Boron neutron capture therapy (BNCT) is a binary therapeutic approach. Nonradioactive boron-10 atoms accumulated in tumor cells combining with the neutron beams produce two highly energetic particles that could eradicate the cell that takes it and the neighboring cells. Small molecules that carry boron atom, e.g. 5- and 6-boronated and 2,7-diboronated tryptophans, were assessed for their boron accumulation in U87-MG, LN229, and 3T3 for BNCT. TriBoc tryptophan, TB-6-BT, shows boron-10 at 300 ppm in both types of tumor cells with a tumor to normal ratio (T/N) of 5.19-5.25 (4 h). TB-5-BT and DBA-5-BT show boron-10 at 300 ppm (2 h) in U87-MG cells. TB-5-BT exerts a T/N of >9.66 (1 h) in LN229 compared with the current clinical boronophenyl alanine with a highest T/N of 2.3 (1 h) and accumulation concentration of <50 ppm. TB-5-BT and TB-6-BT warrant further animal study.

中文翻译：

---

通过Boc保护的色氨酸将硼积累在脑肿瘤细胞中，作为硼中子捕获疗法的载体。

硼中子捕获疗法（BNCT）是一种二元治疗方法。肿瘤细胞中积累的非放射性10硼原子与中子束结合产生两个高能粒子，它们可以消灭接受它的细胞和附近的细胞。评估了携带硼原子的小分子，例如5-和6-硼硼酸和2,7-二硼酸色氨酸，它们在BNCT的U87-MG，LN229和3T3中的硼积累情况。TriBoc色氨酸TB-6-BT在两种类型的肿瘤细胞中均显示300 ppm的硼10，肿瘤与正常比例（T / N）为5.19-5.25（4小时）。TB-5-BT和DBA-5-BT在U87-MG电池中显示300 ppm（2 h）的硼10。TB-5-BT在LN229中的T / N大于9.66（1 h），而目前临床上的硼烷苯基丙氨酸的T / N最高为2.3（1 h），累积浓度小于50 ppm。