Bifunctional ruthenium(ii) polypyridyl complexes of curcumin as potential anticancer agents†

IF 3.3 3区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR
Shuang Li, Gang Xu, Yuhua Zhu, Jian Zhao and Shaohua Gou
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引用次数: 11

Abstract

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.

Abstract Image

姜黄素双功能钌(ii)多吡啶配合物的潜在抗癌作用
Ru(II)-多吡啶配合物因其抗肿瘤特性而被广泛研究和证实。通过选择合适的配体来改变Ru原子周围的配位环境,可以导致不同的作用模式,从而大大提高抗癌效果。本文合成了两个姜黄素Ru(II)-多吡啶配合物,并将其表征为潜在的抗癌剂。体外实验表明,复合物1和2对肿瘤细胞系具有良好的抗增殖活性,特别是复合物2,与姜黄素和顺铂相比,具有更强的细胞毒性。进一步的生物学评价表明,复合物1和2可以通过DNA相互作用和MEK/ERK信号通路引起细胞凋亡,这是Ru(II)-多吡啶复合物抑制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,与生物活性药物配合可以使Ru(II)-多吡啶配合物具有更好的药物特性和癌症治疗的协同作用。
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来源期刊
Dalton Transactions
Dalton Transactions 化学-无机化学与核化学
CiteScore
6.60
自引率
7.50%
发文量
1832
审稿时长
1.5 months
期刊介绍: Dalton Transactions is a journal for all areas of inorganic chemistry, which encompasses the organometallic, bioinorganic and materials chemistry of the elements, with applications including synthesis, catalysis, energy conversion/storage, electrical devices and medicine. Dalton Transactions welcomes high-quality, original submissions in all of these areas and more, where the advancement of knowledge in inorganic chemistry is significant.
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