碳硼烷作为药效团在硼中子俘获疗法中的研究进展  

Research Progress of Carborane as Pharmacophore in Boron Neutron Capture Therapy

作　　者：廖才智 叶涛生 钟琴 姜涛 衷友泉[1] LIAO Caizhi;YE Taosheng;ZHONG Qin;JIANG Tao;ZHONG Youquan(College of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330000,Jiangxi,China)

机构地区：[1]江西中医药大学药学院,江西南昌330000

出　　处：《现代诊断与治疗》2024年第12期1767-1774,共8页Modern Diagnosis and Treatment

基　　金：江西省教育厅科技项目-2023年大学生省级创新创业训练计划(项目编号:S202310412099)。

摘　　要：硼中子俘获疗法(Boron neutron capture therapy,BNCT)是一种肿瘤选择性粒子放疗,是基于给予肿瘤细胞优先掺入的硼载体,然后用热或超热中子束照射,能最大限度地减少对健康组织的损伤。然而,目前已经进入临床研究的两个硼载体-硼苯丙氨酸(BPA)和巯基钠氢氯十二碳酸钠(BSH),存在硼含量低、体内稳定性差、溶解度差、缺乏靶向性和成像示踪功能等问题,导致BNCT的临床治疗并未得到广泛应用。因此,开发符合BNCT要求的新一代硼载体或硼药是促进BNCT发展的关键。碳硼烷化合物由于10B含量高、稳定性好、毒性低,现已逐渐成为BNCT中的硼递送剂和抗肿瘤研究的热门选择。现简要介绍碳硼烷分子,并综述碳硼烷及其衍生物在BNCT中的应用以及作为BNCT/PDT双重增敏剂在抗肿瘤研究中的研究进展。Boron neutron capture therapy(BNCT)is a form of tumor-selective particle radiotherapy that involves administering a boron carrier to tumor cells,followed by irradiation with thermal or epithermal neutron beam to minimize damage to healthy tissue.However,current boron carriers used in clinical studies,such as boron phenylalanine(BPA)and sodium mercaptoundecahydro-closo-dodecaborate(BSH),have limitations including low boron content,poor stability in vivo,low solubility,and a lack of targeting and imaging capabilities,which has hindered the widespread use of BNCT in clinical settings.Therefore,the development of new boron carriers or drugs that meet the requirements of BNCT is crucial for advancing this therapy.Due to its high content of 10B,good stability,and low toxicity,carborane compounds have emerged as promising boron delivery agents for BNCT and a hotspot in anti-tumor research.This paper provides a brief overview of carborane molecules and discusses the application of carborane and its derivatives in BNCT,as well as the research progress of their role as dual sensitizers for BNCT/PDT in anti-tumor research.

关 键 词：BNCT 碳硼烷 药物化学 抗肿瘤 

分 类 号：R730.55[医药卫生—肿瘤]