Imperio Daniela, Postuma Ian, Villani Salvatore, Del Grosso Erika, Cansolino Laura, Ferrari Cinzia, Fallarini Silvia, Bortolussi Silva, Panza Luigi
Department for Sustainable Development and Ecological Transition, University of Eastern Piedmont, Piazza Sant'Eusebio 5, 13100 Vercelli, Italy.
National Institute of Nuclear Physics (INFN), Unit of Pavia, Via A. Bassi 6, 27100 Pavia, Italy.
Pharmaceuticals (Basel). 2025 Jun 30;18(7):986. doi: 10.3390/ph18070986.
Boron Neutron Capture Therapy (BNCT) is a promising cancer treatment that combines tumor-selective boron delivery agents with thermal neutrons to kill cancer cells while sparing normal tissue. BNCT requires boron-containing compounds that exhibit high tumor selectivity and achieve therapeutic boron concentrations within tumor cells. This work focuses on the early development of a novel boron cluster carbohydrate derivative based on the glucosamine structure. Our results indicate that this derivative may have advantages over the typical boron delivery agent used in clinical applications and may significantly improve boron delivery capacity at the cellular level. The performance of the compound in terms of boron uptake was tested in the U87-MG glioblastoma cell line employing neutron autoradiography imaging and quantification. The compound was non-toxic for cells, and it showed a remarkable capacity to enrich cells with boron. The ratio between boron concentration provided in the culture medium and boron concentration achieved in cells was compared to that obtained with boronophenylalanine (BPA), the gold standard in BNCT. The result demonstrated a significantly better performance compared with BPA, showing that the novel agent can concentrate boron in cells more than in culture medium. : The encouraging preliminary results provide a starting point for its potential application in in vivo tests.
硼中子俘获疗法（BNCT）是一种很有前景的癌症治疗方法，它将肿瘤选择性硼递送剂与热中子相结合，以杀死癌细胞同时 sparing normal tissue（此处英文有误，推测应为“保护正常组织”）。BNCT 需要具有高肿瘤选择性且能在肿瘤细胞内达到治疗性硼浓度的含硼化合物。这项工作聚焦于基于氨基葡萄糖结构的新型硼簇碳水化合物衍生物的早期研发。我们的结果表明，这种衍生物可能比临床应用中使用的典型硼递送剂具有优势，并且可能在细胞水平上显著提高硼递送能力。利用中子放射自显影成像和定量分析，在U87 - MG胶质母细胞瘤细胞系中测试了该化合物在硼摄取方面的性能。该化合物对细胞无毒，并且显示出显著的使细胞富集硼的能力。将培养基中提供的硼浓度与细胞中达到的硼浓度之比与用硼替苯胺（BPA，BNCT中的金标准）获得的比值进行比较。结果表明，与BPA相比，该新型试剂的性能明显更好，表明该新型试剂在细胞中浓缩硼的能力比在培养基中更强。这些令人鼓舞的初步结果为其在体内试验中的潜在应用提供了一个起点。
