可控去除放射性标记基团以优化核成像的一氧化氮响应性生物正交裂解反应。
Controllable stripping of radiolabeled group to optimize nuclear imaging NO-responsive bioorthogonal cleavage reaction.
作者信息
Li Hua, Huang Lumei, Jiang Hailong, Fang Jianyang, Guo Zhide, Gao Fei, Chen Mei, Xu Duo, Li Zijing, Zhang Xianzhong
机构信息
Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University Xiamen Fujian 361102 China
College of Materials Science and Engineering, Hunan University Changsha Hunan 410082 China.
出版信息
RSC Adv. 2020 Nov 3;10(66):40030-40034. doi: 10.1039/d0ra07186b. eCollection 2020 Nov 2.
A novel "turn-off" strategy for controllable radionuclide clearance is established. 1,4-dihydropyridine (DHP) is used as a conditional linker to connect a radioisotope labeled moiety and nano-agent. A highly specific, sensitive and effective C-C bond cleavage of DHP happens when treated with nitric oxide which is provided by glyceryl trinitrate (GTN). The radioactive cut-off part from the nanoparticle is observed to be cleared quickly by microSPECT-CT. 3-5 times decreases of radioactivity in the blood, kidneys, intestine, heart and lungs are observed after GTN treatment in a biodistribution assay. The radioactivity redistribution indicates that the radioactive leaving part is indeed cut off and the radionuclide metabolism accelerated. Organ level internal dose assessment reveals the GTN treated groups carry only ½ the radiation dose of the control group. Collectively, a feasible pathway for controllable radionuclide clearance is for the first time provided for high contrast and low radiation nuclear imaging.
建立了一种用于可控放射性核素清除的新型“关闭”策略。1,4-二氢吡啶（DHP）用作条件连接体，连接放射性同位素标记部分和纳米剂。当用由三硝酸甘油酯（GTN）提供的一氧化氮处理时，DHP会发生高度特异性、灵敏且有效的C-C键断裂。通过微型单光子发射计算机断层扫描-计算机断层扫描（microSPECT-CT）观察到纳米颗粒上的放射性切断部分被快速清除。在生物分布试验中，GTN处理后，血液、肾脏、肠道、心脏和肺部的放射性降低了3至5倍。放射性重新分布表明放射性离开部分确实被切断，放射性核素代谢加速。器官水平的内照射剂量评估显示，GTN处理组的辐射剂量仅为对照组的一半。总体而言，首次为高对比度和低辐射核成像提供了一条可行的可控放射性核素清除途径。
Zotero 插件