4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 43, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128102

Keywords

[(TcN)-Tc-99m](2+); Deferoxamine; Dithiocarbamate; Bacterial infection; SPECT; CT imaging

Funding

  1. National Natural Science Foundation of China [21771023, 22076013]
  2. Beijing Municipal Science and Technology Commission [Z181100002218033]

Ask authors/readers for more resources

The 99mTc-labeled deferoxamine radiotracer showed high radiochemical purity and good in vitro stability, with specific binding to bacteria. In mice study, it demonstrated higher uptake in bacterial infection tissues compared to sterile inflammation, suggesting its potential as a bacterial infection imaging radiotracer.
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.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.5
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available