In-Silico Study, Preparation and Biological Evaluation of 99M TC-Mesalamine Complex as Radiotracer for Diagnostics and Monitoring of Ulcerative Colitis in Mice

Pharmaceutical Chemistry Journal(2022)

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摘要
This work centralizes on pursuit ulcerative colitis localized in mice. High radiolabeling and purity were ensured during the formation of a radiotracer, [ 99m Tc]nitrido-mesalamine complex, due to inspecting many parameters under optimum conditions including pH of the reaction mixture (pH 6), reducing agent content (tin(II), 50 μg), reaction time (30 min), mesalamine content (200 μg), Tc-99m (200 – 350 MBq), stability in rat serum (24 h), and reaction temperature (37°C) giving high radiolabeling yield of 98%. In silico molecular docking study was performed to evaluate the possible mechanism of action on the target peroxisome proliferator-activated receptor gamma (PPARγ). Results of biological studies obtained in this work illuminate the usefulness of [ 99m Tc]nitrido-mesalamine complex as a radiotracer that can be used for ulcerative colitis imaging up to 24 h in microbial model (76% dose/g organ (ID/g)) as monitored in mice.
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[ 99m Tc]nitrido-mesalamine complex
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