{"title":"I-124标记小分子探针的合成与构建用于CAIX表达的无创PET成像。","authors":"Xianteng Yang, Chengxue He, Feng Wang, Li Wen, Haifeng Huang, Jing Wang, Zhi Yang, Hua Zhu","doi":"10.1007/s11307-025-02004-5","DOIUrl":null,"url":null,"abstract":"<p><strong>Purpose: </strong>Carbonic anhydrase IX (CAIX) which is high expression in the most of hypoxic tumor than normal tissue, promoting the growth, invasion, and metastasis of the tumor. Therefore, the study aimed to evaluate the retention and diagnostic ability of [<sup>124</sup>I]I-XYIMSR- 01 in CAIX-overexpression tumor by using positron emission tomography (PET) imaging.</p><p><strong>Procedures: </strong>[<sup>124/125</sup>I]I-XYIMSR- 01 was labeled by <sup>124/125</sup>I, and its CAIX-targeting properties in different cell lines were assayed by cell uptaken study. Its diagnose and retention ability in vivo were verified in different CAIX-expression models using PET imaging and biodistribution study. Pathological tissues were obtained for immunohistochemical (IHC) and Hematoxylin-Eosin (HE) staining to explore the relationship between CAIX and hypoxic, and further analyze PET/CT results.</p><p><strong>Results: </strong>[<sup>124</sup>I]I-XYIMSR- 01 was obtained with high specific activity, good radiochemical purity, and good stability. The uptake of of [<sup>124</sup>I]I-XYIMSR- 01 in HT- 29 cells, which have high CAIX expression, was significant higher than that in HCT116 cells with low CAIX expression (12.78 ± 0.47 vs 1.06 ± 0.10, p = 0.000, at 1 h). This indicated that the probe has good targeting capability and specificity for CAIX. In Micro-PET imaging, clear molecular images lasting for 48 h were achieved in HT29 model. Quantitative biodistribution results showed that the tumor and digestive tract background tissues had a good signal-to-noise ratio within 24 h after injection, indicating [<sup>124</sup>I]I-XYIMSR- 01 could enable delayed imaging in digestive tract tumors (tumor-to-small intestine: 8.79 ± 0.98). Tumors uptakes were also confirmed by IHC pathology.</p><p><strong>Conclusion: </strong>The study have shown that [<sup>124</sup>I]I-XYIMSR- 01 is an ideal molecular probe for tumor hypoxia, enabling long-term dynamic monitoring and imaging of hypoxic tumors.</p>","PeriodicalId":18760,"journal":{"name":"Molecular Imaging and Biology","volume":" ","pages":"485-494"},"PeriodicalIF":2.5000,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Construction of I-124 Labeled Small Molecular Probe for Noninvasive PET Imaging of CAIX Expression.\",\"authors\":\"Xianteng Yang, Chengxue He, Feng Wang, Li Wen, Haifeng Huang, Jing Wang, Zhi Yang, Hua Zhu\",\"doi\":\"10.1007/s11307-025-02004-5\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Purpose: </strong>Carbonic anhydrase IX (CAIX) which is high expression in the most of hypoxic tumor than normal tissue, promoting the growth, invasion, and metastasis of the tumor. Therefore, the study aimed to evaluate the retention and diagnostic ability of [<sup>124</sup>I]I-XYIMSR- 01 in CAIX-overexpression tumor by using positron emission tomography (PET) imaging.</p><p><strong>Procedures: </strong>[<sup>124/125</sup>I]I-XYIMSR- 01 was labeled by <sup>124/125</sup>I, and its CAIX-targeting properties in different cell lines were assayed by cell uptaken study. Its diagnose and retention ability in vivo were verified in different CAIX-expression models using PET imaging and biodistribution study. Pathological tissues were obtained for immunohistochemical (IHC) and Hematoxylin-Eosin (HE) staining to explore the relationship between CAIX and hypoxic, and further analyze PET/CT results.</p><p><strong>Results: </strong>[<sup>124</sup>I]I-XYIMSR- 01 was obtained with high specific activity, good radiochemical purity, and good stability. The uptake of of [<sup>124</sup>I]I-XYIMSR- 01 in HT- 29 cells, which have high CAIX expression, was significant higher than that in HCT116 cells with low CAIX expression (12.78 ± 0.47 vs 1.06 ± 0.10, p = 0.000, at 1 h). This indicated that the probe has good targeting capability and specificity for CAIX. In Micro-PET imaging, clear molecular images lasting for 48 h were achieved in HT29 model. Quantitative biodistribution results showed that the tumor and digestive tract background tissues had a good signal-to-noise ratio within 24 h after injection, indicating [<sup>124</sup>I]I-XYIMSR- 01 could enable delayed imaging in digestive tract tumors (tumor-to-small intestine: 8.79 ± 0.98). Tumors uptakes were also confirmed by IHC pathology.</p><p><strong>Conclusion: </strong>The study have shown that [<sup>124</sup>I]I-XYIMSR- 01 is an ideal molecular probe for tumor hypoxia, enabling long-term dynamic monitoring and imaging of hypoxic tumors.</p>\",\"PeriodicalId\":18760,\"journal\":{\"name\":\"Molecular Imaging and Biology\",\"volume\":\" \",\"pages\":\"485-494\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2025-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Imaging and Biology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s11307-025-02004-5\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/4/9 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Imaging and Biology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s11307-025-02004-5","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/4/9 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
Synthesis and Construction of I-124 Labeled Small Molecular Probe for Noninvasive PET Imaging of CAIX Expression.
Purpose: Carbonic anhydrase IX (CAIX) which is high expression in the most of hypoxic tumor than normal tissue, promoting the growth, invasion, and metastasis of the tumor. Therefore, the study aimed to evaluate the retention and diagnostic ability of [124I]I-XYIMSR- 01 in CAIX-overexpression tumor by using positron emission tomography (PET) imaging.
Procedures: [124/125I]I-XYIMSR- 01 was labeled by 124/125I, and its CAIX-targeting properties in different cell lines were assayed by cell uptaken study. Its diagnose and retention ability in vivo were verified in different CAIX-expression models using PET imaging and biodistribution study. Pathological tissues were obtained for immunohistochemical (IHC) and Hematoxylin-Eosin (HE) staining to explore the relationship between CAIX and hypoxic, and further analyze PET/CT results.
Results: [124I]I-XYIMSR- 01 was obtained with high specific activity, good radiochemical purity, and good stability. The uptake of of [124I]I-XYIMSR- 01 in HT- 29 cells, which have high CAIX expression, was significant higher than that in HCT116 cells with low CAIX expression (12.78 ± 0.47 vs 1.06 ± 0.10, p = 0.000, at 1 h). This indicated that the probe has good targeting capability and specificity for CAIX. In Micro-PET imaging, clear molecular images lasting for 48 h were achieved in HT29 model. Quantitative biodistribution results showed that the tumor and digestive tract background tissues had a good signal-to-noise ratio within 24 h after injection, indicating [124I]I-XYIMSR- 01 could enable delayed imaging in digestive tract tumors (tumor-to-small intestine: 8.79 ± 0.98). Tumors uptakes were also confirmed by IHC pathology.
Conclusion: The study have shown that [124I]I-XYIMSR- 01 is an ideal molecular probe for tumor hypoxia, enabling long-term dynamic monitoring and imaging of hypoxic tumors.
期刊介绍：
Molecular Imaging and Biology (MIB) invites original contributions (research articles, review articles, commentaries, etc.) on the utilization of molecular imaging (i.e., nuclear imaging, optical imaging, autoradiography and pathology, MRI, MPI, ultrasound imaging, radiomics/genomics etc.) to investigate questions related to biology and health. The objective of MIB is to provide a forum to the discovery of molecular mechanisms of disease through the use of imaging techniques. We aim to investigate the biological nature of disease in patients and establish new molecular imaging diagnostic and therapy procedures.
Some areas that are covered are:
Preclinical and clinical imaging of macromolecular targets (e.g., genes, receptors, enzymes) involved in significant biological processes.
The design, characterization, and study of new molecular imaging probes and contrast agents for the functional interrogation of macromolecular targets.
Development and evaluation of imaging systems including instrumentation, image reconstruction algorithms, image analysis, and display.
Development of molecular assay approaches leading to quantification of the biological information obtained in molecular imaging.
Study of in vivo animal models of disease for the development of new molecular diagnostics and therapeutics.
Extension of in vitro and in vivo discoveries using disease models, into well designed clinical research investigations.
Clinical molecular imaging involving clinical investigations, clinical trials and medical management or cost-effectiveness studies.
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