대한방사성의약품학회지 (Journal of Radiopharmaceuticals and Molecular Probes)

  • 제4권2호
  • /
  • Pages.85-89
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  • 2018
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  • 2384-1583(pISSN)
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  • 2508-3848(eISSN)
대한방사성의약품학회 (Korean Society of Radiopharmaceuticals and Molecular Probes)
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Synthesis of 125I-labeled thiol-reactive prosthetic group for site-specific radiolabeling of human serum albumin

  • Shim, Ha Eun (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute) ;
  • Song, Lee (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute) ;
  • Jeon, Jongho (Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute)
  • 투고 : 2018.12.12
  • 심사 : 2018.12.21
  • 발행 : 2018.12.30
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초록

We demonstrate a detail protocol for the radiosynthesis of an $^{125}I$-labeled MSTP prosthetic group and its application to the efficient radiolabeling of human serum albumin (HSA). Radioiodination of the precursor (2) was carried out by using $[^{125}I]$NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I$-labeled MSTP ($[^{125}I]1$) was obtained with high radiochemical yield ($73{\pm}5%$, n = 3) and excellent radiochemical purity (>99%). Site-specific reaction between ($[^{125}I]1$) and HSA gave the $^{125}I$-labeled human serum albumin ($[^{125}I]3$) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly demonstrate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of thiol-bearing biomolecules.

키워드

DHBSB1_2018_v4n2_85_f0001.png 이미지

Figure 1. Synthetic scheme for [125I]1 and [125I]3.

DHBSB1_2018_v4n2_85_f0002.png 이미지

Figure 2. Radio-HPLC results for synthesis of [125I]1. (A) Before purification of [125I]1 (crude mixture); (B) After purification of [125I]1; (C) UV HPLC chromatogram of 1.

DHBSB1_2018_v4n2_85_f0003.png 이미지

Figure 3. Radio-TLC results for synthesis of [125I]3 using [125I]1 (eluent: acetone). (A) Before purification of [125I]3 (crude mixture); (B) After purification of [125I]3.

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