvants, acting by bacterial efflux pump inhibition in S. aureus. |
| format | Article |
| id | doaj-art-8cff6f8aa20a4583abfc4af768b57741 |
| institution | OA Journals |
| issn | 2090-908X |
| language | English |
| publishDate | 2016-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Scientifica |
| spelling | doaj-art-8cff6f8aa20a4583abfc4af768b577412025-08-20T02:09:34ZengWileyScientifica2090-908X2016-01-01201610.1155/2016/68947586894758Modulation of Drug Resistance in Staphylococcus aureus with Coumarin DerivativesRodrigo Santos Aquino de Araújo0José Maria Barbosa-Filho1Marcus Tullius Scotti2Luciana Scotti3Ryldene Marques Duarte da Cruz4Vivyanne dos Santos Falcão-Silva5José Pinto de Siqueira-Júnior6Francisco Jaime Bezerra Mendonça-Junior7Post-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilLaboratory of Genetics of Microorganisms, Molecular Biology Department, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilPost-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, 58051-900 João Pessoa, PB, BrazilSemisynthetic and commercial coumarins were investigated for their antibacterial and adjuvant properties with antibiotic agents against norfloxacin, erythromycin, and tetracycline resistant Staphylococcus aureus as based on efflux mechanisms. The coumarins and certain commercial antibiotics had their Minimum Inhibitory Concentrations determined by broth microdilution assay against resistant S. aureus strains which overexpress efflux pump proteins. For evaluation of the modulatory activity, the antibiotics MICs were determined in the presence of the coumarin derivatives at subinhibitory concentration. Although the coumarins did not display relevant antibacterial activity (MIC ≥ 128 µg/mL), they did modulate the antibiotics activities. Various coumarins, especially the alkylated derivatives in combination with antibiotics at subinhibitory concentrations, modulated antibiotic activity, reducing the MIC for tetracycline and norfloxacin by 2 to 8 times. Polar Surface Area (PSA) studies were performed and the fact that the presence of apolar groups is an important factor for the modulatory activity of coumarins was corroborated. Docking on the Penicillin-Binding Protein from MRSA identified that 18 is a potential ligand presenting low Ebinding. The results indicate that coumarin derivatives modulated antibiotic resistance and may be used as potential antibiotic adjuvants, acting by bacterial efflux pump inhibition in S. aureus.http://dx.doi.org/10.1155/2016/6894758 |
| spellingShingle | Rodrigo Santos Aquino de Araújo José Maria Barbosa-Filho Marcus Tullius Scotti Luciana Scotti Ryldene Marques Duarte da Cruz Vivyanne dos Santos Falcão-Silva José Pinto de Siqueira-Júnior Francisco Jaime Bezerra Mendonça-Junior Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives Scientifica |
| title | Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives |
| title_full | Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives |
| title_fullStr | Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives |
| title_full_unstemmed | Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives |
| title_short | Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives |
| title_sort | modulation of drug resistance in staphylococcus aureus with coumarin derivatives |
| url | http://dx.doi.org/10.1155/2016/6894758 |
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