Radionuclide-labeled boron delivery agents
Radionuclide-labeled boron delivery agents
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DOI：
10.1360/tb-2021-0891
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发表时间：
2021-10
影响因子：
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通讯作者：
S. Li;Taiwei Chu
中科院分区：
文献类型：
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作者：
S. Li;Taiwei Chu
硼中子俘获疗法（BNCT）作为一种结合中子照射和含硼靶向药物的二元放射治疗方法，备受关注。 BNCT的成功主要取决于三个方面：（1）理想的硼输送剂；（2）合理的中子源；（3）准确的剂量测量系统。因此，实现患者体内硼浓度的快速、准确测量非常重要。有多种方法用于测量硼浓度。间接测量方法往往需要血液/组织样本，因此只能给出单个时间点和采样点的硼浓度的估计，而不能准确描述 10 B浓度的生物分布以及靶组织和非靶组织之间的硼浓度比。磁共振成像（MRI）的灵敏度较差，而放射性核素成像是一种非侵入性方法，可以提供硼输送剂在体内的分布情况。本文简要介绍了BNCT中硼浓度的现有测量方法，以及用于放射性核素成像的硼传递剂（如4-硼基-L-苯丙氨酸（BPA）和硫醇十氢十二硼酸二钠（BSH））的放射性核素（ 18 F、 125 I/ 131 I和 99m Tc）标记方法的进展。用 18 F 标记硼递送剂的常用方法是使用载体的[ 18 F]F 2 亲电取代、不使用载体的[ 18 F]F - 亲核取代以及同位素交换。 18 F标记的BPA（[ 18 F]-FBPA）首先通过亲电取代法制备。研究表明，BPA 和 [ 18 F]-FBPA 具有相似的药代动力学，并且
Boron neutron capture therapy (BNCT), as a duality radiotherapy method that combines neutron irradiation and boron-containing targeted drugs, has attracted much attention. The successful BNCT mainly depends on three aspects: (1) Ideal boron delivery agents, (2) reasonable neutron source, and (3) accurate dose measurement system. Therefore, it is very important to realize the rapid and accurate measurement of the boron concentration in the patient. There are a variety of methods that have been used to measure the boron concentration. The indirect measurement method often requires the blood/tissue sample, so it can only give an estimate of the boron concentration at a single time point and sampling point, but cannot accurately describe the biodistribution of 10 B concentration and the boron concentration ratio between target and non-target tissues. The sensitivity of magnetic resonance imaging (MRI) is poor, while radionuclide imaging is a non-invasive method and can provide the distribution of boron delivery agents in vivo . This article briefly describes the existing methods of measuring the boron concentration in BNCT, and the progress of radionuclide ( 18 F, 125 I/ 131 I, and 99m Tc) labeling methods of boron delivery agents (such as 4-borono- L -phenylalanine (BPA) and disodium mercaptoundecahydrodode-caborate (BSH)) for radionuclide imaging. The common methods for labeling boron delivery agents with 18 F are [ 18 F]F 2 electrophilic substitution with a carrier, [ 18 F]F − nucleophilic substitution without a carrier, and isotope exchange. 18 F-labeled BPA ([ 18 F]-FBPA) was first prepared by the electrophilic substitution method. Researches have shown that BPA and [ 18 F]-FBPA had similar pharmacokinetics and