Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Molecules. 2020 Dec 10;25(24):5837. doi: 10.3390/molecules25245837.

Abstract

In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [99mTcN]2+ core to obtain the 99mTcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that 99mTcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that 99mTcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation. Compared to 99mTcN-CPFXDTC, the abscess/blood and abscess/muscle ratios of 99mTcN-CPF2XT were higher and the uptakes of 99mTcN-CPF2XT in the liver and lung were obviously decreased. The results suggested that 99mTcN-CPF2XT would be a potential bacterial infection imaging agent.

Keywords: 99mTc-radiolabeling; ciprofloxacin xanthate; infection imaging; quinolones.

MeSH terms

  • Animals
  • Bacterial Infections / diagnostic imaging*
  • Bacterial Infections / microbiology
  • Chemical Phenomena
  • Chemistry Techniques, Synthetic
  • Ciprofloxacin / chemistry*
  • Drug Design*
  • Isotope Labeling
  • Mice
  • Molecular Imaging* / methods
  • Molecular Structure
  • Organotechnetium Compounds / chemistry*
  • Organotechnetium Compounds / isolation & purification
  • Radiopharmaceuticals / chemistry*
  • Technetium / chemistry*
  • Tissue Distribution

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Ciprofloxacin
  • Technetium