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KMID : 1145520200060010003
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Journal of Radiopharmaceuticals and Molecular Probes
2020 Volume.6 No. 1 p.3 ~ p.9
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Synthesis and in vitro evaluation of 99mTc-labeled tetraiodothyroacetic acid for tumor angiogenesis imaging
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Kim Hyun-Jung
Koo Hyun-Jung
Choe Yearn-Seong
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Abstract
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Tetraiodothyroacetic acid (tetrac) is a derivative of thyroid hormone T4 and causes anti-angiogenesis by blocking T4 binding to integrin αvβ3. In this study, we synthesized [99mTc]Tc-Cys-Asp-Gly(CDG)-tetrac and evaluated it in vitro as a tumor angiogenesis imaging ligand. The CDG was conjugated to tetrac as a chelator for technetium-99m labeling. The cold vial containing CDG-tetrac, sodium glucoheptonate, and reducing agent was completed under nitrogen-filled atmospheric glove bag. [99mTc]Tc-CDG-tetrac was synthesized in quantitative yield by heating the cold vial with [99mTc]TcO4- at 100 oC for 30 min. In vitro serum stability of [99mTc]Tc-CDG-tetrac was measured by incubating the radioligand in 50% fetal bovine serum at 37 oC and analyzing the incubation mixture by radio-TLC, which showed high stability over 6 h (≥ 98%). Cell binding study was carried out by incubating [99mTc]Tc-CDG-tetrac with human umbilical vein endothelial (HUVE) cells at 37 oC for 6 h. The cell binding of the radioligand increased from 100% at 0.5 h to 293.7% at 6 h in a time-dependent manner. For blocking study, the cells were incubated with the radioligand in the presence of either tetrac (20 μM) or cRGDyK (20 μ) at 37 oC for 4 h. The results demonstrated that the cell binding of the radioligand was inhibited by tetrac (19.1%) or cRGDyK (35.6%), indicating specific binding of the radioligand to integrin αvβ3. Thus, this study suggests that [99mTc]Tc-CDG-tetrac may be a potential radioligand for tumor angiogenesis imaging.
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KEYWORD
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Tetraiodothyroacetic acid (tetrac), CDG-tetrac, 99mTc, Tumor angiogenesis
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