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Tumor cell uptake and selectivity of gadolinium(III)-phosphonium complexes: The role of delocalisation at the phosphonium centre
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2017-07-05 , DOI: 10.1016/j.jinorgbio.2017.07.004
Madleen Busse , Madeline S.A. Windsor , Alexander J. Tefay , Mingyue Kardashinsky , Jacob M. Fenton , Daniel E. Morrison , Hugh H. Harris , Louis M. Rendina

The synthesis of a series of bifunctional Gd(III) complexes 13 covalently bound to arylphosphonium cations possessing a varying degree of delocalisation at the phosphonium centre is presented. The influence of the degree of delocalisation was investigated with regards to in vitro cytotoxicity, cellular uptake of Gd, tumor-cell selectivity and intracellular localisation of Gd within human glioblastoma (T98G) and human glial (SVG p12) cells. Cellular uptake and selectivity studies for the Gd(III) complexes indicate that a reduced delocalisation at the phosphonium centre can lead to an enhanced Gd uptake into SVG p12 cells which results in a decrease in the overall tumor cell selectivity. Synchrotron X-ray fluorescence (microbeam XRF) imaging has demonstrated for the first time that uniform uptake of Gd(III) complex 2 within a population of T98G cells increased as a function of increasing Gd incubation times. The Gd maps show dispersed spots of high intensity which are consistent with mitochondrial uptake.



中文翻译:

mor(III)-phosph配合物的肿瘤细胞摄取和选择性:phospho中心的离域作用

一系列双官能的Gd(III)的合成配合物1 - 3共价结合至芳基鏻阳离子具有在鏻中心不同程度的离域的呈现。研究了离域程度对体外的影响人胶质母细胞瘤(T98G)和人胶质细胞(SVG p12)细胞内的Gd的细胞毒性,细胞摄取Gd,肿瘤细胞选择性和细胞内Gd定位。对Gd(III)配合物的细胞摄取和选择性研究表明,center中心的离域减少可导致SVG p12细胞对Gd的摄取增加,从而导致整体肿瘤细胞选择性降低。同步加速器X射线荧光(微束XRF)成像首次证明,随着Gd孵育时间的增加,T98G细胞群中Gd(III)配合物2的均匀摄取量增加。Gd图显示了高强度的分散斑点,与线粒体摄取一致。

更新日期:2017-07-05
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