硼
中子俘获
放射化学
化学
体内
细胞毒性
核化学
体外
生物化学
有机化学
生物
生物技术
作者
Ruixi Li,Juanjuan Zhang,Jing-xuan Guo,Yue Xu,Kunyuan Duan,Jinrong Zheng,Hao Wan,Zhenwei Yuan,Haiyan Chen
标识
DOI:10.1021/acs.molpharmaceut.9b00898
摘要
Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content and/or poor tumor-targeting ability, limiting their application. In this study, we designed and synthesized a series of nontoxic, dual-target boron carriers (B139, B142, and B151) with the ability to accumulate specifically in tumor cells. We found that the B139 uptake into hypoxic tumor regions was high, with a 70-fold boron content compared to BPA. In addition, in vivo observation showed that B139 can be trapped in tumor cells for a prolonged period and maintains an effective therapeutic concentration, with a peak boron concentration of 50.7 μg/g and a high tumor: blood boron ratio of >3, achieving ideal BNCT conditions. Cytotoxicity evaluation in mice further proved that B139 is safe and reliable. Therefore, B139 has great potential for BNCT application as a dual-target, safe, and efficient boron carrier.
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