Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment
Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radi...
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MDPI AG
2025-06-01
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| author | Tsung-Ming Wang Shih-Chang Chuang Kuo-Chen Hung Chang-Ching Yu Tzu-Chuan Ho Kuo-Pin Chuang Cheng-Hui Yuan Ming-Hui Yang Yu-Chang Tyan |
| author_facet | Tsung-Ming Wang Shih-Chang Chuang Kuo-Chen Hung Chang-Ching Yu Tzu-Chuan Ho Kuo-Pin Chuang Cheng-Hui Yuan Ming-Hui Yang Yu-Chang Tyan |
| author_sort | Tsung-Ming Wang |
| collection | DOAJ |
| description | Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radioactive iodine. While it has been primarily studied for imaging applications, its potential therapeutic effects when labeled with iodine-125 (<sup>125</sup>I) remain to be explored. Methods: In this study, IMPY was synthesized and labeled with <sup>125</sup>I for therapeutic purposes. Three different labeling methods were employed: isotope exchange reaction, redox reaction, and the Iodogen technique. The radiochemical yield of each method was determined to identify the most effective approach. Additionally, the effects of <sup>125</sup>I-IMPY on neuroblastoma cells were evaluated by assessing its toxicity and cellular uptake. Results: The radiochemical yields for the isotope exchange reaction, redox reaction, and Iodogen technique were found to be 0.96%, 10.74%, and 96.52%, respectively. The Iodogen technique exhibited the highest yield, exceeding 90% even after 48 h, making it the most efficient method. Furthermore, the impact of <sup>125</sup>I-IMPY on neuroblastoma cells was analyzed, revealing significant cellular uptake and potential therapeutic effects. Conclusions: This study demonstrated that the Iodogen technique is the most effective method for labeling IMPY with <sup>125</sup>I. The high labeling efficiency and observed cellular effects suggest that <sup>125</sup>I-IMPY could be considered not only as a tracer but also as a potential therapeutic agent for neuroblastoma. Further studies are needed to explore its full therapeutic potential and mechanism of action. |
| format | Article |
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| institution | DOAJ |
| issn | 2075-1729 |
| language | English |
| publishDate | 2025-06-01 |
| publisher | MDPI AG |
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| series | Life |
| spelling | doaj-art-4c3088cf8bd044f1bb95b17e5820b5f32025-08-20T03:16:33ZengMDPI AGLife2075-17292025-06-0115693010.3390/life15060930Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and TreatmentTsung-Ming Wang0Shih-Chang Chuang1Kuo-Chen Hung2Chang-Ching Yu3Tzu-Chuan Ho4Kuo-Pin Chuang5Cheng-Hui Yuan6Ming-Hui Yang7Yu-Chang Tyan8Department of Medical Imaging, China Medical University Hospital, Taichung 404, TaiwanDivision of General and Digestive Surgery, Department of Surgery, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 807, TaiwanDivision of General and Digestive Surgery, Department of Surgery, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 807, TaiwanDepartment of Nuclear Medicine, Kaohsiung Veterans General Hospital, Kaohsiung 813, TaiwanDepartment of Medical Imaging and Radiological Sciences, Kaohsiung Medical University, Kaohsiung 807, TaiwanGraduate Institute of Animal Vaccine Technology, College of Veterinary Medicine, National Pingtung University of Science and Technology, Pingtung 912, TaiwanMass Spectrometry Laboratory, Department of Chemistry, National University of Singapore, Singapore 119077, SingaporeDivision of General and Digestive Surgery, Department of Surgery, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 807, TaiwanDepartment of Medical Imaging and Radiological Sciences, Kaohsiung Medical University, Kaohsiung 807, TaiwanBackground: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radioactive iodine. While it has been primarily studied for imaging applications, its potential therapeutic effects when labeled with iodine-125 (<sup>125</sup>I) remain to be explored. Methods: In this study, IMPY was synthesized and labeled with <sup>125</sup>I for therapeutic purposes. Three different labeling methods were employed: isotope exchange reaction, redox reaction, and the Iodogen technique. The radiochemical yield of each method was determined to identify the most effective approach. Additionally, the effects of <sup>125</sup>I-IMPY on neuroblastoma cells were evaluated by assessing its toxicity and cellular uptake. Results: The radiochemical yields for the isotope exchange reaction, redox reaction, and Iodogen technique were found to be 0.96%, 10.74%, and 96.52%, respectively. The Iodogen technique exhibited the highest yield, exceeding 90% even after 48 h, making it the most efficient method. Furthermore, the impact of <sup>125</sup>I-IMPY on neuroblastoma cells was analyzed, revealing significant cellular uptake and potential therapeutic effects. Conclusions: This study demonstrated that the Iodogen technique is the most effective method for labeling IMPY with <sup>125</sup>I. The high labeling efficiency and observed cellular effects suggest that <sup>125</sup>I-IMPY could be considered not only as a tracer but also as a potential therapeutic agent for neuroblastoma. Further studies are needed to explore its full therapeutic potential and mechanism of action.https://www.mdpi.com/2075-1729/15/6/930isotope labelingIMPYradioactive iodineiodogenneuroblastoma |
| spellingShingle | Tsung-Ming Wang Shih-Chang Chuang Kuo-Chen Hung Chang-Ching Yu Tzu-Chuan Ho Kuo-Pin Chuang Cheng-Hui Yuan Ming-Hui Yang Yu-Chang Tyan Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment Life isotope labeling IMPY radioactive iodine iodogen neuroblastoma |
| title | Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment |
| title_full | Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment |
| title_fullStr | Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment |
| title_full_unstemmed | Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment |
| title_short | Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment |
| title_sort | synthesis and evaluation of sup 125 sup i impy application in neuroblastoma tracing and treatment |
| topic | isotope labeling IMPY radioactive iodine iodogen neuroblastoma |
| url | https://www.mdpi.com/2075-1729/15/6/930 |
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