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<p>Recently, boron neutron capture therapy (BNCT) has attracted attention as a new cancer therapy. We have previously developed a fluorophenyl boronic acid-modified polyrotaxane (FPBA-PRX), as a novel supramolecular boron compund for BNCT. FPBA in FPBA-PRX binds to sialic acid, which is highly expressed on the surface of tumor cells, and functions not only as a tumor-targeting ligand but also as a boron compound because it has boron in the molecule. In this study, to enhance cancer-accumulating properties of FPBA-PRX, we prepared two targeting materials; namely, (1) polyethylene glycol-modified dopamine (PEG-Dopamine), which prevents FPBA-PRX from binding to sialic acid onto normal cells under normal tissue pH conditions, and (2) a folate-modified β-cyclodextrin (FA7-β-CyD), which is selectively taken up by cells with high expression of folate receptors (FR-α). As a result, FPBA in FPBA-PRX bound to PEG-Dopamine at pH 7.4, resulting in decreased uptake by sialic acid highly expressing cells, but dissociated PEG-Dopamine at pH 6.5 in tumor microenvironment, resulting in restored cellular uptake. FA7-β-CyD interacted with adamantane present at both ends of FPBA-PRX. In addition, FPBA-PRX/FA7-β-CyD was taken up into cells more efficiently than FPBA-PRX alone in FR-α-over expressing tumor cells. These results suggest that FPBA-PRX/PEG-Dopamine and FPBA-PRX/FA7-β-CyD have potential as boron compounds by improving the tumor selectivity of FPBA-PRX.</p>

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Preparation of targeting materials for a boron-containing polyrotaxane in boron neutron capture therapy

  • 期刊论文

  • 发表日期：

    2025年6月27日

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  • Honatsu Ishiki,
  • Toru Taharabaru,
  • Haruki Arase,
  • Yoshitaka Matsumoto,
  • Risako Onodera,
  • Keiichi Motoyama,
  • Taishi Higashi

摘要

Recently, boron neutron capture therapy (BNCT) has attracted attention as a new cancer therapy. We have previously developed a fluorophenyl boronic acid-modified polyrotaxane (FPBA-PRX), as a novel supramolecular boron compund for BNCT. FPBA in FPBA-PRX binds to sialic acid, which is highly expressed on the surface of tumor cells, and functions not only as a tumor-targeting ligand but also as a boron compound because it has boron in the molecule. In this study, to enhance cancer-accumulating properties of FPBA-PRX, we prepared two targeting materials; namely, (1) polyethylene glycol-modified dopamine (PEG-Dopamine), which prevents FPBA-PRX from binding to sialic acid onto normal cells under normal tissue pH conditions, and (2) a folate-modified β-cyclodextrin (FA7-β-CyD), which is selectively taken up by cells with high expression of folate receptors (FR-α). As a result, FPBA in FPBA-PRX bound to PEG-Dopamine at pH 7.4, resulting in decreased uptake by sialic acid highly expressing cells, but dissociated PEG-Dopamine at pH 6.5 in tumor microenvironment, resulting in restored cellular uptake. FA7-β-CyD interacted with adamantane present at both ends of FPBA-PRX. In addition, FPBA-PRX/FA7-β-CyD was taken up into cells more efficiently than FPBA-PRX alone in FR-α-over expressing tumor cells. These results suggest that FPBA-PRX/PEG-Dopamine and FPBA-PRX/FA7-β-CyD have potential as boron compounds by improving the tumor selectivity of FPBA-PRX.