Abstract
Diagnosis of tumour hypoxia is an important aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, 99mTcethylenedicysteine- bis-misonidazole (99mTc-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4 -) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumour was observed.
Keywords: Tumour hypoxia, imaging agent, misonidazole (MISO), technetium-99m-labeled.
Medicinal Chemistry
Title:Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia
Volume: 11 Issue: 7
Author(s): Feng Wang, Di Fan, Jun Qian, Zhe Zhang, Jianhua Zhu and Jian Chen
Affiliation:
Keywords: Tumour hypoxia, imaging agent, misonidazole (MISO), technetium-99m-labeled.
Abstract: Diagnosis of tumour hypoxia is an important aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, 99mTcethylenedicysteine- bis-misonidazole (99mTc-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4 -) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumour was observed.
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Cite this article as:
Wang Feng, Fan Di, Qian Jun, Zhang Zhe, Zhu Jianhua and Chen Jian, Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia, Medicinal Chemistry 2015; 11 (7) . https://dx.doi.org/10.2174/1573406411666150504124103
DOI https://dx.doi.org/10.2174/1573406411666150504124103 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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