Departamento de Química Analítica, Nutrición y Bromatología, Facultad de Ciencias Químicas, Universidad de Salamanca, Plaza de la Merced s/n, Salamanca 37008, Spain.
Centro de Investigación del Cáncer (CIC; IBMCC CSIC/USAL), Servicio de Citometría, Departamento de Medicina and IBSAL, Universidad de Salamanca, Salamanca 37007, Spain.
J Inorg Biochem. 2014 Feb;131:8-11. doi: 10.1016/j.jinorgbio.2013.10.021. Epub 2013 Oct 31.
This article explores the potential cytotoxic activity of bile-acid cisplatin derivatives like bisursodeoxycholate(ethylenediamine)platinum(II), PtU2, when conjugated with gold nanoparticles, being a promising alternative to cisplatin in the treatment of cancer due to their lower toxicity. For our purpose we analyzed the intracellular delivery ability of these compounds after conjugation with 20-nm gold nanoparticles (PtU2-AuNPs) in the MG63 (osteosarcoma) cell line. Same platinum uptake after incubation with PtU2 and PtU2-AuNPs-derivatives is associated with a higher cytotoxic activity in case of the platinum-gold nanoparticle conjugate, the overall IC50 of PtU2 being reduced more than 10 fold for these new conjugates. When conjugated with gold nanoparticles, this bile-acid derivative is more efficient than the platinum compound alone in terms of their cytotoxic activity.
本文探讨了胆汁酸顺铂衍生物（如双牛磺脱氧胆酸（乙二胺）铂(II)，PtU2）的潜在细胞毒性活性，当与金纳米粒子缀合时，由于其毒性较低，有望成为癌症治疗中顺铂的替代物。为此，我们分析了这些化合物在与 20nm 金纳米粒子（PtU2-AuNPs）缀合后在 MG63（骨肉瘤）细胞系中的细胞内递药能力。在与 PtU2 和 PtU2-AuNPs 衍生物孵育后，相同的铂摄取与更高的细胞毒性活性相关，对于这些新的缀合物，PtU2 的总 IC50 降低了 10 倍以上。与金纳米粒子缀合时，与单独的铂化合物相比，这种胆汁酸衍生物在细胞毒性活性方面更有效。
