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Radio-Iodinated arbutin for tumor imaging

  • Huynh, Phuong Tu (Department of Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University) ;
  • Ha, Yeong Su (Department of Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University) ;
  • Lee, Woonghee (Department of Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University) ;
  • Yoo, Jeongsoo (Department of Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University)
  • Received : 2017.12.08
  • Accepted : 2017.12.22
  • Published : 2017.12.30

Abstract

Arbutin is a hydroquinone derivative with a glucose moiety. As a tyrosinase inhibitor, it is widely used as a skin-whitening cosmetic agent for the treatment of cutaneous hyperpigmentary disorders, such as melasma and freckles. In the medical field, many studies have addressed the use of arbutin in various tumors, but the mechanism for tumor uptake of arbutin is still unclear. In this paper, we radiolabeled arbutin using radioiodine and studied its pharmacokinetics and tumor uptake via biodistribution experiments and single-photon emission computed tomography (SPECT) imaging. Radiolabeled $^{131}I-arbutin$ was stable for up to 24 h in PBS and serum. Biodistribution studies and SPECT imaging indicated high uptake of the compound in the bladder and kidneys shortly after injection. Twenty-four hours post-injection, significant deiodination was observed. Apart from high thyroid uptake, selective tumor uptake was clearly observed. The tumor-to-muscle and tumor-to-blood ratios were 26 and 9, respectively.

Acknowledgement

Supported by : National Research Foundation of Korea, Korea Health Industry Development Institute (KHIDI)

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