The usefulness of 2-nitroimidazole-sodium borocaptate-10B conjugates as 10B-carriers in boron neutron capture therapy
The usefulness of 2-nitroimidazole-sodium borocaptate-10B conjugates as 10B-carriers in boron neutron capture therapy
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DOI：
10.1016/j.apradiso.2004.05.018
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发表时间：
2004-11-01
影响因子：
1.6
通讯作者：
Ono, K
中科院分区：
文献类型：
--
作者：
Masunaga, S;Nagasawa, H;Ono, K
我们评估了五种新的B-10化合物（TX-2016、TX-2017、TX-2018、TX-2041和TX-2042）作为硼中子俘获治疗（BNCT）中的B-10载体的有用性。它们是2-硝基咪唑-硼酸钠-B-10（BSH）共轭物，即同时具有γ射线照射下的乏氧肿瘤细胞增敏单元2-硝基咪唑和热中子增敏单元BSH的杂化化合物。肿瘤和血液中的B-10分布分析表明，TX-2041具有最有利的特性，可将足够量的B-10定位到肿瘤中，并在中子束照射期间保持高B-10浓度。此外，TX-2041对实体瘤中的总（=增殖（P）+静止（Q））和富缺氧Q细胞群的放射增敏作用显著高于BSH。此外，TX-2041清楚地证明了γ射线对两种细胞群的放射增敏作用，这是BSH永远无法实现的。B-10-载体，具有对肿瘤的低氧肿瘤细胞的γ射线敏化作用以及选择性定位和保持B-10在肿瘤中的潜力，如TX-2041。有望用于实际的BNCT。(C)2004爱思唯尔有限公司保留所有权利。
We evaluated the usefulness of five new B-10-compounds (TX-2016, TX-2017, TX-2018, TX-2041, and TX-2042) as B-10-carriers in boron neutron capture therapy (BNCT). They are 2-nitroimidazole-sodium borocaptate-B-10 (BSH) conjugates, that is, hybrid compounds that have both hypoxic tumor cell sensitizing unit under gamma-ray irradiation, 2-nitroimidazoles, and thermal neutron-sensitizing unit, BSH. B-10 distribution analyses in tumors and blood indicated that TX-2041 has the most favorable characteristics for localizing a sufficient amount of B-10 into tumors and keeping the B-10 concentration high during neutron beam irradiation. In addition, TX-2041 showed a significantly higher radio-sensitization effect with reactor thermal neutron beams than BSH on both total (= proliferating (P) + quiescent (Q)) and hypoxia-rich Q cell populations in solid tumors. Further, TX-2041 clearly demonstrated a radio-sensitization effect with gamma-rays on both cell populations, which could never be achieved by BSH. B-10-carrier with a hypoxic tumor cell-sensitizing effect on tumors with gamma-rays as well as the potential to selectively localize and keep B-10 in tumors, such as TX-2041. are promising for use in actual BNCT. (C) 2004 Elsevier Ltd. All rights reserved.