含 BODIPY 和姜黄素类硼追踪药物的设计、合成及用于中子动态治疗的破坏动态效应。

Design, synthesis and destructive dynamic effects of BODIPY-containing and curcuminoid boron tracedrugs for neutron dynamic therapy.

机构信息

Department of Life System, Institute of Technology and Science, Graduate School, The University of Tokushima, Minamijosanjimacho-2, Tokushima, 770-8506 Japan.

出版信息

Anticancer Res. 2011 Jul;31(7):2477-81.

PMID:21873162

Abstract

BACKGROUND

We previously designed the boron tracedrugs UTX-42, UTX-43, and UTX-44, which possess antioxidant potency. In order to explore their destructive dynamic effects when bombarded by weak thermal neutrons, we performed thermal neutron irradiation of bovine serum albumin (BSA) treated with the boron tracedrugs.

MATERIALS AND METHODS

Boron tracedrugs, including the boron dipyrromethene (BODIPY)-containing compounds UTX-42, UTX-44, and UTX-47 and the curcuminoid compounds UTX-50 and UTX-51, were designed for neutron dynamic therapy based on their molecular orbital calculation. Newly designed UTX-47, UTX-50, and UTX-51 were synthesized. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was performed to detect decomposition by thermal neutron irradiation of BSA treated with these boron tracedrugs.

RESULTS

The combination of 1.0 μM BSA with 100 μM of each of the boron tracedrugs showed a decrease in band intensity after irradiation.

CONCLUSION

All boron tracedrugs tested caused destructive dynamic damage of BSA during thermal neutron irradiation, suggesting that boron tracedrugs could be used as dynamic drugs for neutron dynamic therapy.

摘要

背景

我们之前设计了具有抗氧化能力的硼示踪药物 UTX-42、UTX-43 和 UTX-44。为了探索它们在弱热中子轰击下的破坏动力学效应，我们对用硼示踪药物处理的牛血清白蛋白（BSA）进行了热中子辐照。

材料和方法

硼示踪药物，包括含有硼二吡咯甲川（BODIPY）的化合物 UTX-42、UTX-44 和 UTX-47 以及姜黄素化合物 UTX-50 和 UTX-51，是根据它们的分子轨道计算设计用于中子动力学治疗的。新设计的 UTX-47、UTX-50 和 UTX-51 已被合成。用热中子辐照用这些硼示踪药物处理的 BSA 后，通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳（SDS-PAGE）检测分解情况。