Synthesis and Use of Hyaluronic Acid–10B Polymeric Chelates for Neutron-Capture Therapy
Synthesis and Use of Hyaluronic Acid–10B Polymeric Chelates for Neutron-Capture Therapy
复制标题
透明质酸-10B聚合物螯合物的合成及其在中子捕获治疗中的应用
DOI：
10.1007/s11094-013-0947-9
复制
发表时间：
2013
影响因子：
0.9
通讯作者：
S. Ulyanenko
中科院分区：
文献类型：
--
作者：
S. Koryakin;P. Ivanov;V. N. Khabarov;V. Yadrovskaya;E. Isaeva;E. Beketov;A. Zelenetskii;S. Uspenskii;M. Selyanin;S. Ulyanenko
开发了十氢硼酸钠在布里奇曼砧中变形固态修饰透明质酸（HA）的技术。变形在1GPa的压力和500°的旋转角度下进行。研究了所得配合物的结构。使用拉曼光谱和红外傅里叶光谱表明，HA 和聚硼酸盐可以形成环状聚合物螯合物网络，其中 HA 作为多齿配体。在单次瘤内给药后，研究了基于 HA 的含 B 化合物在 B-16 黑色素瘤小鼠器官和组织中的生物分布。给药后15分钟观察到肿瘤中B含量最大。但1小时后减半，3小时后减少5倍。进行硼中子捕获治疗的最佳时间是给药后 30 分钟，此时肿瘤 B 浓度 >30 μg/g 并超过周围组织的含量。肿瘤/肌肉和肿瘤/血液的比率分别达到3和5。根据临床前研究，使用这种无毒化合物进行中子捕获疗法被认为是有前途的。
The technology of solid-state modification of hyaluronic acid (HA) with sodium decahydroborate by deformation in Bridgman anvils was developed. The deformation was carried out at a pressure of 1 GPa and a rotation angle of 500°. The structure of the obtained complexes was studied. It was shown using Raman and IR-Fourier spectroscopy that HA and the polyborates could form a network of cyclic polymeric chelate complexes in which HA acted as a multidentate ligand. The biodistribution of the HA-based B-containing compound in organs and tissues of mice with B-16 melanoma was studied after a single intratumoral administration. The maximum B content in the tumor was observed 15 min after administration. However, it was halved after 1 h and decreased by 5 times by 3 h. The most opportune time for performing a boron-neutron-capture therapy session was 30 min after administration when the tumor B concentration was >30 μg/g and exceeded the content in surrounding tissues. The tumor/muscle and tumor/blood ratios reached 3 and 5, respectively. Use of this non-toxic compound for neutron-capture therapy was deemed promising based on preclinical studies.