Startseite Design of a novel complex 99mTc-Nilutamide as a tracer for prostate cancer disorder detection in mice
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Design of a novel complex 99mTc-Nilutamide as a tracer for prostate cancer disorder detection in mice

  • M.H. Sanad ORCID logo EMAIL logo , Safaa B. Challan ORCID logo EMAIL logo , H.M. Essam , Fatma Y. Abdou und A.B. Farag
Veröffentlicht/Copyright: 3. Dezember 2024

Abstract

Male prostate cancer (PCa) is considered among the most fatal illnesses. Despite the recent decrease in prostate cancer incidence attributed to advancements in early detection and therapy, these reductions have not effectively mitigated the elevated fatality rate linked to this disease. The drug Nilutamide was effectively radiolabeled with technetium-99m, producing a radiochemical yield of 96 ± 0.14 % under optimal conditions. In our study, two cohorts of mice were utilized, namely the control group and the group with prostate cancer. Various biochemical parameters, including PSA levels in serum, were assessed, revealing a significantly elevated value in the group with prostate cancer, indicating potential tumor development. Furthermore, the activities of antioxidant enzymes (CAT, SOD) were notably lower in the group with prostate cancer compared to the healthy control group, while the oxidative activity reflected by MDA levels, the final product of lipid peroxidation, was higher in the prostate cancer group than in the healthy control group. The biodistribution analysis showed rapid localization of 99mTc-Nilutamide in prostate cancer tissue after 2 h post-injection, with a substantial value of 11.4 ± 1.1 % I. D/g tissue. Consequently, it was deduced that radiolabeled 99mTc-Nilutamide can serve as an effective imaging tool for prostate cancer.


Corresponding authors: M.H. Sanad, Department of Labeled Compounds, Hot Laboratories Center, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt, E-mail: ; and Safaa B. Challan, Department of Labeled Compounds, Hot Laboratories Center, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt; and Cyclotron Project, Nuclear Research Center, Egyptian Atomic Energy Authority, Box 13759, Cairo, Egypt, E-mail:
.

  1. Research ethics: All experimental procedures were conducted at the Labeled Compounds Department within the Hot Laboratories Center of the Egyptian Atomic Energy Authority. Research Ethics of animal treatment was approved by the Animal Care Committee of the National Centre for Radiation Research and Technology (NCRRT)-Egyptian Atomic Energy Authority, Cairo, Egypt (Permit Number:60A/23).

  2. Informed consent: None.

  3. Author contributions: M. H. Sanad: He developed the research idea, conceptualization, methodology, biodistribution, validation, investigation, labeling, and writing-original draft. Safaa B. Challan: she has shared in developing the research idea, conceptualization, methodology, biodistribution, validation, investigation, labeling, and writing-original draft. H. M. Essam: She has Participated in developing the research idea, resources, labeling, resources and methodology, and biodistribution. Fatma, Y. Abdou: she has shared in methodology, validation, investigation biodistribution specially the biodistribution of prostate cancer. model. A. B. Farag: He has shared in all parts of the work.

  4. Use of Large Language Models, AI and Machine Learning Tools: None.

  5. Conflict of interest: The authors declare that there are no competing interests and that all authors have consented to publication. The authors say the reported study is unique and has never been published before.

  6. Research funding: No funding was received to conduct this study.

  7. Data availability: Not applicable.

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86. Sanad, M. H.; Marzook, F. A.; Challan, S. B.; Essam, H. M.; Ayman, B. F. Radioiodination, and Biological Assessment of Olsalazine, as a Highly Selective Radiotracer for Ulcerative Colitis Imaging in Mice. Arab. J. Nucl. Sci. Applic. 2023, 56, 105–120; https://doi.org/10.21608/ajnsa.2022.163538.1639.Suche in Google Scholar

87. Eyssa, H. M.; Mohamed, M.; El Refay, H. M.; Sanad, M. H. In-vitro Evaluation of Blood Bags Based on Poly (vinyl chloride)/Selenium Nanocomposites and Exposed to Electron Beam Irradiation. Egypt. J. Chem. 2024. https://doi.org/10.21608/ejchem.2024.303268.9984.Suche in Google Scholar

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90. Sanad, M. H.; Eyssa, H. M.; Marzook, F. A.; Farag, A. B.; Rizvi, S. F. A.; Mandal, S. K. Optimized Chromatographic Separation and Bioevalution of Radioiodinated Ilaprazole as a New Labeled Compound for Peptic Ulcer Localization in Mice. Rdiochemistry 2021, 63 (6), 811–819.10.1134/S1066362221060138Suche in Google Scholar

91. Sanad, M. H.; Fouzy, A. S. M.; Sobhy, H. M.; Hathout, A. S.; Hussain, O. A. Tracing the Protective Activity of Lactobacillus Plantarum Using Technetium-99m-labeled Zearalenone for Organtoxicity. Int. J. Radiat. Biol. 2018, 94, 1151–1158.10.1080/09553002.2019.1524990Suche in Google Scholar PubMed

92. Moustapha, M. E.; Motaleb, M. A.; Sanad, M. H. Synthesis and Biological Evaluation of 99mTc-labetalol for β1-adrenoceptormediated Cardiac Imaging. J. Radioanal. Nucl. Chem. 2016, 309, 511–516.10.1007/s10967-015-4622-3Suche in Google Scholar

93. Sanad, M. H.; Ibrahim, A. A.; Talaat, H. M. Synthesis, Bioevaluation and Gamma Scintigraphy of 99mTc-N-2-(Furylmethyliminodiacetic acid) Complex as a New Renal Radiopharmaceutical. J. Radioanal. Nucl. Chem. 2018, 315, 57–63.10.1007/s10967-017-5617-zSuche in Google Scholar

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95. Sanad, M. H.; Marzook, F. A.; Abd-Elhaliem, S. M. Radioiodination and Biological Evaluation of Irbesartan as a Tracer for Cardiac Imaging. Radiochim. Acta 2021, 109, 41–46.10.1515/ract-2020-0025Suche in Google Scholar

96. Sanad, M. H.; Eyssa, H. M.; Gomaa, N. M.; Marzook, F. A.; Sabry, B. A. Radioiodinated Esomeprazole as a Model for Peptic Ulcer Localization. Radiochim. Acta 2021, 109, 711–716.10.1515/ract-2021-1056Suche in Google Scholar

97. Sanad, M. H.; Eyssa, H. M.; Marzook, F. A.; Farag, A. B.; Rizvic, S. F. A.; Mandal, S. K.; Patnaik, S. S.; Fouzy, A. S. M.; Sabry, B. A.; Verpoort, F. Radiosynthesis and Biological Evaluation of 99mTc Nitrido-Levetiracetam as a Brain Imaging Agent. Radiochemistry. 2021, 63, 635–641.10.1134/S106636222105012XSuche in Google Scholar

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99. Sanad, M. H.; Saleh, G. M.; Marzook, F. A. Radioiodination and Biological Evaluation of Nizatidine as a New Highly Selective Radiotracer for Peptic Ulcer Disorder Detection. J. Label. Compd. Radiopharm. 2017, 60, 600–607.10.1002/jlcr.3541Suche in Google Scholar PubMed

100. Sanad, M. H.; Salama, D. H.; Marzook, F. A. Radioiodinated Famotidine as a New Highly Selective Radiotracer for Peptic Ulcer Disorder Detection, Diagnostic Nuclear Imaging and Biodistribution. Radiochim. Acta 2017, 105, 389–398.10.1515/ract-2016-2683Suche in Google Scholar

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102. Sanad, M. H.; Ibrahim, I. T. Radiodiagnosis of Peptic Ulcer with Technetium-99m Labeled Rabeprazole. Radiochemistry 2015, 57, 422–430.10.1134/S1066362215040165Suche in Google Scholar

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105. Sanad, M. H.; Sallam, K. M.; Marzook, F. Labeling and Biological Evaluation of 99mTc-Tricarbonyl-Chenodiol for Hepatobiliary Imaging. Radiochemistry 2017, 59, 525–529.Suche in Google Scholar

106. Motaleb, M. A.; Selim, A. A.; El-Tawoosy, M.; Sanad, M. H.; El-Hashash, M. A. Synthesis, Radiolabeling and Biological Distribution of a New Dioxime Derivative as a Potential Tumor Imaging Agent. J. Radioanal. Nucl. Chem. 2017, 314, 1517–1522.10.1007/s10967-017-5310-2Suche in Google Scholar

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109. Sanad, M. H.; Abelrahman, M. A.; Marzook, F. M. A. Radioiodination and Biological Evaluation of Levalbuterol as a New Selective Radiotracer: A β2-Adrenoceptor Agonist. Radiochim. Acta 2016, 104, 345–353.10.1515/ract-2015-2518Suche in Google Scholar

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113. Sanad, H. M.; Ibrahim, A. A. Radioiodination, Diagnostic Nuclear Imaging and Bioevaluation of Olmesartan as a Tracer for Cardiac Imaging. Radiochim. Acta 2018, 106, 843–850.10.1515/ract-2018-2960Suche in Google Scholar

114. Sanad, M. H.; Sakr, T. M.; Walaa, H. A. A.; Marzook, E. A. In Silico Study and Biological Evaluation of 99mTc-Tricabonyl Oxiracetam as a Selective Imaging Probe for AMPA Receptors. J. Radioanal. Nucl. Chem. 2017, 314, 1505–1515.10.1007/s10967-016-5120-ySuche in Google Scholar

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117. Sanad, M. H.; Alhussein, A. I. Preparation and Biological Evaluation of 99mTcN-Histamine as a Model for Brain Imaging: In Silico Study and Preclinical Evaluation. Radiochim. Acta 2018, 106, 229–238.10.1515/ract-2017-2804Suche in Google Scholar

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122. Borai, E. H.; Sanad, M. H.; Fouzy, A. S. M. Optimized Chromatographic Separation and Biological Evaluation of 99mTc-clarithromycin for Infective Inflammation Diagnosis. Radiochemistry 2016, 58, 84–91.10.1134/S1066362216010136Suche in Google Scholar

123. Sanad, M. H.; Sallam, K. M.; Marzook, F. Labeling and Biological Evaluation of 99mTc-tricarbonyl-chenodiol for Hepatobiliary Imaging. Radiochemistry 2017, 59, 525–529.10.1134/S10663622170500149Suche in Google Scholar

124. Sanad, M. H.; Emad, H. B. Performance Characteristics of Biodistribution of 99mTc-cefprozil for in-vivo Infection Imaging. J. Anal. Sci. Technol. 2014, 5, 32.10.1186/s40543-014-0032-3Suche in Google Scholar

125. Sanad, M. H.; Farag, A. B.; Saleh, G. M. Radiosynthesis and Biological Evaluation of 188Re-5,10,15,20–Tetra (4-pyridyl)- 21H,23H-porphyrin Complex as a Tumor-targeting Agent. Radiochemistry 2019, 61, 347–351.10.1134/S106636221903010XSuche in Google Scholar

126. Motaleb, M. A.; Sanad, M. H.; Selim, A. A.; El-Tawoosy, M.; El-Hashash, M. A. Synthesis, Characterization, and Radiolabeling of Heterocyclic Bisphosphonate Derivative as a Potential Agent for Bone Imaging. Radiochemistry 2018, 60, 201–207.10.1134/S106636221802011XSuche in Google Scholar

127. Motaleb, M. A.; Adli, A. S. A.; El-Tawoosy, M.; Sanad, M. H.; AbdAllah, M. An Easy and Effective Method for Synthesis and Radiolabelling of Risedronate as a Model for Bone Imaging. J. Label Compd. Radiopharm. 2016, 59, 157–163.10.1002/jlcr.3384Suche in Google Scholar PubMed

128. Sanad, M. H.; El-Bayoumy, A. S. A.; Alhussein, A. I. Comparative Biological Evaluation Between 99mTc(CO)3 and 99mTc-Sn(II) Complexes of Novel Quinoline Derivative: A Promising Infection Radiotracer. J. Radioanal. Nucl. Chem. 2017, 311, 1–14.10.1007/s10967-016-4945-8Suche in Google Scholar

129. Sanad, M. H.; Emad, H. B. Comparative Biological Evaluation Between 99mTc- tricarbonyl and 99mTc-Sn(II) levosalbutamol as a β2- adrenoceptor Agonist. Radiochim. Acta 2015, 103, 879–891.10.1515/ract-2015-2428Suche in Google Scholar

130. Sanad, M. H.; El-Tawoosy, M. Labeling of Ursodeoxycholic Acid with Technetium-99m for Hepatobiliary Imaging. J. Radioanal. Nucl. Chem. 2013, 298, 1105–1109.10.1007/s10967-013-2512-0Suche in Google Scholar

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132. Sanad, M. H.; Talaat, H. M.; Fouzy, A. S. M. Radioiodination and Biological Evaluation of Mesalamine as a Tracer for Ulcerative Colitis Imaging. Radiochim. Acta 2018, 106, 393–400.10.1515/ract-2017-2840Suche in Google Scholar

133. Sanad, M. H.; Sallam, K. M.; Salama, D. H. 99mTc-Oxiracetam as a Potential Agent for Diagnostic Imaging of Brain: Labeling, Characterization, and Biological Evaluation. Radiochemistry 2018, 60, 58–63.10.1134/S1066362218010101Suche in Google Scholar

134. Sanad, M. H.; Hanan, T.; Ibrahim, I. T.; Gehan, S.; Abozaid, L. A. Radioiodinated Celiprolol as a New Highly Selective Radiotracer for β1-adrenoceptormyocardial Perfusion Imaging. Radiochim. Acta 2018, 106, 751–757.10.1515/ract-2017-2903Suche in Google Scholar

135. Sanad, M. H.; Rizvi, F. A.; Kumar, R. R.; Ibrahim, A. A. Synthesis and Preliminary Biological Evaluation of 99mTc-Tricarbonyl Ropinirole as a Potential Brain Imaging Agent. Radiochemistry 2019, 61, 754–758.10.1134/S1066362219060195Suche in Google Scholar

136. Sanad, M. H.; Ibrahim, I. T. Preparation and Biological Evaluation of 99mTc-Timonacic Acid as a New Complex for Hepatobiliary Imaging. Radiochemistry 2017, 59, 92–97.10.1134/S106636221701012XSuche in Google Scholar

137. Sanad, M. H.; Eyssa, H. M.; Marzook, F. A.; Abd-Elhaliem, S. M.; Abdou, F. Y. Radiosynthesis, Preparation, and Biological Evaluation of [99MTC]Tricarbonyl Pantoprazole for Stomach Ulcer Detection in Mice. Pharm. Chem. J. 2024, 58, 1–7.10.1007/s11094-024-03228-5Suche in Google Scholar

138. Sanad, M. H.; Abd-Elhaliem, S. M.; Abdou, F. Y.; Soliman, A. M.; Farag, A. B. Radiolabeled Nefiracetam for Brain Imaging: Chromatographic Separation, Bio-Evaluation and Preclinical Assessment Studies. Pharm. Chem. J. 2024, 58, 1–9.10.1007/s11094-024-03206-xSuche in Google Scholar

139. Sanad, M. H.; Nermien, M. G.; Nermeen, M. E.; Ismail, T. I.; Ayman, M. Radioiodination of Balsalazide, Bioevaluation and Characterization as a Highly Selective Radiotracer for Imaging of Ulcerative Colitis in Mice. J. Label Compd. Radiopharm. 2022, 65, 71–82.10.1002/jlcr.3961Suche in Google Scholar PubMed

140. Sanad, M. H., M. H.; Farag, A. B.; Sabry, A. B. A.; Marzook, F. A. Radioiodination of Zearalenone and Determination of Lactobacillus Plantarum Effect of on Zearalenone Organ Distribution: In Silico Study and Preclinical Evaluation. Toxicol. Rep. 2022, 9, 470–479.10.1016/j.toxrep.2022.02.003Suche in Google Scholar PubMed PubMed Central

Received: 2024-05-09
Accepted: 2024-11-05
Published Online: 2024-12-03
Published in Print: 2025-03-26

© 2024 Walter de Gruyter GmbH, Berlin/Boston

Heruntergeladen am 12.9.2025 von https://www.degruyterbrill.com/document/doi/10.1515/ract-2024-0303/html
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