Ru(II)-polypyridyl complexes have been widely studied and well established for their antitumor properties. Modifications of the coordination environment around the Ru atom through a proper choice of the ligand can lead to different modes of action and result in greatly improved anticancer efficacy. Herein, two Ru(II)-polypyridyl complexes of curcumin were synthesized and characterized as potential anticancer agents. In vitro tests indicated that complexes 1 and 2 displayed excellent antiproliferative activity against the tested cancer cell lines, especially complex 2, which exhibited superior cytotoxicity compared to curcumin and cisplatin. Further biological evaluations demonstrated that complexes 1 and 2 can cause cell apoptosis via DNA interaction and MEK/ERK signaling pathway, which is the first example of a Ru(II)-polypyridyl complex inhibiting the MEK/ERK signaling pathway and DNA intercalation. Overall, this work suggests that coordination with bioactive agents may endow Ru(II)-polypyridyl complexes with improved pharmaceutical properties and synergistic effects for cancer therapy.

中文翻译：

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姜黄素双功能钌（ii）聚吡啶基复合物作为潜在的抗癌药。

Ru（II）-聚吡啶基配合物已被广泛研究并因其抗肿瘤特性而得到了充分的确立。通过正确选择配体来修饰Ru原子周围的配位环境可导致不同的作用方式，并大大提高抗癌功效。在此，合成了姜黄素的两种Ru（II）-聚吡啶基复合物，并将其表征为潜在的抗癌剂。体外测试表明，复合物1和2对测试的癌细胞系，尤其是复合物2具有优异的抗增殖活性与姜黄素和顺铂相比具有更高的细胞毒性。进一步的生物学评估表明，复合物1和2可通过DNA相互作用和MEK / ERK信号通路引起细胞凋亡，这是Ru（II）-聚吡啶基复合物抑制MEK / ERK信号通路和DNA嵌入的第一个例子。总的来说，这项工作表明与生物活性剂的协调可以使Ru（II）-聚吡啶基复合物具有改善的药物特性和协同作用，以治疗癌症。