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

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Pharmaceutical Chemistry Journal Aims and scope

This work centralizes on pursuit ulcerative colitis localized in mice. High radiolabeling and purity were ensured during the formation of a radiotracer, [99mTc]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 [99mTc]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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CONFLICT OF INTEREST

The authors declare that they have no conflicts of interest.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Laboratories Center, Egyptian Atomic Energy Authority, P. O. Box 13759, Cairo, Egypt

    M. H. Sanad & F. A. Marzook

  2. College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, Gansu, China

    S. F. A. Rizvi

  3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, 12578, Egypt

    A. B. Farag

Authors
  1. M. H. Sanad
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  2. S. F. A. Rizvi
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  3. F. A. Marzook
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  4. A. B. Farag
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Correspondence to M. H. Sanad.

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Sanad, M.H., Rizvi, S.F.A., Marzook, F.A. et al. In-Silico Study, Preparation and Biological Evaluation of 99MTC-Mesalamine Complex as Radiotracer for Diagnostics and Monitoring of Ulcerative Colitis in Mice. Pharm Chem J 56, 754–761 (2022). https://doi.org/10.1007/s11094-022-02706-y

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  • DOI: https://doi.org/10.1007/s11094-022-02706-y

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