doi:10.12202/j.0476-0301.2021013赵云岺^,
北京师范大学化学学院，100875，北京

详细信息

通讯作者:赵云岺（1963—），博士，高级实验师. 研究方向：核药物化学. E-mail: ylzhao@bnu.edu.cn

中图分类号:O61

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出版历程

收稿日期:2021-01-24
网络出版日期:2021-03-31
刊出日期:2021-09-02

Glucose regulates cellular uptake of boric acid and substituted boric acid

Yunling ZHAO^,
College of Chemistry, Beijing Normal University, 100875, Beijing, China



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摘要
摘要:硼中子俘获治疗(boron neutron capture therapy, BNCT)是肿瘤治疗的一种二元体系，利用含¹⁰B药物对肿瘤细胞的高选择性、在肿瘤细胞中有足够的富集量和滞留时间，用具有合适能量的超热中子束照射肿瘤部位，发生中子俘获反应¹⁰B(n，α)⁷Li，反应释放出的高传能线密度α粒子和⁷Li，在一个细胞大小范围杀死肿瘤细胞．因此，含¹⁰B药物的高效、高选择性对肿瘤细胞的靶向输送是BNCT有效性提高的关键．为了提高肿瘤细胞对含硼化合物的吸收，本文基于糖类物质与硼酸及其衍生物的相互作用，以及糖类具有在肿瘤细胞中富集的性质，研究了葡萄糖对正常细胞和肿瘤细胞吸收硼酸及其衍生物的影响，探讨了利用糖类物质增加肿瘤细胞中¹⁰B含量的可能性．研究结果表明，随着葡萄糖含量的增加，肿瘤细胞对硼酸及取代硼酸的吸收增加，而正常细胞的吸收增加不明显．此外，葡萄糖对硼化合物在细胞中的滞留无明显的影响．
关键词:硼中子俘获治疗/
葡萄糖/
硼酸/
取代硼酸
Abstract:Boron neutron capture therapy (BNCT) is a binary radiotherapeutic modality based on nuclear capture and fission reactions that occur when the stable isotope boron-10 is irradiated with neutrons to produce high energy α particles．For this to be successful,?about 20 μg·g^?1 of ¹⁰B (per weight of tumor) must be selectively delivered to tumor cells (≈?10⁹ atoms·cell^?1), and enough neutrons must be absorbed to sustain a lethal ¹⁰B(n, α)⁷Li capture reaction．Therefore the key to enhance effectiveness of BNCT is for ¹⁰B to be targeted to tumor cells efficiently and selectively．Carbohydrates are known to accumulate in tumor cells．Increased boron uptake in tumor cells is expected after introducing carbohydrates in the form of covalently-bonded complexes of boric acid or derivatives．It was found that the uptake of boric acid and derivatives by tumor cells increased with increasing concentrations of glucose, but glucose uptake by normal cells did not increase markedly．Glucose had no effect on cellular persistence of boron compounds．
Key words:boron neutron capture therapy (BNCT)/
glucose/
boric acid/
substituted boric acid