New rhenium complexes with ciprofloxacin as useful models for understanding the properties of [99mTc]-ciprofloxacin radiopharmaceutical

Lecina, Joan; Cortés, Pilar; Llagostera, Montserrat; Piera, Carlos; Suades, Joan

doi:10.1016/j.bmc.2014.04.058

Cited by 14 publications

(10 citation statements)

References 58 publications

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“…Rhenium ions were also tested in combination with ciprofloxacin ( in vivo ), where they destroyed bacterial cells by disrupting DNA gyrase synthesis (Lecina et al . ). molybdenum‐rhenium coated struts have been used for applications within replacement heart‐valve components (Beall mitral valves) (Ribeiro et al .…”

Section: Resultsmentioning

confidence: 97%

“…Previous work has shown that mono/di-rhenium complexes have demonstrated antimicrobial activity against Gram-positive S. aureus and Gram-negative E. coli (Kumar et al 2016). Rhenium ions were also tested in combination with ciprofloxacin (in vivo), where they destroyed bacterial cells by disrupting DNA gyrase synthesis (Lecina et al 2014). molybdenum-rhenium coated struts have been used for applications within replacement heart-valve components (Beall mitral valves) (Ribeiro et al 2016).…”

Section: Resultsmentioning

confidence: 99%

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Rhenium and yttrium ions as antimicrobial agents against multidrug resistant Klebsiella pneumoniae and Acinetobacter baumannii biofilms

Slate

Shalamanova

Akhidime

2019

Lett Appl Microbiol

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Antimicrobial resistance presents major global concerns to patient health. In this study, metal ions of molybdenum, rhenium, yttrium and thallium were tested against bacteria in planktonic and biofilm form using one strain of Klebsiella pneumoniae and Acinetobacter baumannii. The antimicrobial efficacy of the metal ions was evaluated against the planktonic bacterial strains using minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations, whilst the efficacy of the metal ions against biofilms was tested using a crystal violet biofilm assay. Live Dead staining was used to visualize the antimicrobial activity elicited by the metal ions on the bacterial cell. The results showed that higher concentrations of the metals were required to inhibit the growth of biofilms (72·9 mg l−1 to 416·7 mg l−1), in comparison to their planktonic counterparts. MICs of the metal ions (<46·9 mg l−1) (planktonic cells) did not affect biofilm formation. Overall, rhenium and yttrium were effective antimicrobial agents. Molybdenum demonstrated the greatest level of biotoxicity. When taking into account these results and the known toxicity of thallium, it is possible that rhenium or yttrium ions could be developed as effective biocidal formulations in order to prevent transmission in healthcare environments. Significance and Impact of the Study The metal ions, molybdenum, rhenium, thallium and yttrium were tested against both Klebsiella pneumoniae and Acinetobacter baumannii in planktonic and biofilm forms. This research demonstrated that all the metal ions may be effective antimicrobial agents. However, molybdenum induced high levels of cytotoxicity, whilst, there was no significant difference in the toxicity of the other metal ions tested. When considering the results for the antimicrobial efficacy and biotoxicity of the metal ions, in conjunction with the known toxicity of thallium in certain chemical compositions, it was concluded that overall rhenium or yttrium ions may be effective antimicrobial agents, one potential application may be utilizing these metal ions in hospital surface cleaning formulations.

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Section: Resultsmentioning

confidence: 97%

Section: Resultsmentioning

confidence: 99%

Rhenium and yttrium ions as antimicrobial agents against multidrug resistant Klebsiella pneumoniae and Acinetobacter baumannii biofilms

Slate

Shalamanova

Akhidime

2019

Lett Appl Microbiol

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“…These ternary complexes (cleaved complexes) are the hallmark of quinolone action, as they rapidly block DNA replication and interfere with the movement of transcription complexes. When ciprofloxacin was complexed to rhenium, which is chemically similar to technetium, and then used to study formation of the drug-gyrase-DNA complexes, 24 the Re-ciprofloxacin reagent was at least 100-fold less active than free ciprofloxacin (interaction with gyrase could be even lower than reported, because release of free ciprofloxacin from the Re-ciprofloxacin complex could have contributed to the apparent, low-level activity).…”

Section: Interaction Of 99mtc-ciprofloxacin With Bacterial Cellsmentioning

confidence: 99%

Fluoroquinolones as imaging agents for bacterial infection

Naqvi

Drlica

2017

Dalton Trans.

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Diagnosis of deep-seated bacterial infection is difficult, as neither standard anatomical imaging nor radiolabeled, autologous leukocytes distinguish sterile inflammation from infection. Two recent imaging efforts are receiving attention: 1) radioactive derivatives of sorbitol show good specificity with Gram-negative infections, and 2) success from combining anatomical and functional imaging for cancer diagnosis has rekindled interest in 99mTc-fluoroquinolone-based imaging. With the latter, computed tomography (CT) would be combined with single-photon-emission-computed tomography (SPECT) to detect a 99mTc-fluoroquinolone-bacterial interaction. The present minireview provides a framework for advancing with fluoroquinolone-based imaging by identifying gaps in our understanding of the process. One issue is the reliance of 99mTc labeling on reduction of sodium pertechnetate, which can lead to colloid formation and loss of specificity. Specificity problems may be reduced by altering quinolone structure (an example is switching from ciprofloxacin to sitafloxacin). Another issue is the uncharacterized nature of 99mTc-ciprofloxacin binding to, or sequestration in, bacteria -- specific interactions with DNA gyrase, an intracellular fluoroquinolone target, are unlikely. Replacing the C6-F of the fluoroquinolone with 18F provides an alternative to pertechnetate that may lead to imaging based on drug interactions with gyrase. Gyrase-based imaging requires knowledge of fluoroquinolone action, which we update. We conclude that quinolone-based probes show promise for diagnosis of bacterial infection, but improvements in specificity and sensitivity are needed. Those improvements require optimization of quinolone structure and reduction of pertechnetate, chemistry efforts that can be accelerated by refining microbiological assays.

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“…They have a bactericidal effect and are therefore used to treat bacterial infections. The structure of quinolones allows various modifications to the molecule to be introduced without it losing its properties and therapeutic effect [13], so they are applied in radiopharmaceuticals for imaging bacterial infections after labelling with 99m Tc [11,[14][15][16][17][18] or 18 F [10,19,20].…”

Section: Introductionmentioning

confidence: 99%

Physicochemical and Biological Study of 99mTc and 68Ga Radiolabelled Ciprofloxacin and Evaluation of [99mTc]Tc-CIP as Potential Diagnostic Radiopharmaceutical for Diabetic Foot Syndrome Imaging

et al. 2021

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This paper presents the application of ciprofloxacin as a biologically active molecule (vector) for delivering diagnostic radiopharmaceuticals to the sites of bacterial infection. Ciprofloxacin-based radioconjugates containing technetium-99m or gallium-68 radionuclides were synthesised, and their physicochemical (stability, lipophilicity) and biological (binding study to Staphylococcus aureus and Pseudomonas aeruginosa) properties were investigated. Both the tested radiopreparations met the requirements for radiopharmaceuticals, and technetium-99m-labelled ciprofloxacin turned out to be a good radiotracer for the tomography of diabetic foot syndrome using SPECT.

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New rhenium complexes with ciprofloxacin as useful models for understanding the properties of [99mTc]-ciprofloxacin radiopharmaceutical

Cited by 14 publications

References 58 publications

Rhenium and yttrium ions as antimicrobial agents against multidrug resistant Klebsiella pneumoniae and Acinetobacter baumannii biofilms

Rhenium and yttrium ions as antimicrobial agents against multidrug resistant Klebsiella pneumoniae and Acinetobacter baumannii biofilms

Fluoroquinolones as imaging agents for bacterial infection

Physicochemical and Biological Study of 99mTc and 68Ga Radiolabelled Ciprofloxacin and Evaluation of [99mTc]Tc-CIP as Potential Diagnostic Radiopharmaceutical for Diabetic Foot Syndrome Imaging

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