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Synthesis and biodistribution of a novel (⁹⁹m)TcN complex of norfloxacin dithiocarbamate as a potential agent for bacterial infection imaging.

Abstract
Achieving a (⁹⁹m)Tc-labeled fluoroquinolone derivative as a single photon emission computed tomography (SPECT) tracer is considered to be of great interest. The norfloxacin dithiocarbamate (NFXDTC) was synthesized and radiolabeled with a [(⁹⁹m)TcN]²(+) intermediate to form the (⁹⁹m)TcN-NFXDTC complex in high yield. The radiochemical purity of (⁹⁹m)TcN-NFXDTC was over 90%, as measured by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC), without any notable decomposition at room temperature over a period of 6 h. The partition coefficient and electrophoresis results indicated that (⁹⁹m)TcN-NFXDTC was lipophilic and neutral. The bacterial binding assay studies showed tht (⁹⁹m)TcN-NFXDTC had a good binding affinity. Biodistribution results in bacterial infected mice showed that (⁹⁹m)TcN-NFXDTC had a higher uptake at the sites of infection and better abscess/blood and abscess/muscle ratios than those of (⁹⁹m)Tc-ciprofloxacin and (⁹⁹m)TcN-CPFXDTC (CPFXDTC = ciprofloxacin dithiocarbamate). The biodistribution results of (⁹⁹m)TcN-NFXDTC in bacterially infected mice and in mice with turpentine-induced abscesses indicated that (⁹⁹m)TcN-NFXDTC was suited to be a bacteria-specific infection imaging agent. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in infection sites, suggesting that it would be a promising candidate for bacterial infection imaging.
AuthorsShijian Zhang, Weifang Zhang, Yue Wang, Zhonghui Jin, Xuebin Wang, Junbo Zhang, Yanyan Zhang
JournalBioconjugate chemistry (Bioconjug Chem) Vol. 22 Issue 3 Pg. 369-75 (Mar 16 2011) ISSN: 1520-4812 [Electronic] United States
PMID21319731 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Ligands
  • Organotechnetium Compounds
  • norfloxacin dithiocarbamate
  • Norfloxacin
Topics
  • Animals
  • Bacterial Infections (diagnostic imaging)
  • Drug Stability
  • Electrophoresis, Paper
  • Inflammation (diagnostic imaging)
  • Isotope Labeling
  • Ligands
  • Male
  • Mice
  • Norfloxacin (analogs & derivatives, chemical synthesis, chemistry, pharmacokinetics)
  • Organotechnetium Compounds (chemistry)
  • Rabbits
  • Tomography, Emission-Computed, Single-Photon (methods)

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