Tolpin E I, Wellum G R, Dohan F C, Kornblith P L, Zamenhof R G
Oncology. 1975;32(5-6):223-46. doi: 10.1159/000225073.
The use of the blood-brain barrier and of tumor-specific antibodies to concentrate boron selectivity in gliomas for neutron capture therapy is considered experimentally and theoretically. The time-dependent concentration of two anionic boranes, B12 H11 SH2- and B12 H11 SOSB12 H114-, in the blood, brain, and tumor of rats bearing a tumor of gliomatous origin is reported. The rate of clearance of each anionic borane from the blood is correlated with the fraction of non-protein bound anion in the plasma. The use of antibodies to carry therapeutical useful amounts of boron to tumor-specific or tumor-associated antigens on the tumor cell surface will require different numbers of boron atoms bound per antibody depending on several immunological and physical parameters. Calculations using published values of antibody-antigen association constants and of cell surface antigen densities predict that in order to obtain 10mug 10B/g tumor from 10 to over 10,000 boron-10 atoms will have to be bound per tumor antigenic site.
对利用血脑屏障和肿瘤特异性抗体将硼选择性地富集于神经胶质瘤中以进行中子俘获治疗进行了实验和理论上的探讨。报道了携带神经胶质瘤源性肿瘤的大鼠血液、脑和肿瘤中两种阴离子硼烷B12H11SH2-和B12H11SOSB12H114-随时间的浓度变化。每种阴离子硼烷从血液中的清除速率与血浆中非蛋白结合阴离子的比例相关。利用抗体将治疗有效量的硼携带至肿瘤细胞表面的肿瘤特异性或肿瘤相关抗原，根据若干免疫学和物理参数，每个抗体结合的硼原子数将有所不同。利用已发表的抗体-抗原结合常数和细胞表面抗原密度值进行的计算预测，为了从每个肿瘤抗原位点获得10μg 10B/g肿瘤，每个肿瘤抗原位点必须结合10至超过10000个硼-10原子。
