99mTc-radiolabeled imidazo[2,1-b]benzothiazole derivatives as potential radiotracers for glioblastoma

This study presents [^99mTc]BPTG-1 and [^99mTc]BPTG-2 for glioblastoma imaging. In vitro cellular uptakes of these radiotracers were examined in SKOV-3, MCF-7, U87-MG, HT-29, and A549 cell lines. U87-MG cell line displayed the highest radiotracers uptakes. Biodistribution study in U87-MG tumor bearing mice revealed higher uptake of radiotracers in tumor than muscle and brain. Liver, intestine, and kidneys displayed the highest radioactivity uptakes. The main route of radiotracers elimination was hepatobiliary. Due to the brain uptake of these radiotracers, they are promising radiotracers for future studies in the diagnosis of glioblastoma.

     

Preparation and biodistribution study of technetium-99m-labeled quercetin as a potential radical scavenging agent

Free radicals and oxidative stress are the primary causes of several chronic diseases such as cancer and heart disease. Quercetin is a natural compound with potent antioxidant activity. We have prepared and evaluated technetium-99m (^99mTc)-labeled quercetin as a potential radical scavenging radiotracer. A ^99mTc-quercetin complex was prepared using quercetin, SnCl₂ and Na^99mTcO₄ in a buffered solution over 30 min. The participation coefficient was measured in octanol and queues solutions. The stability was determined in phosphate buffered saline and serum. The biodistribution in normal mice was evaluated at 0.5, 2, 6 and 24 h post-injection. The radiochemical purity (>99%) was determined by thin layer chromatography (TLC) in normal saline solution as the mobile phase. It has a log P of 0.204. It was mainly cleared by the kidneys and showed negligible brain uptake at four time points measured post-injection. The pharmacological properties of quercetin, mainly its free radical scavenging, may potentially cat as a radiopharmaceutical agent for radical-targeted imaging of tissue with high levels of reactive oxygen species.