Radioiodinated Nitroxide Derivative for the Detection of Lipid Radicals
Radioiodinated Nitroxide Derivative for the Detection of Lipid Radicals
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用于检测脂质自由基的放射性碘化氮氧化物衍生物
DOI：
10.1021/acsmedchemlett.9b00416
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发表时间：
2020
影响因子：
4.2
通讯作者：
Mukai Takahiro
中科院分区：
文献类型：
--
作者：
Yamasaki Toshihide;Azuma Risa;Sano Kohei;Munekane Masayuki;Matsuoka Yuta;Yamada Ken-ichi;Mukai Takahiro
迄今为止，还没有开发出检测引起脂质过氧化的脂质烷基自由基（脂质自由基）的精确测量技术。因此，我们的目标是开发一种核医学成像探针，该探针可以通过与那里产生的脂质自由基特异性反应而被吸收到细胞（如生物膜）的亲脂位点。我们设计并合成了4-（4-[125 I]碘苯甲酰氨基）-2，2，6，6-四甲基哌啶-1-氧自由基，它对脂质自由基有很高的反应活性，具有很高的放化产率和纯度。细胞内滞留被发现显着增加时，脂质自由基的产生。
Thus far, no accurate measurement technology has been developed to detect lipid alkyl radicals (lipid radicals), which cause lipid peroxidation. Therefore, we aimed to develop a nuclear medical imaging probe that can be taken up in the lipophilic site in cells such as biological membranes, by reacting specifically with the lipid radicals generated there. We designed and synthesized 4-(4-[125I]iodobenzamido)-2,2,6,6-tetramethylpiperidine-1-oxyl, which shows high reactivity to lipid radicals with a high radiochemical yield and purity. Intracellular retention was found to increase significantly when lipid radicals were produced.