姜黄素钯(II)配合物的合成、表征及 ROS 介导的抗肿瘤作用。
Synthesis, characterization and ROS-mediated antitumor effects of palladium(II) complexes of curcuminoids.
机构信息
Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, College of Chemistry & Environmental Science, Hebei University, Baoding 071002, China.
Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, College of Chemistry & Environmental Science, Hebei University, Baoding 071002, China.
出版信息
Eur J Med Chem. 2018 Jan 20;144:662-671. doi: 10.1016/j.ejmech.2017.12.027. Epub 2017 Dec 8.
Based on the synthesis of curcumin and its derivatives from aromatic aldehydes, a novel series of palladium(II) complexes with curcumin (or its derivatives) and 2,2'-bipyridine have been synthesized through a directed self-assembly approach that involves spontaneous deprotonation of the curcuminoid ligands in HO/acetone solution. These complexes have been characterized by H (C) NMR, HRMS and elemental analysis. Crystal structure of 3h has been determined by X-ray diffraction analysis. Their cytotoxicity was tested by MTT. The preliminary results showed that complexes 3d, 3f, 3h have significant inhibition on proliferation of three carcinoma cells such as MCF-7, HeLa and A549 cells, which were more active than cisplatin. Further mechanistic studies indicated that the tested complex 3h arrested the cell cycle in the S phase and can disrupted mitochondrial membrane potential and induced tumor cell apoptosis through reactive oxygen species (ROS)-dependent pathway.
基于芳香醛与姜黄素及其衍生物的合成，通过导向自组装方法合成了一系列新型钯（II）配合物，该方法涉及在 HO/丙酮溶液中姜黄素配体的自发去质子化。这些配合物通过 H（C）NMR、高分辨率质谱和元素分析进行了表征。通过 X 射线衍射分析确定了 3h 的晶体结构。通过 MTT 测试了它们的细胞毒性。初步结果表明，配合物 3d、3f、3h 对 MCF-7、HeLa 和 A549 细胞等三种癌细胞的增殖有显著抑制作用，其活性强于顺铂。进一步的机制研究表明，测试的配合物 3h 将细胞周期阻滞在 S 期，并能通过活性氧（ROS）依赖途径破坏线粒体膜电位并诱导肿瘤细胞凋亡。
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