Quiroga Adoración G, Cubo Leticia, de Blas Elena, Aller Patricio, Navarro-Ranninger Carmen
Departamento de Química Inorgánica, Universidad Autónoma de Madrid, 28049 Madrid, Spain.
J Inorg Biochem. 2007 Jan;101(1):104-10. doi: 10.1016/j.jinorgbio.2006.08.012. Epub 2006 Sep 5.
In an attempt to design new antitumoral drugs based on transplatin complexes, we determined the experimental conditions for the preparation of trans-[Pt((CH(3))(2)CNOH)((CH(3))(2)CHNH(2))Cl(2)], and solved the crystal structure. The cytotoxicity of the novel complex, the cis counterpart, cisplatin, and a trans complex with aliphatic amines, as well as the capacity of some of these complexes to cause either apoptotic or necrotic cell death, was comparatively examined in NRK-52E rat renal tubular cells and HepG2 human hepatoma cells. The results indicate that the oxime complex with trans geometry, but not the one with cis geometry, causes death by apoptosis, making the complex potentially suitable for therapeutic purposes. However cytotoxicity values are higher in the case of cis geometry than in trans geometry in both tumoral and non-tumoral cell lines.
为了设计基于反式铂配合物的新型抗肿瘤药物，我们确定了制备反式-[Pt((CH(3))(2)CNOH)((CH(3))(2)CHNH(2))Cl(2)]的实验条件，并解析了其晶体结构。在NRK-52E大鼠肾小管细胞和HepG2人肝癌细胞中，对该新型配合物、其顺式对应物顺铂以及一种含脂肪胺的反式配合物的细胞毒性，以及这些配合物中某些引起凋亡或坏死性细胞死亡的能力进行了比较研究。结果表明，具有反式几何结构的肟配合物而非顺式几何结构的肟配合物可导致细胞凋亡死亡，这使得该配合物具有潜在的治疗用途。然而，在肿瘤细胞系和非肿瘤细胞系中，顺式几何结构的细胞毒性值均高于反式几何结构。
