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<p>[<sup>131</sup>I]I-AMB10, a synthetic derivative of alpha mangostin, was developed to target estrogen receptor alpha (ERα)-positive breast cancer. Radiolabeled using iodine-131 via chloramine-T oxidation, it achieved high radiochemical purity (97.53 ± 1.08%). The compound exhibited moderate lipophilicity (log <i>P</i> = 0.67 ± 0.13) and plasma protein binding (73.66 ± 4.99%). Internalization studies revealed higher uptake in T-47D cells compared to MCF-7 cells, indicating selective affinity for ER + lines. Computational study of the compound showed high binding affinity and stability in the binding pocket of the ERα receptor. These results suggest that [<sup>131</sup>I]I-AMB10 has potential as a targeted theranostic agent for ERα-positive breast cancer.</p>

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Radiopharmaceutical development of alpha mangostin derivative [131I]I-AMB10: radiosynthesis, in silico, and cellular internalization against human breast cancer cell lines

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • Isti Daruwati,
  • Richa Mardianingrum,
  • Yanuar Setiadi,
  • Veronika Yulianti Susilo,
  • Alfian Mahardika Forentin,
  • Ligwina Dita Pertiwi,
  • Ruswanto,
  • Rizky Juwita Sugiharti,
  • Tri Hanggono Achmad,
  • Mukh Syaifudin,
  • Muchtaridi Muchtaridi

摘要

[131I]I-AMB10, a synthetic derivative of alpha mangostin, was developed to target estrogen receptor alpha (ERα)-positive breast cancer. Radiolabeled using iodine-131 via chloramine-T oxidation, it achieved high radiochemical purity (97.53 ± 1.08%). The compound exhibited moderate lipophilicity (log P = 0.67 ± 0.13) and plasma protein binding (73.66 ± 4.99%). Internalization studies revealed higher uptake in T-47D cells compared to MCF-7 cells, indicating selective affinity for ER + lines. Computational study of the compound showed high binding affinity and stability in the binding pocket of the ERα receptor. These results suggest that [131I]I-AMB10 has potential as a targeted theranostic agent for ERα-positive breast cancer.