Synthesis, radiolabeling and in vivo biological evaluation of 99mTc-labeled MAG3-based bisnitroimidazole complexes as tumor hypoxia markers
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Lei Mei
Abstract
Hypoxia, as a common phenomenon in solid tumors, is of interest for its relationship with resistance to tumor therapies and malignant progression of tumor. The noninvasive nuclear medical imaging technique using hypoxia markers is an important method for the detection of tumor hypoxia. The aim of current study is designing tumor hypoxia markers with hypoxia selectivity and improved properties. Two MAG3-based bisnitroimidazole compounds were synthesized and purified by semi-preparative HPLC. Both the MAG3 derivatives were labeled with 99mTc-oxo-technetium core via stannous tartrate exchange method in high yields (> 95%). The 99mTc-MAG3 complexes were stable at 37 ℃, 4 h after preparation, and were more hydrophilic than 99mTc-MAMA complexes. As biodistribution results showed, clearances of background activity for both the complexes were fast and they were excreted mainly through the hepatobiliary tract and part of renal tract. Although tumor uptakes of 99mTc-MAG3-B2NIL were lower than those of 99mTc-MAG3-B4NIL, tumor-to-blood ratios of 99mTc-MAG3-B2NIL showed an increasing trend and were better than those of 99mTc-MAG3-B4NIL after 2 h due to their different blood clearances. Tumor-to-muscle ratios of 99mTc-MAG3-B2NIL and 99mTc-MAG3-B4NIL were similar. Comparing with 99mTc-MAMA complexes, 99mTc-MAG3-B2NIL with better tumor-to-blood ratios exhibits improved feature for hypoxia imaging, though it has lower tumor uptake than 99mTc-MAMA complexes.
©2014 Walter de Gruyter Berlin/Boston
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- Frontmatter
- Editorial
- Preface
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- Radiopharmaceuticals in China: current status and prospects
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- A density functional theory study of the competitive complexation of pyridine against H2O and Cl−− to Cm3+ and Ce4+
- Chemical behavior of neptunium in the presence of technetium in nitric acid media
- Nitrate conversion and supercritical fluid extraction of UO2-CeO2 solid solution prepared by an electrolytic reduction-coprecipitation method
- An advanced purex process based on salt-free reductants
- Extraction behavior of cesium and some typical fission and non-fission products with a new 1,3-di(1-decyloxy)-2,4-crown-6-calix[4]arene
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- Mechanism of thorium biosorption by the cells of the soil fungal isolate Geotrichum sp. dwc-1
- Carbon-11 labeled stilbene derivatives from natural products for the imaging of Aβ plaques in the brain
- Synthesis, radiolabeling and in vivo biological evaluation of 99mTc-labeled MAG3-based bisnitroimidazole complexes as tumor hypoxia markers
- γ-radiation effect on dicyclohexano-18-crown-6 aqueous solution in the presence of metal cations
Articles in the same Issue
- Frontmatter
- Editorial
- Preface
- New nuclear facilities and their analytical applications in China
- Advances in computational actinide chemistry in China
- Recent advances in study of uranium surface chemistry in China
- Nuclear fuel cycle-oriented actinides separation in China
- Radiopharmaceuticals in China: current status and prospects
- Gas-phase chemistry of Mo, Ru, W, and Os metal carbonyl complexes
- Extraction complexes of Pu(IV) with carbamoylmethylphosphine oxide ligands: A relativistic density functional study
- Solvent extraction of uranium(VI) by a dipicolinamide using a room-temperature ionic liquid
- Evaluation study on a macroporous silica-based isohexyl-BTP adsorbent for minor actinides separation from nitric acid medium
- A density functional theory study of the competitive complexation of pyridine against H2O and Cl−− to Cm3+ and Ce4+
- Chemical behavior of neptunium in the presence of technetium in nitric acid media
- Nitrate conversion and supercritical fluid extraction of UO2-CeO2 solid solution prepared by an electrolytic reduction-coprecipitation method
- An advanced purex process based on salt-free reductants
- Extraction behavior of cesium and some typical fission and non-fission products with a new 1,3-di(1-decyloxy)-2,4-crown-6-calix[4]arene
- New insight into Eu(III) sorption mechanism at alumina/water interface by batch technique and EXAFS analysis
- Retention mechanisms and microstructure of Eu(III) on manganese dioxide studied by batch and high resolution EXAFS technique
- Extraction and purification of 227Ac and development of solid 219Rn source
- Mechanism of thorium biosorption by the cells of the soil fungal isolate Geotrichum sp. dwc-1
- Carbon-11 labeled stilbene derivatives from natural products for the imaging of Aβ plaques in the brain
- Synthesis, radiolabeling and in vivo biological evaluation of 99mTc-labeled MAG3-based bisnitroimidazole complexes as tumor hypoxia markers
- γ-radiation effect on dicyclohexano-18-crown-6 aqueous solution in the presence of metal cations
