Alkylaminoquinolines inhibit the bacterial antibiotic efflux pump in multidrug-resistant clinical isolates
| Autor: | Jacques Barbe, Pierre Brouant, Abdallah Mahamoud, Jacqueline Chevalier, Monique Malléa, Sandrine Alibert-Franco, Jean-Marie Pagès |
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| Rok vydání: | 2003 |
| Předmět: |
Drug
medicine.drug_class media_common.quotation_subject Antibiotics Pharmacology Biochemistry Microbiology Aminoquinoline Antibiotic resistance Bacterial Proteins Drug Resistance Multiple Bacterial Membrane Transport Modulators medicine Humans Molecular Biology media_common biology Membrane Transport Proteins Enterobacter aerogenes Cell Biology biology.organism_classification Anti-Bacterial Agents Multiple drug resistance Chloramphenicol Aminoquinolines Efflux Bacteria Intracellular Research Article medicine.drug |
| Zdroj: | Biochemical Journal. 376:801-805 |
| ISSN: | 1470-8728 0264-6021 |
| DOI: | 10.1042/bj20030963 |
| Popis: | Over the last decade, MDR (multidrug resistance) has increased worldwide in microbial pathogens by efflux mechanisms, leading to treatment failures in human infections. Several Gram-negative bacteria efflux pumps have been described. These proteinaceous channels are capable of expelling structurally different drugs across the envelope and conferring antibiotic resistance in various bacterial pathogens. Combating antibiotic resistance is an urgency and the blocking of efflux pumps is an attractive response to the emergence of MDR phenotypes in infectious bacteria. In the present study, various alkylaminoquinolines were tested as potential inhibitors of drug transporters. We showed that alkylaminoquinolines are capable of restoring susceptibilities to structurally unrelated antibiotics in clinical isolates of MDR Gram-negative bacteria. Antibiotic efflux studies indicated that 7-nitro-8-methyl-4-[2´-(piperidino)ethyl]aminoquinoline acts as an inhibitor of the AcrAB–TolC efflux pump and restores a high level of intracellular drug concentration. Inhibitory activity of this alkylaminoquinoline is observed on clinical isolates showing different resistance phenotypes. |
| Databáze: | OpenAIRE |
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