Antistaphylococcal Activities of the New Fluoroquinolone JNJ-Q2

Morrow, Brian J.; Abbanat, Darren; Baum, Ellen Z.; Crespo-Carbone, Steven M.; Davies, Todd A.; He, Wenping; Shang, Wenchi; Queenan, Anne Marie; Lynch, A. Simon

doi:10.1128/aac.00470-11

Cited by 25 publications

(22 citation statements)

References 32 publications

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“…The relative rates or frequencies of the spontaneous development of resistance to JNJ-Q2 at MICs in S. pneumoniae, MRSA, and E. coli were indicative of a lower potential for resistance development than that for current FQLs. In conclusion, JNJ-Q2 exhibits a range of antibacterial activities in vitro that is supportive of its further evaluation as a potential new agent for the treatment of skin and respiratory tract infections [24].…”

Section: Issn: 2380-5021supporting

confidence: 54%

A Mini Review on the Study of New Broad-Spectrum Antimicrobial Fluoroquinolone JNJ-Q2

2014

J Chem Appl

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The prokaryotic type II topoisomerases (DNA gyrase and topoisomerase IV) and the eukaryotic type II topoisomerases represent the cellular targets for quinolone antibacterial and anticancer agents. Both enzymes effort the selectively shift from an antibacterial to an antitumor activity. In the search for potential molecule in the quinolones series, some of quinolone analogs displayed antibacterial and cytotoxic activities. The newly developed quinolone JNJ-Q2 is a broad-spectrum fluoroquinolone, has activity against pathogenic bacteria but its anticancer activity is still disclosed. The studies demonstrated that quinolone series changes the biological profile from antibacterial to cytotoxic activity and have excellent potential as antimicrobial and cytotoxic agents. IntroductionQuinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in humans [1]. They damage the activities of prokaryotic type II topoisomerases, DNA gyrase and topoisomerase IV, and induce them to kill cells by generating high levels of double-stranded DNA breaks. Type II topoisomerases modulate the topological state of the genetic material by passing an intact DNA helix through a transient double stranded break that they generate in a separate DNA segment [2]. Like bacterial cells, eukaryotic species require a type II topoisomerase, known as topoisomerase II, for viability [3]. In addition to the antibacterial quinolones, some quinolones displayed activity against eukaryotic type II topoisomerases, cultured mammalian cells and in vivo tumor models [4]. These antineoplastic quinolones are potentially important as anticancer agents. Several quinolones have been displayed significant activity against eukaryotic type II topoisomerases [5,6]. Quinolones which are built on the ciprofloxacin (CPFX) 1 or norfloxacin (NRFX) 2 nucleus, these selected cytotoxic quinolones 3-5, displayed activity against DNA gyrase or topoisomerase IV. The quinolones are distinguished from the antibacterial quinolones [7,8] and are preferentially target the different prokaryotic and eukaryotic type II topoisomerases [9] (Figure 1). Generations of QuinolonesThe quinolones are divided into generations based on their antibacterial spectrum. The earlier-generation agents are more narrow-spectrum than the later ones. The only standard applied is the grouping of the non-fluorinated drugs found within this quinolones within the 'first-generation' heading. The first generation is rarely used today. A number of the second-, third-, and fourth-generation drugs have been removed from clinical practice due to severe toxicity issues. The drugs most frequently prescribed today consist of moxifloxacin, ciprofloxacin, levofloxacin and, to some extent, their generic equivalents (Figure 2, Figure 3). First-generationVarious first generation quinolones such as cinoxacin, flumequine (veterinary use), nalidixic acid, oxolinic acid, piromidic acid, pipemidic acid, and rosoxacin. Second-generationThe second-generation are ci...

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Section: Issn: 2380-5021supporting

confidence: 54%

A Mini Review on the Study of New Broad-Spectrum Antimicrobial Fluoroquinolone JNJ-Q2

2014

J Chem Appl

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“…The levofloxacin (LVFX) and MFLX minimum inhibitory concentrations (MICs) for ATCC 43300 were 0.16 and 0.03 lg/ml. 27,28 Prior to experimentation, each contact lens was soaked in GFLX eye drop solutions for uptake of the antibiotic. Forty-five Japanese albino rabbits were used for this assay.…”

Section: Prevention Of Bacterial Proliferation In Rabbitsmentioning

confidence: 99%

Development and Efficacy of a Drug-Releasing Soft Contact Lens

Kakisu

Matsunaga²,

Kobayakawa

et al. 2013

Invest. Ophthalmol. Vis. Sci.

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PURPOSE. The purpose of this study was to investigate the uptake and the release of antibiotics from a newly synthesized drug delivery hydrogel soft contact lens (SCL) using an ion ligand mechanism.METHODS. The antibiotics used were Gatifloxacin (GFLX) and Moxifloxacin (MFLX). The uptake amount and the sustained-release kinetics of antibiotics were investigated in vitro, and were also compared with newly synthesized SCLs, etafilcon A and polymacon. The antibiotic concentrations in the cornea, aqueous humor, and crystalline lens, and the effect against bacterial proliferation were investigated in vivo using rabbit subjects. Additionally the drug release efficacy of the new SCL was compared with that of eye drop administrations.RESULTS. In vitro, antibiotic uptake was increased with the weight percent (wt%) of the anionic group, and the released amount of antibiotics was highest during the initial 1 hour period, which then decreased over the next 72 hours. The released antibiotics volume of the new SCLs was significantly higher throughout 72 hours than that of the other two materials, etafilcon A and polymacon (P < 0.01). Whereas in vivo, the concentrations found in the cornea and aqueous humor were higher than those for the eye drop groups (P < 0.05 or P < 0.01). Antibiotic release at those sites decreased over 72 hours. No bacterial populations were detectable in the group treated with the new SCL presoaked in antibiotics throughout the experimental periods. CONCLUSIONS.The new SCLs released the antibiotics over several days, and showed improved penetration into the eye, along with prevention of bacterial proliferation.

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“…Another novel antibiofilm drug was reported by Morrow et al (26). There the benchmark agent was the antibiotic ciprofloxacin, which falls in the middle of the group in the overall dose-response plot for S. aureus (Fig.…”

Section: Measuring Antimicrobial Efficacy Against Biofilmsmentioning

confidence: 98%

Measuring Antimicrobial Efficacy against Biofilms: a Meta-analysis

Stewart

Parker

2019

Antimicrob Agents Chemother

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Through a statistical meta-analysis of published data on antimicrobial efficacy against biofilms formed by two common bacterial species, it was concluded that the particular experimental method used is the most important factor determining the outcome of the test. An expected dose-response relationship (greater killing with higher doses or longer treatment times) was observed for data sets derived from a single method but was not observed when data from multiple studies using diverse methods were pooled. Method-specific properties such as the surface area/ volume ratio, areal biofilm cell density, and microbial species were shown to influence quantitative measurements of biofilm killing. A better appreciation of the method characteristics that affect antibiofilm efficacy tests could aid decision-making related to investment in research and development and regulatory approvals for biofilm control strategies. The following recommendations are offered to those working in research and development related to biofilm control: (i) report the log reduction, surface area/volume ratio, and biofilm areal cell density; (ii) include data for a benchmark agent, making sure that this agent performs competitively at the dose tested; (iii) measure the dose-response relationship, i.e., make measurements at multiple treatment concentrations or dose durations; and (iv) use a standardized method in addition to research methods.

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Antistaphylococcal Activities of the New Fluoroquinolone JNJ-Q2

Cited by 25 publications

References 32 publications

A Mini Review on the Study of New Broad-Spectrum Antimicrobial Fluoroquinolone JNJ-Q2

A Mini Review on the Study of New Broad-Spectrum Antimicrobial Fluoroquinolone JNJ-Q2

Development and Efficacy of a Drug-Releasing Soft Contact Lens

Measuring Antimicrobial Efficacy against Biofilms: a Meta-analysis

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