Radiosynthesis, molecular modeling studies and biological evaluation of 99mTc-Ifosfamide complex as a novel probe for solid tumor imaging
Motaleb M.A.; El-Safoury D.M.; Abd-Alla W.H.; Awad G.A.S.; Sakr T.M.
Date issued:
2018
Publisher:
Taylor and Francis Ltd
Series Info:
International Journal of Radiation Biology
94
Type:
Article
Keywords:
October University for Modern Sciences and Arts
,
جامعة أكتوبر للعلوم الحديثة والآداب
,
University of Modern Sciences and Arts
,
MSA University
,
Ifosfamide
,
imaging
,
labeling
,
technetium-99m
,
tumor targeting
,
ifosfamide
,
ifosfamide complex tc 99m
,
radiopharmaceutical agent
,
technetium 99m
,
unclassified drug
,
DNA topoisomerase
,
ifosfamide
,
technetium
,
animal experiment
,
animal model
,
animal tissue
,
Article
,
complex formation
,
computer simulation
,
controlled study
,
drug distribution
,
drug DNA interaction
,
drug screening
,
drug stability
,
drug synthesis
,
female
,
in vitro study
,
in vivo study
,
isotope labeling
,
molecular docking
,
molecular imaging
,
molecular model
,
mouse
,
nonhuman
,
priority journal
,
radiochemistry
,
solid malignant neoplasm
,
animal
,
chemistry
,
human
,
kinetics
,
metabolism
,
molecular docking
,
molecular imaging
,
procedures
,
protein domain
,
synthesis
,
tissue distribution
,
Animals
,
DNA Topoisomerases, Type I
,
Drug Stability
,
Humans
,
Ifosfamide
,
Kinetics
,
Mice
,
Molecular Docking Simulation
,
Molecular Imaging
,
Protein Domains
,
Radiochemistry
,
Technetium
,
Tissue Distribution
Abstract:
Purpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. Materials and methods: The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 ?g of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. Results: A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3. 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ?3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. Conclusion: These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging. 2018, Copyright 2018 Taylor & Francis Group, LLC.
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