Cyclometalated iridium(III) dithioformic acid complexes as mitochondria-targeted imaging and anticancer agents
作者:Yuting Wu、Jinfeng Liu、Mingxiao Shao、Pei Zhang、Shaohua Song、Ge Yang、Xicheng Liu、Zhe Liu
DOI:10.1016/j.jinorgbio.2022.111855
日期:2022.8
Four neutral cyclometalated iridium(III) (IrIII) dithioformic acid complexes ([(ppy)2Ir(S^S)], Ir1-Ir4) were designed and synthesized. Toxicity assay revealed that these complexes showed favorable anticancer activity, especially for human non-small cell lung cancer cells (A549). Ir1 exhibited the best anticancer activity (11.0 ± 0.4 μM) was about twice that of cisplatin, meanwhile, which could availably
设计并合成了四种中性环金属化铱(III)(Ir III )二硫代甲酸配合物([(ppy) 2 Ir(S^S)], Ir1-Ir4 )。毒性测定表明,这些复合物显示出良好的抗癌活性,尤其是对人类非小细胞肺癌细胞 (A549)。Ir1表现出最佳的抗癌活性(11.0±0.4μM)约为顺铂的两倍,同时可有效抑制A549细胞迁移。复合物可以靶向线粒体,诱导线粒体膜电位 (MMP) 降低,导致细胞内活性氧 (ROS) 增加和细胞周期中断,最终产生细胞凋亡。Western blotting实验表明,复合物可以抑制B细胞CLL/lymphoma-2蛋白(Bcl-2)的表达,诱导BCL2相关X蛋白(Bax)的表达,导致细胞色素C(Cyt-c)的大量释放。 ),通过激活下游通路来放大细胞凋亡信号,促进细胞凋亡。所有这些都证实了这些复合物存在线粒体抗癌通道。首先,