The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria

The potential role of non-antibiotic medicinal products in the treatment of multidrug-resistant Gram-negative bacteria has recently been investigated. It is highly likely that the presence of efflux pumps may be one of the reasons for the weak activity of non-antibiotics, as in the case of some non-...

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Main Authors: Agnieszka E. Laudy, Ewa Kulińska, Stefan Tyski
Format: Article
Language:English
Published: MDPI AG 2017-01-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/22/1/114
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author Agnieszka E. Laudy
Ewa Kulińska
Stefan Tyski
author_facet Agnieszka E. Laudy
Ewa Kulińska
Stefan Tyski
author_sort Agnieszka E. Laudy
collection DOAJ
description The potential role of non-antibiotic medicinal products in the treatment of multidrug-resistant Gram-negative bacteria has recently been investigated. It is highly likely that the presence of efflux pumps may be one of the reasons for the weak activity of non-antibiotics, as in the case of some non-steroidal anti-inflammatory drugs (NSAIDs), against Gram-negative rods. The activity of eight drugs of potential non-antibiotic activity, active substance standards, and relevant medicinal products were analysed with and without of efflux pump inhibitors against 180 strains of five Gram-negative rod species by minimum inhibitory concentration (MIC) value determination in the presence of 1 mM MgSO4. Furthermore, the influence of non-antibiotics on the susceptibility of clinical strains to quinolones with or without PAβN (Phe-Arg-β-naphthylamide) was investigated. The impacts of PAβN on the susceptibility of bacteria to non-antibiotics suggests that amitriptyline, alendronate, nicergoline, and ticlopidine are substrates of efflux pumps in Gram-negative rods. Amitriptyline/Amitriptylinum showed the highest direct antibacterial activity, with MICs ranging 100–800 mg/L against all studied species. Significant decreases in the MIC values of other active substances (acyclovir, atorvastatin, and famotidine) tested with pump inhibitors were not observed. The investigated non-antibiotic medicinal products did not alter the MICs of quinolones in the absence and in the presence of PAβN to the studied clinical strains of five groups of species.
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spelling doaj.art-00288843308b4a26a4fe4e8e4ef980fb2022-12-22T01:28:16ZengMDPI AGMolecules1420-30492017-01-0122111410.3390/molecules22010114molecules22010114The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative BacteriaAgnieszka E. Laudy0Ewa Kulińska1Stefan Tyski2Department of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3 Str., 02-007 Warsaw, PolandDepartment of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3 Str., 02-007 Warsaw, PolandDepartment of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3 Str., 02-007 Warsaw, PolandThe potential role of non-antibiotic medicinal products in the treatment of multidrug-resistant Gram-negative bacteria has recently been investigated. It is highly likely that the presence of efflux pumps may be one of the reasons for the weak activity of non-antibiotics, as in the case of some non-steroidal anti-inflammatory drugs (NSAIDs), against Gram-negative rods. The activity of eight drugs of potential non-antibiotic activity, active substance standards, and relevant medicinal products were analysed with and without of efflux pump inhibitors against 180 strains of five Gram-negative rod species by minimum inhibitory concentration (MIC) value determination in the presence of 1 mM MgSO4. Furthermore, the influence of non-antibiotics on the susceptibility of clinical strains to quinolones with or without PAβN (Phe-Arg-β-naphthylamide) was investigated. The impacts of PAβN on the susceptibility of bacteria to non-antibiotics suggests that amitriptyline, alendronate, nicergoline, and ticlopidine are substrates of efflux pumps in Gram-negative rods. Amitriptyline/Amitriptylinum showed the highest direct antibacterial activity, with MICs ranging 100–800 mg/L against all studied species. Significant decreases in the MIC values of other active substances (acyclovir, atorvastatin, and famotidine) tested with pump inhibitors were not observed. The investigated non-antibiotic medicinal products did not alter the MICs of quinolones in the absence and in the presence of PAβN to the studied clinical strains of five groups of species.http://www.mdpi.com/1420-3049/22/1/114effluxefflux pump inhibitornon-antibioticsmedicinal productsGram-negative bacteriaMDRPAβNdrugsquinolones
spellingShingle Agnieszka E. Laudy
Ewa Kulińska
Stefan Tyski
The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
Molecules
efflux
efflux pump inhibitor
non-antibiotics
medicinal products
Gram-negative bacteria
MDR
PAβN
drugs
quinolones
title The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
title_full The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
title_fullStr The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
title_full_unstemmed The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
title_short The Impact of Efflux Pump Inhibitors on the Activity of Selected Non-Antibiotic Medicinal Products against Gram-Negative Bacteria
title_sort impact of efflux pump inhibitors on the activity of selected non antibiotic medicinal products against gram negative bacteria
topic efflux
efflux pump inhibitor
non-antibiotics
medicinal products
Gram-negative bacteria
MDR
PAβN
drugs
quinolones
url http://www.mdpi.com/1420-3049/22/1/114
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