Medicinal Potential of Ciprofloxacin and Its Derivatives

Castro, William; Navarro, Maribel; Biot, Christophe

doi:10.4155/fmc.12.181

Cited by 61 publications

(42 citation statements)

References 99 publications

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“…Folate auxotrophy in lactobacilli is generally accepted as the intrinsic cause of resistance to trimethoprim [39]. Similarly, reduced affinity of DNA gyrase (GyrA) and topoisomerase IV (ParC) variants for ciprofloxacin and other fluoroquinolones seen in some LAB species has been determined responsible for their insensitivity to this class of antibiotics [40]. Further, the presence of active multidrug efflux systems could contribute to an increase in the MIC for ciprofloxacin in some strains [21].…”

Section: Discussionmentioning

confidence: 99%

Antibiotic Susceptibility Profiles of Lactic Acid Bacteria from the Human Vagina and Genetic Basis of Acquired Resistances

Sirichoat

Flórez

Vázquez

et al. 2020

IJMS

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Lactic acid bacteria can act as reservoirs of antibiotic resistance genes that can be ultimately transferred to pathogens. The present work reports on the minimum inhibitory concentration (MIC) of 16 antibiotics to 25 LAB isolates of five Lactobacillus and one Bifidobacterium species from the human vagina. Acquired resistances were detected to kanamycin, streptomycin, chloramphenicol, gentamicin, and ampicillin. A PCR analysis of lactobacilli failed to identify genetic determinants involved in any of these resistances. Surprisingly, a tet(W) gene was detected by PCR in two Bifidobacterium bifidum strains, although they proved to be tetracycline-susceptible. In agreement with the PCR results, no acquired genes were identified in the genome of any of the Lactobacillus spp. strains sequenced. A genome analysis of B. bifidum VA07-1AN showed an insertion of two guanines in the middle of tet(W) interrupting the open reading frame. By growing the strain in the presence of tetracycline, stable tetracycline-resistant variants were obtained. An amino acid substitution in the ribosomal protein S12 (K43R) was further identified as the most likely cause of VA07-1AN being streptomycin resistance. The results of this work expand our knowledge of the resistance profiles of vaginal LAB and provide evidence for the genetic basis of some acquired resistances.

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Section: Discussionmentioning

confidence: 99%

Antibiotic Susceptibility Profiles of Lactic Acid Bacteria from the Human Vagina and Genetic Basis of Acquired Resistances

Sirichoat

Flórez

Vázquez

et al. 2020

IJMS

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“…Ciprofloxacin is commonly used for the treatment of a number of infections such as acute uncomplicated cystitis, urinary tract infections, acute sinusitis, and chronic bacterial prostatitis. 6 The mechanism of antibacterial action of quinolone, including ciprofloxacin, involves interfering with replication and transcription of DNA via inhibiting bacterial DNA gyrase/topoisomerase II and DNA topoisomerase IV, and further preventing DNA of bacteria from unwinding and duplicating. 7 Thus, complexes of quinolone-enzyme-DNA are formed, leading to the production of cellular poisons and cell death.…”

Section: Introductionmentioning

confidence: 99%

Ciprofloxacin-Induced Antibacterial Activity Is Attenuated by Phosphodiesterase Inhibitors

Masadeh

Alzoubi

Khabour

et al. 2015

Current Therapeutic Research

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BackgroundCiprofloxacin is a commonly used antibiotic for urinary tract infection that interacts with bacterial topoisomerases leading to oxidative radicals generation and bacterial cell death. Phosphodiesterase inhibitors (PDEis), on the other hand, are commonly used drugs for the management of erectile dysfunction. The group includes agents such as sildenafil, vardenafil, and tadalafil.ObjectivesWe investigated whether PDEi could interfere with the antibacterial activity of ciprofloxacin.MethodsPDEis were tested in several reference bacteria, including Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus epidermidis, Acinetobacter baumannii, Proteus mirabilis, and Klebsiella pneumoniae utilizing a standard disc diffusion method and measuring both zones of inhibition and MIC.ResultsResults from both assays indicated that ciprofloxacin demonstrates potent activity against the tested reference bacteria. Additionally, when bacteria were treated with a combination of ciprofloxacin and sildenafil, tadalafil, or vardenafil, the zones of the combination inhibition were significantly reduced, whereas the MIC values were significantly greater than those of ciprofloxacin alone for all tested bacterial strains. In an attempt to examine the mechanism by which PDEis interfere with the action of ciprofloxacin, we utilized the in vitro E coli DNA gyrase cleavage assay. The results showed that PDEi drugs had no effect on ciprofloxacin’s inhibition of E coli gyrase activity.ConclusionsPretreatment of various reference bacterial cells with PDEis largely inhibited the antibacterial activity of ciprofloxacin.

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“…Fluoroquinolones such as ciprofloxacin are among the most prescribed antibiotics for the treatment of various infections (24). Their broad-spectrum efficacy is associated with the mechanism of action, which is the inhibition of DNA replication and repair (25).…”

Section: Significancementioning

confidence: 99%

Design and synthesis of theranostic antibiotic nanodrugs that display enhanced antibacterial activity and luminescence

Xie

Manuguri

Proietti

et al. 2017

Proc. Natl. Acad. Sci. U.S.A.

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We report the modular formulation of ciprofloxacin-based pure theranostic nanodrugs that display enhanced antibacterial activities, as well as aggregation-induced emission (AIE) enhancement that was successfully used to image bacteria. The drug derivatives, consisting of ciprofloxacin, a perfluoroaryl ring, and a phenyl ring linked by an amidine bond, were efficiently synthesized by a straightforward protocol from a perfluoroaryl azide, ciprofloxacin, and an aldehyde in acetone at room temperature. These compounds are propeller-shaped, and upon precipitation into water, readily assembled into stable nanoaggregates that transformed ciprofloxacin derivatives into AIE-active luminogens. The nanoaggregates displayed increased luminescence and were successfully used to image bacteria. In addition, these nanodrugs showed enhanced antibacterial activities, lowering the minimum inhibitory concentration (MIC) by more than one order of magnitude against both sensitive and resistant Escherichia coli. The study represents a strategy in the design and development of pure theranostic nanodrugs for combating drug-resistant bacterial infections.nanodrugs | aggregation-induced emission | fluoroquinolones

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Medicinal Potential of Ciprofloxacin and Its Derivatives

Cited by 61 publications

References 99 publications

Antibiotic Susceptibility Profiles of Lactic Acid Bacteria from the Human Vagina and Genetic Basis of Acquired Resistances

Antibiotic Susceptibility Profiles of Lactic Acid Bacteria from the Human Vagina and Genetic Basis of Acquired Resistances

Ciprofloxacin-Induced Antibacterial Activity Is Attenuated by Phosphodiesterase Inhibitors

Design and synthesis of theranostic antibiotic nanodrugs that display enhanced antibacterial activity and luminescence

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