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

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Abstract

Objective

The APTEDB 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 [99mTc] Tc-APTEDB 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 (Kd) 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 APTEDB was efficiently labeled with technetium-99m in high radiochemical yield (up to 97%). Cellular binding study demonstrated specific binding of the [99mTc] Tc-APTEDB in cultured HT-29 cells. The Kd 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 [99mTc] Tc-APTEDB, which might be beneficial in design and development of new [99mTc] Tc-APTEDB for efficient targeting of tumor in vivo.

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Acknowledgements

This work was the subject of the thesis of Leila ranjbar as an M.Sc. student of the Mazandaran University of Medical Sciences and was supported with grant number 1345.

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Authors and Affiliations

  1. Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, 48471-93698, Sari, Mazandaran, Iran

    Leila Ranjbar, Fariba Maleki, Nourollah Sadeghzadeh & Arezou Masteri Farahani

  2. Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran

    Leila Ranjbar, Fariba Maleki & Arezou Masteri Farahani

  3. Immunogenetics Research Center, Mazandaran University of Medical Sciences, Sari, Iran

    Saied Abediankenari

  4. Department of Radiology, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran

    Alireza Mardanshahi

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  1. Leila Ranjbar
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  2. Fariba Maleki
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  3. Nourollah Sadeghzadeh
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  4. Saied Abediankenari
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Correspondence to Nourollah Sadeghzadeh.

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Ranjbar, L., Maleki, F., Sadeghzadeh, N. et al. In vitro/in vivo assessment of the targeting ability of [99mTc] Tc-labeled an aptide specific to the extra domain B of fibronectin (APTEDB) for colorectal cancer. Ann Nucl Med 34, 460–466 (2020). https://doi.org/10.1007/s12149-020-01472-9

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  • DOI: https://doi.org/10.1007/s12149-020-01472-9

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