<sup>68</sup>Ga‐labeled Ciprofloxacin Conjugates as Radiotracers for Targeting Bacterial Infection

Satpati, Drishty; Arjun, Chanda; Repaka, Krishnamohan; Samuel, Grace; Banerjee, Sharmila

doi:10.1111/cbdd.12701

Cited by 25 publications

(36 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These molecules can be accumulated by different mechanisms at the site of infection site. Therefore, the tiny amount of broad spectrum antibiotics has been evaluated as an infection-seeking imaging agent 17,18 .…”

Section: Discussionmentioning

confidence: 99%

Untitled

2017

IJPSR

View full text Add to dashboard Cite

ABSTRACT:The early identification of infection from sterile inflammation is still challenging step in nuclear medicine. Therefore, several radiopharmaceutical agents have been examined to find the solution of this dilemma in clinical practice. Recently Tc-Ofloxacin was undertaken by thin layer chromatography (TLC) and Radio high performance liquid chromatography (Radio-HPLC) analysis. Twenty adult, male NMRI rats were randomly divide into two groups equally. Infection was induced by S. aureus and sterile inflammation created by Carrageenan test. Then radioisotope studies have been performed after intravenous administration of radiotracer into the contra lateral tail vein in all studies. TLC and Radio-HPLC investigations indicated that the infectionseeking radiotracer could be prepared with appropriate yield. All lesions were visualized by scintigraphy imaging. The quality of images was good and did not change with over time. The sensitivity, specificity and positive predictive value of imaging with new developed radiotracer were 100, 50 and 50 % respectively. In spite of high sensitivity of radionuclide imaging with 99m Tc-Ofloxacin to localize induced lesions, it could not demonstrate to distinct infection from sterile inflammation foci. The other medical modalities must be considered for intelligent interpretation of images if the new developed radiotracer will be introduced as an infection-seeking radiopharmaceutical in clinical practice.

show abstract

Section: Discussionmentioning

confidence: 99%

Untitled

2017

IJPSR

View full text Add to dashboard Cite

show abstract

“…In an initial report, 58 bifunctional chelating agents that bind Ga were attached to the C7 end of ciprofloxacin using a propylamine linker. In this study, two derivatives of ciprofloxacin were generated, one with [2-(p-isothiocyanato)-1,4,7,10-tetraazacyclo-dodecane-1,4,7,10-tetraacetic acid] (p-SCN-Bz-DOTA), shown as compound 17 in Fig.…”

Section: Labeling Fluoroquinolones With Galliummentioning

confidence: 99%

Fluoroquinolones as imaging agents for bacterial infection

Naqvi

Drlica

2017

Dalton Trans.

View full text Add to dashboard Cite

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.

show abstract

“…In rats 99m Tc-ciprofloxacin showed an excellent biodistribution with renal clearance, and targeting experiments showed a high sensitivity but low specificity. Ciprofloxacin was also conjugated with propylamine and then labelled with 68 Ga, revealing to be a good bacteria-specific imaging agent in a S. aureus infected rat model [16–18]. …”

Section: Ciprofloxacinmentioning

confidence: 99%

Imaging bacteria with radiolabelled quinolones, cephalosporins and siderophores for imaging infection: a systematic review

Auletta

Galli

Lauri

et al. 2016

Clin Transl Imaging

View full text Add to dashboard Cite

Bacterial infections are still one of the main causes of patient morbidity and mortality worldwide. Nowadays, many imaging techniques, like computed tomography or magnetic resonance imaging, are used to identify inflammatory processes, but, although they recognize anatomical modifications, they cannot easily distinguish bacterial infective foci from non bacterial infections. In nuclear medicine, many efforts have been made to develop specific radiopharmaceuticals to discriminate infection from sterile inflammation. Several compounds (antimicrobial peptides, leukocytes, cytokines, antibiotics…) have been radiolabelled and tested in vitro and in vivo, but none proved to be highly specific for bacteria. Indeed factors, including the number and strain of bacteria, the infection site, and the host condition may affect the specificity of tested radiopharmaceuticals. Ciprofloxacin has been proposed and intensively studied because of its easy radiolabelling method, broad spectrum, and low cost, but at the same time it presents some problems such as low stability or the risk of antibiotic resistance. Therefore, in the present review studies with ciprofloxacin and other radiolabelled antibiotics as possible substitutes of ciprofloxacin are reported. Among them we can distinguish different classes, such as cephalosporins, fluoroquinolones, inhibitors of nucleic acid synthesis, inhibitors of bacterial cell wall synthesis and inhibitors of protein synthesis; then also others, like siderophores or maltodextrin-based probes, have been discussed as bacterial infection imaging agents. A systematic analysis was performed to report the main characteristics and differences of each antibiotic to provide an overview about the state of the art of imaging infection with radiolabelled antibiotics.

show abstract

⁶⁸Ga‐labeled Ciprofloxacin Conjugates as Radiotracers for Targeting Bacterial Infection

Cited by 25 publications

References 26 publications

Untitled

Untitled

Fluoroquinolones as imaging agents for bacterial infection

Imaging bacteria with radiolabelled quinolones, cephalosporins and siderophores for imaging infection: a systematic review

Contact Info

Product

Resources

About

68Ga‐labeled Ciprofloxacin Conjugates as Radiotracers for Targeting Bacterial Infection

Cited by 25 publications

References 26 publications

Untitled

Untitled

Fluoroquinolones as imaging agents for bacterial infection

Imaging bacteria with radiolabelled quinolones, cephalosporins and siderophores for imaging infection: a systematic review

Contact Info

Product

Resources

About

⁶⁸Ga‐labeled Ciprofloxacin Conjugates as Radiotracers for Targeting Bacterial Infection