硼氨基酸以及碳硼烷类硼中子俘获剂研究进展

Development of boron amino acids and carboranes in boron neutron capture agents

硼中子俘获疗法(BNCT)是一种用于治疗癌症的方法,可以用于治疗头颈部肿瘤等。虽然一些临床前研究已经证明了BNCT的潜力,但该技术还尚未作为治疗肿瘤的主流方案中得到完全接受。部分原因是由于患者对携带剂摄取和分布的差异性较大,另外也归因于肿瘤与血液中10B浓度比存在不确定性。现在主要使用成像技术来确定硼中子俘获剂在生物体内的生物分布。硼苯丙氨酸(BPA)和巯基钠氢氯十二碳酸钠(BSH)是目前硼中子俘获疗法(BNCT)主要的硼传递剂,其中18FBPA已被用于BPA-BNCT治疗,而研究者也在BSH结构的启发下对碳硼烷进行了各种放射性核素标记。本篇综述调查了近年来硼氨基酸以及碳硼烷类硼传递剂的研究,并概述放射性核素标记的硼传递剂在核医学影像中的研究和应用。

Boron neutron capture therapy(BNCT)is a method used to treat cancer,and it can be used to treat brain and head and neck tumors.Although the potential of BNCT has been demonstrated in some preclinical studies,the technology has not yet been fully accepted in many options for the treatment of tumors.Part of the reason is the difference in the uptake and distribution of 10B by patients,and it is also due to the uncertainty of the ratio of tumor to blood 10B concentration.Imaging techniques are now mainly used to determine the in vivo biodistribution of BNCT agents.At present,most researches are devoted to the most promising BNCT reagents.Boron phenylalanine(BPA)and sodium borocaptate(BSH)are the main boron delivery agents for boron neutron capture therapy.18FBPA has been developed to assist the treatment plan of BPA-BNCT,and some researchers have also carried out various nuclide labeling of carborane inspired by the structure of BSH.The research on BPA and carborane type boron delivery agents in the past few years was investigated in this review,and research and application of the radionuclide-labeled boron delivery agents in nu-clear medicine imaging research were reviewed.