Hirase Shiori, Araki Yurina, Hattori Yoshihide, Aoki Ayako, Fujiwara Daisuke, Michigami Masataka, Takatani-Nakase Tomoka, Fujii Ikuo, Futaki Shiroh, Kirihata Mitsunori, Nakase Ikuhiko
Graduate School of Science, Osaka Metropolitan University, Sakai 599-8531, Japan.
Research Center for BNCT, Osaka Metropolitan University, Sakai 599-8570, Japan.
Biol Pharm Bull. 2025;48(4):344-354. doi: 10.1248/bpb.b24-00651.
Boron neutron capture therapy (BNCT), a type of nuclear capture-based radiotherapy, has received extensive attention because of its strong anticancer effects, especially in head and neck cancers. This therapy was approved for clinical use in 2020 in Japan. This study demonstrated a technique that effectively uses the electrostatic interactions of negatively charged borane cage (polyhedral borane anion) of disodium mercaptoundecahydro-closo-dodecaborate (BSH) and positively charged cationic lipids or arginine-rich cell-penetrating peptides as carriers to enhance the efficiency of cellular uptake. Mixing of fluorescein isothiocyanate (FITC)-labeled BSH (FITC-BSH) with the cationic lipids led to increased cytosolic release and nuclear accumulation of FITC-BSH, resulting in superior cancer cell-killing activity following thermal neutron irradiation. This simple technique and our experimental results provide essential insights for the further development of BNCT.
硼中子俘获疗法（BNCT）是一种基于核俘获的放射疗法，因其强大的抗癌效果，尤其是对头颈部癌症的疗效，而受到广泛关注。该疗法于2020年在日本获批用于临床。本研究展示了一种技术，该技术有效利用了巯基十氢-闭式-十二硼酸钠（BSH）带负电荷的硼烷笼（多面体硼烷阴离子）与带正电荷的阳离子脂质或富含精氨酸的细胞穿透肽之间的静电相互作用作为载体，以提高细胞摄取效率。异硫氰酸荧光素（FITC）标记的BSH（FITC-BSH）与阳离子脂质混合导致FITC-BSH在胞质中的释放增加和核内积累，从而在热中子照射后产生卓越的癌细胞杀伤活性。这种简单的技术和我们的实验结果为BNCT的进一步发展提供了重要见解。
