Author/Authors :
مقدم بناعم، ليلا نويسنده Nuclear Science and Technology Research Institute (NSTRI) Moghaddam-Banaem, Leila , جليليان ، اميررضا نويسنده Jalilian, A.R , جمره، مينا نويسنده Faculty of Nuclear Engineering and Physics, Amirkabir University of Technology, Tehran, Iran Jamre, Mina , سالك، نفيسه نويسنده Faculty of Nuclear Engineering and Physics, Amirkabir University of Technology, Tehran, Iran Salek, Nafise , مزيدي، محمد نويسنده Mazidi, M , قنادي -مراغه، محمد نويسنده Nuclear Science and Technology Research Institute (NSTRI), Ghannadi-Maragheh, Mohammad
Abstract :
Introduction: Due to the anti-proliferative properties of platinum group-thiosemicarbazone complexes, the production of
191Os-labeled 2-acetyl pyridine 4-N-methylthiosemicarbazone (191Os-APMTS) was investigated.
Methods: [191Osmium (T½= 15.4d) was produced via the 190Os(n,?)191Os nuclear reaction using enriched target irradiated
with thermal neutrons. Reaction of in-house synthesized 2-acetylpyridine thiosemicarbazone (APMTS) with 191Os yielded
[191Os]APMTS checked by ITLC followed by stability, partition co-efficient and biodistribution determination.
Results: Following synthesis and spectroscopic determination of the ligand ( > 99% chemical purity), the complex was
prepared with a radiochemical purity of more than 95% (RTLC) and specific activity of 21.5 GB/mM and was stable in the
formulation and presence of human serum at 37°C for up to 48h. The partition coefficient was determined (log P. 1.23). The
biodistribution study up to 4 days demonstrated significant tissue uptake differences in the bone, blood, heart and thyroid.
Conclusion: This is the first Os-191 labeled thiosemicarbazone designed as an in-vivo therapeutic radionuclide generator.
Further investigation is ongoing on the evaluation of the complex in tumor bearing animals.
