新型半三明治铱 OˆC（卡宾）-配合物：通过线粒体和溶酶体之间 ROS 介导的串扰，在体外和体内抑制肿瘤生长和促进细胞凋亡。
Novel half-sandwich iridium OˆC (carbene)-Complexes: In vitro and in vivo tumor growth suppression and pro-apoptosis via ROS-mediated cross-talk between mitochondria and lysosomes.
机构信息
College of Chemistry, Chemistry Engineering and Materials Science, Shandong Normal University, Jinan, 250014, China; Institute of Anticancer Agents Development and Theranostic Application, The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine, Department of Chemistry and Chemical Engineering, Qufu Normal University, Qufu, 273165, China.
Institute of Anticancer Agents Development and Theranostic Application, The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine, Department of Chemistry and Chemical Engineering, Qufu Normal University, Qufu, 273165, China.
出版信息
Cancer Lett. 2019 Apr 10;447:75-85. doi: 10.1016/j.canlet.2019.01.018. Epub 2019 Jan 20.
Herein we present half-sandwich Ir complexes [(η-Cp)Ir(OˆC)Cl] containing OˆC(NHC)-chelating ligand as anticancer and antimetastasis agents. All the complexes displayed high potency in vitro against a wide range of cancer cells. In addition, Ir2 significantly curb tumor growth in a colon cancer mouse xenograft model in vivo. Further mechanism of action studies indicate that Ir2-initiated apoptosis occurs through ROS-mediated cross-talk between mitochondria and lysosomes.
在此，我们提出了含有 OˆC(NHC)-螯合配体的半三明治 Ir 配合物 [(η-Cp)Ir(OˆC)Cl]，作为抗癌和抗转移药物。所有配合物在体外对广泛的癌细胞均显示出高活性。此外，Ir2 在体内结肠癌小鼠异种移植模型中显著抑制肿瘤生长。进一步的作用机制研究表明，Ir2 诱导的细胞凋亡是通过 ROS 介导的线粒体和溶酶体之间的串扰发生的。
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