Radiolabeling and evaluation of a novel [99mTcN]2+ complex with deferoxamine dithiocarbamate as a potential agent for bacterial infection imaging

Bioorg Med Chem Lett. 2021 Jul 1:43:128102. doi: 10.1016/j.bmcl.2021.128102. Epub 2021 May 10.

Abstract

In order to find a 99mTc-labeled deferoxamine radiotracer for bacterial infection imaging, deferoxamine dithiocarbamate (DFODTC) was successfully synthesized and it was radiolabeled with [99mTcN]2+ core to prepare the 99mTcN(DFODTC)2 complex. 99mTcN(DFODTC)2 was obtained with high radiochemical purity without further purification. The complex was lipophilic and exhibited good in vitro stability. According to the result of bacterial binding study, the binding of 99mTcN(DFODTC)2 to bacteria was specific. Biodistribution in mice study indicated that 99mTcN(DFODTC)2 had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses at 120 min after injection, which showed that the radiotracer could differentiate between bacterial infection and sterile inflammation. SPECT/CT images showed that there was a clear accumulation in infection sites, suggesting that 99mTcN(DFODTC)2 could be a potential bacterial infection imaging radiotracer.

Keywords: Bacterial infection; Deferoxamine; Dithiocarbamate; SPECT/CT imaging; [(99m)TcN](2+).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bacterial Infections / diagnostic imaging*
  • Deferoxamine / chemistry*
  • Inflammation / diagnostic imaging
  • Mice
  • Molecular Structure
  • Organotechnetium Compounds / chemical synthesis
  • Organotechnetium Compounds / chemistry*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Thiocarbamates / chemistry*

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Thiocarbamates
  • Deferoxamine