Abstract
Antineoplastons (ANPs) are compounds that have antitumor activities. ANPA10 was labeled with technetium-99m using stannous chloride as a reducing agent with the labeling yield of approximately 98% at pH 6. The conditions required to optimize the labeling yield were studied in details. The tumor binding specificity of the [99mTc]Tc-ANPA10 radiotracer was evaluated. The uptake of [99mTc]Tc-ANPA10 in ascitic fluid uptake was 10, 16, and 12.8% ID/g at 30, 60, and 120 min post injection. The preclinical biological evaluation of [99mTc]Tc-ANPA10 complex in solid tumor bearing mice showed a high tumor uptake at 1 h post injection (11.2 ± 0.30 % ID/g). The selective uptake of [99mTc]Tc-ANPA10 in solid tumors and rapid clearance from nontarget organs make it promising for solid tumor imaging, but further clinical trials are required.
Similar content being viewed by others
REFERENCES
Aboumanei, M.H., Abdelbary, A.A., Ibrahim, I.T., Tadros, M.I., and El-Kolaly, M.T., Int. J. Pharm., 2018, vol. 545, nos. 1–2, pp. 240–253.
Aboumanei, M.H., Abdelbary, A.A., Ibrahim, I.T., Tadros, M.I., and El-Kolaly, M.T., Cancer Biother. Radiopharm., 2018, vol. 33, no. 6, pp. 221–232.
Figg, W.D., Lancet Oncol., 2018, vol. 19, no. 6, pp. 733–734. https://doi.org/10.1016/S1470-2045(18)30338-3
Badria, F., Mabed, M., El-Awadi, M., Abou-Zeid, L., Al-Nashar, E., and Hawas, S., Cancer Lett., 2000, vol. 157, no. 1, pp. 57–63.
Burzynski, S.R., Efficacy of antineoplastons A-10 and AS2-1, in Mayo Clinic Proc.,Amsterdam: Elsevier, 1999.
Sołtysiak-Pawłuczuk, D. and Burzyński, S.R., Cancer Lett., 1995, vol. 88, no. 1, pp. 107–112.
Othman, S.A. et al., ALL AUTHORS IOP Conf. Ser. Mater. Sci. Eng., 2019. Vol. 555, ID 012032.
Binion, A.K., Radiopharmaceuticals: the Application of Technetium-99m and Rhenium Complexes, A Capstone Project Submitted in Partial Fulfillment of the Requirements of the Renée Crown University Honors Program at Syracuse University, Syracuse, 2014.
NIH (National Institutes of Health) Guide for the Care and Use of Laboratory Animals, Washington, DC: National Academy, 1996, 7th ed.
El-Kawy, O., Ibrahim, I., and Farah, K., J. Label. Compd. Radiopharm., 2015, vol. 58, no. 8, pp. 336–341.
El-Kawy, O. and Talaat, H., J. Label. Compd. Radiopharm., 2016, vol. 59, no. 2, pp. 72–77.
Hoye, A., J. Chromatogr, 1967, vol. 28, no. 2, pp. 379–384. https://doi.org/10.1016/s0021-9673(01)85979-3
Rajkapoor, B., Jayakar, B., and Murugesh, N., Indian J. Pharmacol., 2004, vol. 36, pp. 38–40.
Abd El-Rahman, A.M., Mohamed, A.A., Mohamed, S.A., and Mostafa, M.A., Pain Med., 2018, vol. 19, no. 3, pp. 561–568.
Motaleb, M. and Sakr, T., J. Label. Compd. Radiopharm., 2011, vol. 54, no. 9, pp. 597–601.
Spies, H. and Pietzsch, H.J., Stannous Chloride in the Preparation of 99mTc Pharmaceuticals, Technetium-99m Pharmaceuticals, Zolle, I., Ed., Berlin: Springer, 2007. https://doi.org/10.1007/978-3-540-33990-8_3
El-Ghany, E.A., Marzouk, F., Abd El-Azim, S.A., Awwad, M.H., and Barakat, M.A., Egypt. J. Hospital Med., 2007, vol. 29, pp. 647–663.
Zhang, J., Yu, Q., Huo, J., Pang, Y., Yang, S., He, Y., Tang, T., Yang, C., and Wang, X., J. Radioanal. Nucl. Chem., 2010, vol. 283, no. 2, pp. 481–485.
Sakr, T., Motaleb, M., and Ibrahim, I., J. Radioanal. Nucl. Chem., 2012, vol. 292, no. 2, pp. 705–710.
Sakr, T., Essa, B., El-Essawy, F., and El-Mohty, A., Radiochemistry, 2014, vol. 56, no. 1, pp. 76–80.
De Barros, A.L.B., das Graças Mota, L., de Aguiar Ferreira, C., de Oliveira, M.C., de Góes, A.M., and Cardoso, V.N., Bioorg. Med. Chem. Lett., 2010, vol. 20, no. 21, pp. 6182–6184.
Ding, R., He, Y., Xu, J., Liu, H., Wang, X., Feng, M., Qi, C., Zhang, J., and Peng, C., Med. Chem. Res., 2012, vol. 21, no. 4, pp. 523–530.
Sakr, T., El-Safoury, D., Awad, G.A., and Motaleb, M., J. Label. Compd. Radiopharm., 2013, vol. 56, no. 8, pp. 392–395.
Abou-Zeid, L., El-Mowafy, A.M., El-Kerdawy, M.M., Hamza, H., and Abdel-Hamid, M.E., Farmaco, 2001, vol. 56, no. 10, pp. 763–770.
Mishra, S., Tamta, A.K., Sarikhani, M., et al., ALL AUTHORS Sci. Rep., 2018, vol. 8, p. 5599.
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
The author declares that she has no conflict of interest.
Rights and permissions
About this article
Cite this article
Dawood, M., Alani, B.G., Salim, K.S. et al. Technetium-99m Labeling of Antineoplaston A10 and Its Bioevaluation as a Potential Tumor Imaging Agent. Radiochemistry 64, 219–227 (2022). https://doi.org/10.1134/S106636222202014X
Received:
Revised:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1134/S106636222202014X