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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Cyclometalated iridium(III)-guanidinium complexes as mitochondria-targeted anticancer agents
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Cyclometalated iridium(III)-guanidinium complexes as mitochondria-targeted anticancer agents

机译：与线粒体靶向抗癌剂的环状氧化铱（III） - 胍含量

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Abstract Guanidinium-functionalized molecules are commonly studied for their use as pharmaceutically active compounds and drugs carriers. Herein, four cyclometalated iridium(III) complexes containing guanidinium ligands have been synthesized and characterized as potential anticancer agents. These complexes exhibit moderate antitumor activity in HeLa, MCF-7, HepG2, CNE-2, and A549 human tumor cells. Interestingly, all complexes showed higher cytotoxicity than cisplatin against a cisplatin-resistant cell line A549R, and less cytotoxicity on the nontumorigenic LO2 cells. Intracellular distribution studies suggest that these complexes are selectively localized in the mitochondria. Mechanism studies indicate that these complexes arrested the cell cycle in the G0/G1 phase and can influence mitochondrial integrity, inducing cancer cell death through reactive oxygen species (ROS)-dependent pathways. Graphical abstract Four cyclometalated iridium(III) complexes containing guanidinium ligands have been synthesized and characterized. These complexes display moderate cytotoxicity by specifically targeting mitochondria and inducing a cascade of apoptotic events related to mitochondrial dysfunction. Display Omitted Highlights ? Four Ir(III) complexes containing guanidinium ligands were synthesized. ? Four complexes displayed higher antiproliferative activities than cisplatin against cisplatin-resistant A549?cells. ? Complexes 1 and 2 mainly located mitochondria in HeLa cancer cells. ? Complexes 1 and 2 increased ROS production and induced cell cycle arrest in G0/G1 phase.
机译：摘要鸟蛋白官能化分子通常用于它们用作药物活性化合物和药物载体的用途。这里，已经合成了含有胍配体的四种环状氧化铱（III）络合物，并表征为潜在的抗癌剂。这些配合物在Hela，MCF-7，HepG2，CNE-2和A549人肿瘤细胞中表现出中度抗肿瘤活性。有趣的是，所有复合物都显示出比顺铂的细胞毒性更高，而不是顺铂抗性细胞系A549R，并且在非致素LO2细胞上的细胞毒性较少。细胞内分布研究表明这些配合物在线粒体中选择性地局部地局部化。机制研究表明，这些复合物在G0 / G1相中停止了细胞周期，并可影响线粒体完整性，通过反应性氧（ROS）依赖性途径诱导癌细胞死亡。图解摘要四种环状铱（III）含有胍配体的络合物已经合成并表征。这些复合物的特异性靶向线粒体和诱导与线粒体功能障碍凋亡事件的级联显示中等毒性。显示省略亮点？合成含有胍配体的四种IR（III）配合物。还是四个复合物显示比顺铂抗顺蛋白抗性A549？细胞的四个复合物。还是复合物1和2主要位于Hela癌细胞中的线粒体。还是复合物1和2增加了ROS生产和G0 / G1相中的诱导细胞周期停滞。

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