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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Bifunctional ruthenium(ii) polypyridyl complexes of curcumin as potential anticancer agents
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Bifunctional ruthenium(ii) polypyridyl complexes of curcumin as potential anticancer agents

机译:双官能钌(II)姜黄素复合物作为潜在的抗癌剂

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摘要

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 vitrotests indicated that complexes 1 and 2 displayed excellent antiproliferative activity against the tested cancer cell lines, especially complex2, which exhibited superior cytotoxicity compared to curcumin and cisplatin. Further biological evaluations demonstrated that complexes 1 and 2 can cause cell apoptosisviaDNA 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.
机译:Ru(II) - 普隆吡啶络合物已被广泛研究并为其抗肿瘤性质建立得很好。 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.在此,合成姜黄素的两种Ru(II) - 戊吡啶吡啶络合物,其特征为潜在的抗癌剂。蒸料表明,与姜黄素相比,复合物1和2显示出对测试的癌细胞系,尤其是复合物2的优异抗增殖活性,这与姜黄素相比表现出优异的细胞毒性。和顺铂。进一步的生物学评价证明了复合物1和2可以引起细胞凋亡症互动和MEK / ERK信号通路,这是抑制MEK / ERK信号通路和DNA嵌入的Ru(II)-polypyridyl复合物的第一实例。总体而言,这项工作表明,与生物活性剂的协调可以赋予Ru(II) - 丙基吡啶络合物,其具有改善的药物性能和癌症治疗的协同作用。

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