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静脉注射一种高度亲水性八面体铼簇配合物(一种新的有前景的X射线造影剂)后的细胞内化及形态学分析

Cellular internalization and morphological analysis after intravenous injection of a highly hydrophilic octahedral rhenium cluster complex - a new promising X-ray contrast agent.

作者信息

Krasilnikova Anna A, Solovieva Anastasiya O, Trifonova Kristina E, Brylev Konstantin A, Ivanov Anton A, Kim Sung-Jin, Shestopalov Michael A, Fufaeva Maria S, Shestopalov Alexander M, Mironov Yuri V, Poveshchenko Alexander F, Shestopalova Lidia V

机构信息

Federal State Budgetary Scientific Institution "Scientific Institute of Clinical and Experimental Lymphology", Novosibirsk, Russian Federation.

Novosibirsk State University, Novosibirsk, Russian Federation.

出版信息

Contrast Media Mol Imaging. 2016 Nov;11(6):459-466. doi: 10.1002/cmmi.1707. Epub 2016 Aug 4.

Abstract

The octahedral cluster compound Na H [{Re Se }(P(C H CONH )(C H COO) ) ] has been shown to be highly radio dense, thus becoming a promising X-ray contrast agent. It was also shown that this compound had low cytotoxic effect in vitro, low acute toxicity in vivo and was eliminated rapidly from the body through the urinary tract. The present contribution describes a more detailed cellular internalization assay and morphological analysis after intravenous injection of this hexarhenium cluster compound at different doses. The median lethal dose (LD ) of intravenously administrated compound was calculated (4.67 ± 0.69 g/kg). Results of the study clearly indicated that the cluster complex H [{Re Se }(P(C H CONH )(C H COO) ) ] was not internalized into cells in vitro and induced only moderate morphological alterations of kidneys at high doses without any changes in morphology of liver, spleen, duodenum, or heart of mice. Copyright © 2016 John Wiley & Sons, Ltd.

摘要

八面体簇合物 NaH[{ReSe}(P(C₆H₅CONH)(C₂H₅COO)₃)] 已被证明具有高放射密度,因此成为一种有前景的 X 射线造影剂。还表明该化合物在体外具有低细胞毒性作用,在体内具有低急性毒性,并且通过尿路从体内迅速消除。本论文描述了在静脉注射不同剂量的这种六铼簇合物后更详细的细胞内化试验和形态学分析。计算了静脉给药化合物的半数致死剂量(LD₅₀)(4.67 ± 0.69 g/kg)。研究结果清楚地表明,簇合物 H[{ReSe}(P(C₆H₅CONH)(C₂H₅COO)₃)] 在体外不会内化到细胞中,并且在高剂量时仅引起小鼠肾脏的中度形态改变,而肝脏、脾脏、十二指肠或心脏的形态没有任何变化。版权所有 © 2016 约翰威立父子有限公司。

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