&lt;i&gt;In vitro&lt;/i&gt; Investigations with Oxolinic Acid, a New Chemotherapeutic Agent

Neussel, H; Linzenmeier, G

doi:10.1159/000221269

Cited by 7 publications

(3 citation statements)

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“…Oxolinic acid has activity against several Enterobacterales, including Escherichia coli and indole‐positive Proteus species, but demonstrates only little activity against P. aeruginosa . It also possesses in vitro activity for Staphylococcus aureus but has no activity for other Gram‐positive aerobic cocci (Neussel and Linzenmeier, 1973 ; Gleckman et al., 1979 ). Oxolinic acid is about 10‐fold more active than the structurally related nalidixic acid (Staudenbauer, 1976 ).…”

Section: Introductionmentioning

confidence: 99%

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Koutsoumanis¹,

Allende²,

Álvarez‐Ordóñez³

et al. 2021

EFS2

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The specific concentrations of flumequine and oxolinic acid in non-target feed for food-producing animals, below which there would not be an effect on the emergence of, and/or selection for, resistance in bacteria relevant for human and animal health, as well as the specific antimicrobial concentrations in feed which have an effect in terms of growth promotion/increased yield were assessed by EFSA in collaboration with EMA. Details of the methodology used for this assessment, associated data gaps and uncertainties, are presented in a separate document. To address antimicrobial resistance, the Feed Antimicrobial Resistance Selection Concentration (FARSC) model developed specifically for the assessment was applied. However, due to the lack of data on the parameters required to calculate the FARSC, it was not possible to conclude the assessment until further experimental data are available. To address growth promotion, data from scientific publications obtained from an extensive literature review were used. No suitable data for the assessment were available. It was recommended to carry out studies to generate the data that are required to fill the gaps which prevented the calculation of the FARSC for these antimicrobials.

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Section: Introductionmentioning

confidence: 99%

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Koutsoumanis¹,

Allende²,

Álvarez‐Ordóñez³

et al. 2021

EFS2

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“…Oxolinic acid (5-ethyl-5,8-dihydro-8-oxo-l,3 dioxolo[4,5-g]quinoline-7-carboxylic acid, Figure 1A) is a first generation quinolone, developed by Warner-Lambert, approved by the FDA in the 1970s for the treatment of bacterial urinary infections not associated with bacteremia in adults [24]. The spectrum of activity is rather narrow and includes some Gram-negative bacteria [25][26][27]. Still, it has not proven itself to be more effective or better tolerated than other drugs such as nalidixic acid, ampicillin or trimethoprim-sulfamethoxazole [24,28,29].…”

Section: Introductionmentioning

confidence: 99%

Rare-Earth Metal Complexes of the Antibacterial Drug Oxolinic Acid: Synthesis, Characterization, DNA/Protein Binding and Cytotoxicity Studies

Măciucă

Arbănași

Mihăilă³

et al. 2020

Molecules

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“Drug repositioning” is a current trend which proved useful in the search for new applications for existing, failed, no longer in use or abandoned drugs, particularly when addressing issues such as bacterial or cancer cells resistance to current therapeutic approaches. In this context, six new complexes of the first-generation quinolone oxolinic acid with rare-earth metal cations (Y3+, La3+, Sm3+, Eu3+, Gd3+, Tb3+) have been synthesized and characterized. The experimental data suggest that the quinolone acts as a bidentate ligand, binding to the metal ion via the keto and carboxylate oxygen atoms; these findings are supported by DFT (density functional theory) calculations for the Sm3+ complex. The cytotoxic activity of the complexes, as well as the ligand, has been studied on MDA-MB 231 (human breast adenocarcinoma), LoVo (human colon adenocarcinoma) and HUVEC (normal human umbilical vein endothelial cells) cell lines. UV-Vis spectroscopy and competitive binding studies show that the complexes display binding affinities (Kb) towards double stranded DNA in the range of 9.33 × 104 − 10.72 × 105. Major and minor groove-binding most likely play a significant role in the interactions of the complexes with DNA. Moreover, the complexes bind human serum albumin more avidly than apo-transferrin.

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“…Data suggest that the 5-,ug disk more satisfactorily fulfills requirements for susceptibility testing than the 1-or 2-,g disks evaluated. Ultraviolet spectral analysis studies for absorption maxima and extinction coefficients were done to verify the authenticity and concentration of oxolinic acid in the aqueous solutions studied.Previous studies (1,3,8,12,13; R. Shapera and J. M. Matsen, Am. J. Dis.…”

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In Vitro Susceptibility Comparisons and Recommendations for Oxolinic Acid

Klein¹,

Matsen

1976

Antimicrob Agents Chemother

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Minimal inhibitory concentration and disk diffusion susceptibility studies were carried out with oxolinic acid to determine a recommended disk content for disk susceptibility testing. Regression curve analyses were performed with disks containing 1, 2, and 5 ug of oxolinic acid. Data suggest that the 5-,ug disk more satisfactorily fulfills requirements for susceptibility testing than the 1-or 2-,g disks evaluated. Ultraviolet spectral analysis studies for absorption maxima and extinction coefficients were done to verify the authenticity and concentration of oxolinic acid in the aqueous solutions studied.Previous studies (1,3,8,12,13; R. Shapera and J. M. Matsen, Am. J. Dis. Child., in press) of the in vitro activity of the newly available antimicrobial drug, oxolinic acid, have shown wide variations in the reported values for minimal inhibitory concentrations and disk diffusion inhibitory zone sites. In some cases the standard methods were not followed, but analysis of these studies would indicate that discrepancies in the concentration of antimicrobial agents may have played a role, since oxolinic acid is indeed difficult to uniformly bring into solution. With the aid of ultraviolet spectral analysis studies for absorption maxima and extinction coefficients, in addition to standardized susceptibility test methods, the study reported here attempts to establish the true activity of oxolinic acid and to ascertain the disk content most suitable for use in disk diffusion susceptibility tests. Currently, the 2-,ug disk is used for susceptibility testing.MATERIALS AND METHODS Organisms. One hundred and ninety-nine (199) bacterial strains representing 16 genera were tested for susceptibility of oxolinic acid. These organisms were identified by standard procedures (4, 9) in the Diagnostic Microbiology Laboratory of the University of Minnesota Hospitals and were maintained as stock cultures in the dark on sealed Trypticase soy agar deeps at ambient room temperatures.Antimicrobial susceptibility testing. Inoculum from an overnight culture of each strain was incubated for 4 h at 35 C in tryptose phosphate broth. Cultures were then standardized against a 0.5 MacFarland BaSO, standard, which has an opacity I Present address: Duke University Medical Center, Durham, N.C. 27710. equivalent to between 5.0 x 107 and 4.0 x 108 organisms (11)/ml. Disk diffusion tests were run in duplicate using the standard Food and Drug Administration single high concentration disk method (2, 6, 7). Three strengths of commercially prepared paper disks impregnated with 1.0, 2.0, and 5.0 j,g of oxolinic acid were used. The duplicate diffusion zone values for each disk strength were read by two observers, and the four values obtained were averaged to arrive at the accepted disk zone size. Agar dilution studies were performed with Mueller-Hinton agar media according to the International Collaborative Study Method (5) using the replicating device of Steers et al. (13). Swarming strains of Proteus were contained in clear plastic Raschig rings. Minima...

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<i>In vitro</i> Investigations with Oxolinic Acid, a New Chemotherapeutic Agent

Cited by 7 publications

References 3 publications

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Rare-Earth Metal Complexes of the Antibacterial Drug Oxolinic Acid: Synthesis, Characterization, DNA/Protein Binding and Cytotoxicity Studies

In Vitro Susceptibility Comparisons and Recommendations for Oxolinic Acid

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<i>In vitro</i> Investigations with Oxolinic Acid, a New Chemotherapeutic Agent

Cited by 7 publications

References 3 publications

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Rare-Earth Metal Complexes of the Antibacterial Drug Oxolinic Acid: Synthesis, Characterization, DNA/Protein Binding and Cytotoxicity Studies

In Vitro Susceptibility Comparisons and Recommendations for Oxolinic Acid

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Product

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Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid

Maximum levels of cross‐contamination for 24 antimicrobial active substances in non‐target feed. Part 10: Quinolones: flumequine and oxolinic acid