Tumor cell uptake and selectivity of gadolinium(III)-Phosphonium (cas 16749-13-6) complexes: The role of delocalisation at the Phosphonium (cas 16749-13-6) centre

Add time:07/19/2019    Source:sciencedirect.com

The synthesis of a series of bifunctional Gd(III) complexes 1–3 covalently bound to arylPhosphonium (cas 16749-13-6) 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.

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