In vitro/in vivo assessment of the targeting ability of [ 99m Tc] Tc-labeled an aptide specific to the extra domain B of fibronectin (APT EDB ) for colorectal cancer.

Autor: Ranjbar L; Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, 48471-93698, Sari, Mazandaran, Iran.; Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran., Maleki F; Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, 48471-93698, Sari, Mazandaran, Iran.; Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran., Sadeghzadeh N; Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, 48471-93698, Sari, Mazandaran, Iran. nsadeghzadeh@mazums.ac.ir., Abediankenari S; Immunogenetics Research Center, Mazandaran University of Medical Sciences, Sari, Iran., Mardanshahi A; Department of Radiology, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran., Masteri Farahani A; Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, 48471-93698, Sari, Mazandaran, Iran.; Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran.
Jazyk: angličtina
Zdroj: Annals of nuclear medicine [Ann Nucl Med] 2020 Jul; Vol. 34 (7), pp. 460-466. Date of Electronic Publication: 2020 May 10.
DOI: 10.1007/s12149-020-01472-9
Abstrakt: Objective: The APT EDB is an aptide specific to the extra domain B (EDB) of fibronectin with high affinity for EDB, which is expressed in malignant tumors including brain cancer (U87MG) and colorectal cancer (HT-29). Aim of this study was to evaluate the [ 99m Tc] Tc-APT EDB potential as an imaging probe for colorectal cancer.
Methods: Radiochemical purity was evaluated by HPLC and radio-isotope TLC scanner. Blocking study for specific binding assay and affinity calculation (K d ) on HT-29 cell lines were also carried out. Planar imaging and bio-distribution studies were performed in HT-29 tumor-bearing mice.
Results: The APT EDB was efficiently labeled with technetium-99m in high radiochemical yield (up to 97%). Cellular binding study demonstrated specific binding of the [ 99m Tc] Tc-APT EDB in cultured HT-29 cells. The K d value was found to be 40.46 ± 13.39 nM. The tumor-to-muscle ratio was ~ 1.5 in ex vivo bio-distribution study at 1 h after injection. Planar imaging study showed higher activity accumulation in EDB expressing HT-29 tumor relative to muscle (used as control) (~ 1.7) at 1 h.
Conclusions: Although more studies are required to find out the full potential of this radio-ligand as an imaging probe, the present results nevertheless provide useful information about [ 99m Tc] Tc-APT EDB , which might be beneficial in design and development of new [ 99m Tc] Tc-APT EDB for efficient targeting of tumor in vivo.
Databáze: MEDLINE
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