Institut für Anorganische und Analytische Chemie Friedrich-Schiller-Universität Jena Humboldtstraße 8, 07743 Jena, Germany.
Department of Gynecology, Jena University Hospital - Friedrich Schiller University Jena, Germany.
Dalton Trans. 2016 Nov 29;45(47):18876-18891. doi: 10.1039/c6dt01388k.
We report on platinum(ii) complexes with different cinnamic acid derivatives as ligands with cytotoxic activity against Cisplatin resistant ovarian cancer cell line subcultures of SKOV3 and A2780. A typical mechanism of action for platinum(ii) complexes as Cisplatin itself is binding to the DNA and inducing double-strand breaks. We examined the biological behavior of these potential drugs with 9-methylguanine using NMR spectroscopic methods and their DNA damage potential including γH2AX-foci analyses. X-ray diffraction methods have been used to elucidate the molecular structures of the platinum(ii) complexes. Interactions with the model protein lysozyme have been evaluated by different techniques including UV-Vis absorption spectroscopy, fluorescence and X-ray crystallography.
我们报告了一系列以不同肉桂酸衍生物作为配体的铂（II）配合物，这些配合物对顺铂耐药的卵巢癌细胞系 SKOV3 和 A2780 的亚系具有细胞毒性。铂（II）配合物与顺铂本身一样，其典型的作用机制是与 DNA 结合并诱导双链断裂。我们使用 NMR 光谱方法研究了这些潜在药物与 9-甲基鸟嘌呤的相互作用，并通过 γH2AX 焦点分析研究了它们的 DNA 损伤潜力。X 射线衍射方法已被用于阐明铂（II）配合物的分子结构。通过包括紫外可见吸收光谱、荧光和 X 射线晶体学在内的不同技术，评估了它们与模型蛋白溶菌酶的相互作用。
