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终端连接体的PEGylation作为一种降低无线电对比物 Re₆-集群毒性的途径

Aleksei S Pronin¹, Tatiana N Pozmogova¹, Yuri A Vorotnikov¹

¹Nikolaev Institute of Inorganic Chemistry SB RAS, 3 Acad. Lavrentiev Ave., Novosibirsk 630090, Russia.

International journal of molecular sciences

|December 9, 2023

概括

研究人员开发了PEGylated rhenium集群作为更安全的X射线对比剂. 这种修改显著降低了毒性,使得通过血管学和CT扫描在老鼠中有效地可视化血管.

科学领域:

无机化学无机化学
材料科学材料科学材料科学
放射学放射学是一门学科.

背景情况:

传统的X射线对比介质表现出副作用,需要开发新的药物.
团 (Na2H14[{Re6Q8}(P(C2H4COO)3) [6]) 显示出作为X射线对比剂的潜力,但由于它们的电荷,它们具有高毒性.

研究的目的:

为了降低团的毒性,用于用作X射线对比剂.
评估PEGylation作为一种减轻团毒性策略的有效性.

主要方法:

使用聚乙烯糖醇 (PEG-400) 在酸性水性介质中对集群进行PEGylation.
对Hep-2细胞的细胞毒性和小鼠的急性毒性的评估.
用血管学和计算机断层学评估PEGylated化合物用于大鼠的血管可视化.

主要成果:

最多5个碳酸盐组与PEG成功结合到团.
在PEGylation后,观察到细胞毒性和急性毒性减少了两倍.
PEGylated rhenium集群有效地可视化了实验室老鼠的血管.

结论:

基化是一种成功的策略,可以降低团的毒性.
修改后的团是更安全的X射线对比剂的有希望的候选者.
这项研究表明了这些药物在诊断成像应用中的潜力.

关键词:

通过PEGylation进行化.在X射线对比介质中,X射线对比介质是对比的.剧烈毒性的急性毒性血管造影 - 血管造影计算机断层扫描 (CT) 是一种计算机断层扫描.细胞毒性细胞毒性八面体的石化化团团.氨酸氨酸是什么意思

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