Preparation and Biological Evaluation of 67Gallium- Labeled Iranian Hemiscorpius Lepturus Scorpion Venom

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Author(s): Amir Jalali*, Mona Haddad Zahmatkesh, Amir Reza Jalilian, Amir Taheri Borujeni, Behrouz Alirezapour.

Journal Name: Current Radiopharmaceuticals

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Background: The Hemiscorpius lepturus (H. lepturus), a deadly scorpion species living in the southern Iran. Objective: H. lepturus induces delayed toxicity symptoms and understanding the long term biodistribution/biokinetic of the venom is of great interest in toxinology.

Methods: A Ga-67 labeled venom was prepared using a DOTA -conjugated venom followed by radiolabeling using 67GaCl3 at 40 ̊C in 90 min. The purification of the radiolabeled venom was performed using size exclusion-chromatography (radiochemical purity 71%). The radiolabeled venom was stable in the final solution and the presence of human serum at 37 ̊C for 72 hours. The tissue distribution was studied in blood, heart, liver, spleen, muscle, brain, kidney, intestine and skin tissues at intervals of 1, 4, 24, 48 and 72 hours using tissue counting and SPECT imaging. Results: The radiolabeld venom mixture obtained with an estimated molar activity of 0.52 MBq/µg. The main accumulation tissues during the first 72 hours were kidneys, blood, liver, intestines, stomach and skin, respectively. Therefore, it is likely that H. lepturus’ clinical effects and renal toxicity are primary and caused by direct effects of the H. lepturus venom.

Conclusion: The results have largely shown the direct clinical effects on the studied tissues during the 72-hour period and antivenom administration can strongly alleviate the toxicity effects as early as 72 hours in the management of the patients.

Keywords: Hemiscorpius lepturus, Scorpion venom, Gallium-67, Radiolabeling, SPECT

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(E-pub Ahead of Print)
DOI: 10.2174/1874471012666190828155227