Preparation and biological evaluation of radioiodine-labeled triphenylphosphine derivatives as mitochondrial targeting probes.
Preparation and biological evaluation of radioiodine-labeled triphenylphosphine derivatives as mitochondrial targeting probes.
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DOI：
10.1002/jlcr.3910
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发表时间：
2021-04
影响因子：
1.8
通讯作者：
Shuyu Shi;Zelan Liu;Zhenmin Wu;Hang Zhou;Jie Lu
中科院分区：
文献类型：
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作者：
Shuyu Shi;Zelan Liu;Zhenmin Wu;Hang Zhou;Jie Lu
带正电荷的亲脂三苯基膦阳离子(TPPS+)已被用作各种探针的线粒体靶向载体。在本研究中，我们发展了一种新的方法来制备放射性碘标记的TPPS+。以B5-B8的三苯基膦-苯基硼酸酯为原料，通过优化的铜催化一步法合成了4个125I标记的TPPS+，[125I]9-[125I]12，放化产率高(~gt；95%)。经RadioHplc纯化后，可得到比活性较高的最终产物。对其理化性质、体外细胞摄取和小鼠体内分布进行了研究。结果提示，125I标记的TPPS+具有亲脂性，可通过线粒体膜电位在富含线粒体的心肌细胞中特异性蓄积。
The positive-charged lipophilic triphenylphosphonium cations (TPPs+ ) have been served as mitochondrial targeting vehicles for the delivery of various probes. In this study, we developed a new method for the preparation of radioiodine-labeled TPPs+ . Four 125 I-labeled TPPs+ , [125 I] 9-[125 I] 12 were prepared from the corresponding triphenylphosphine phenylborate precursors of B 5-B 8 via an optimized copper-catalyzed one-step procedure in high radiochemical yield (> 95%). After Radio-HPLC purification, the final products could be obtained with high specific activity. Their physicochemical properties, in vitro cellular uptake, and ex vivo mice biodistribution were investigated. The results suggested the 125 I-labeled TPPs+ were lipophilic and could specifically accumulate in the mitochondrial-rich myocardial cells through the mitochondrial membrane potential.