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Metabolizer in vivo of fullerenes and metallofullerenes by positron emission tomography

机译:正电子发射断层显像技术在体内富勒烯和金属富勒烯的代谢产物

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摘要

Fullerenes (C-60) and metallofullerenes (Gd@C-82) have similar chemical structure, but the bio-effects of both fullerene-based materials are. distinct in vivo. Tracking. organic carbon-based materials such as C-60 and Gd@C-82 is difficult in vivo due to the high content of carbon element in the living tissues themselves. In this study, the biodistribution and metabolism of fullerenes (C-60 and Gd@C-82) radiolabeled with Cu-64 were observed by positron emission tomography (PET). Cu-64-C-60 and Cu-64-Gd@C-82 were prepared using 1, 4, 7, 10-tetrakis (carbamoylmethyl)-1, 4, 7, 10-tetra-azacyclodo-decanes grafted on. carbon cages as a. chelator for Cu-64, and were obtained rapidly with high radiochemical yield (>= 90%). The new radio-conjugates were evaluated in vivo in the normal mouse model and. tissue distribution by small animal PET/CT imaging and histology was carried out. The PET imaging, the biodistribution and the excretion of C-60 and Gd@C-82. indicated that C-60 samples have. higher blood retention and. lower renal clearance than the Gd@C-82 samples in vivo and suggested that the differences in. metabolism and distribution in vivo were caused by the structural. differences of the groups on the fullerene cages though there is chemical similarity between C-60 and Gd@C-82.
机译:富勒烯(C-60)和金属富勒烯(Gd @ C-82)具有相似的化学结构,但两种基于富勒烯的材料的生物效应都相同。不同的体内。跟踪。有机碳基材料(例如C-60和Gd @ C-82)在体内是困难的,因为活组织本身中的碳元素含量很高。在这项研究中,通过正电子发射断层扫描(PET)观察了用Cu-64放射性标记的富勒烯(C-60和Gd @ C-82)的生物分布和代谢。使用接枝的1、4、7、10-四(氨基甲酰基甲基)-1、4、7、10-四氮杂双环癸烷制备Cu-64-C-60和Cu-64-Gd @ C-82。碳笼Cu-64的螯合剂,并以高放射化学收率(> = 90%)快速获得。在正常小鼠模型中和体内评估了新的放射性结合物。通过小动物PET / CT成像和组织学进行组织分布。 PET成像,C-60和Gd @ C-82的生物分布和排泄。表示有C-60样品。血液保持力更高。体内肾清除率比Gd @ C-82样本低,提示体内代谢和分布的差异是由结构引起的。 C-60和Gd @ C-82在化学上有相似之处,但富勒烯笼上基团的差异。

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