苯并噻唑
硼
体内
中子俘获
胶质瘤
脑瘤
血脑屏障
药品
磁导率
药理学
化学
癌症研究
放射化学
医学
内科学
病理
生物化学
有机化学
生物
中枢神经系统
生物技术
膜
作者
Jung Dug Yang,Soyeon Kim,Kyo Chul Lee,Yong Jin Lee,Jung Young Kim,Ji Ae Park
标识
DOI:10.1021/acsmedchemlett.2c00284
摘要
Boron neutron capture therapy (BNCT) is a precision treatment technology that ideally damages only boron-accumulating cells. The effectiveness of BNCT depends on the amount of boron in the tumor cells and the concentration ratio between normal and tumor tissues. Therefore, for successful brain-tumor treatment using BNCT, it is essential to develop a drug with high blood-brain barrier (BBB) permeability and high tumor accumulation. The benzothiazole-based boron complex 4-(benzo[d]thiazol-2-yl)phenylboronic acid (BTPB) is a hydrophobic, low-molecular-weight compound that has shown high BBB permeability and brain accumulation. The highest boron concentration of BTPB is 36.11 ± 2.73 μg/g (at 1 h post-injection) in the brain, and the highest brain/blood ratio is 3.94 ± 0.46 (at 2 h post-injection), which is sufficient for the BNCT drug condition. In addition, BTPB showed good tumor-targeting ability in vivo in a U87MG glioma tumor model. In this study, we conducted a biological evaluation of BTPB compared to boronophenylalanine as a novel drug for BNCT.
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