| 陈锦灿,蔡先洪,彭发,等.基于β-咔啉的环金属化Ru(II)配合物诱导HeLa细胞凋亡及抗氧化活性研究[J].中国海洋药物,2022,41(6):31-40. |
| 基于β-咔啉的环金属化Ru(II)配合物诱导HeLa细胞凋亡及抗氧化活性研究 |
| The apoptosis-inducing properties and antioxidant activity of cyclometalated Ru(II)-β-carboline complexes |
| 投稿时间：2021-10-25 修订日期：2021-12-09 |
| DOI：10.13400/j.cnki.cjmd.2022.06.009 |
| 中文关键词: β-咔啉生物碱 环金属化Ru(II)配合物 细胞凋亡 细胞毒性 抗氧化活性 |
| English Keywords:β carboline alkaloid cyclometalated Ru(II) complexes apoptosis cytotoxicity antioxidant activity |
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| 摘要点击次数: 2002 |
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| 中文摘要: |
| 目的探究新型环金属化Ru(II)-β-咔啉配合物[Ru(dmb)2(NO2-Ph-βC)](PF6)(NO2-Ph-βC=NO2-phenyl-9H-pyrido[3,4-b]indole;RuβC-5)和[Ru(bpy)2(NO2-Ph-βC)](PF6) (RuβC-6) 诱导HeLa细胞凋亡的机理。方法 通过元素分析、ES-MS、1H NMR对配合物进行表征；采用电感耦合等离子体质谱仪(ICP-MS)测定配合物的油水分配系数logP；细胞毒性实验检测RuβC-5和RuβC-6对 A549、HeLa、NCI-H460、HepG-2和MCF-7细胞的毒性作用；Hoechst 33342、AO/EB、Annexin V-FITC/PI染色法检测配合物诱导HeLa细胞凋亡；流式细胞术分析配合物对HeLa细胞凋亡、细胞周期阻滞、线粒体膜电位(MMP)、活性氧(ROS)的影响,蛋白免疫印迹实验(Western blot)检测Caspase信号通路及线粒体凋亡通路相关蛋白的影响。结果 配合物RuβC-5、RuβC-6对HeLa细胞表现出相对较高的细胞毒性和较好的选择性,能诱导HeLa细胞的G0/G1期阻滞和凋亡,降低MMP,抑制细胞内ROS的产生。结论 新型Ru(II)-β-咔啉配合物可诱导HeLa细胞凋亡；此外,RuβC-5具有抗氧化活性,可以通过清除细胞内ROS的含量诱导HeLa细胞凋亡。 |
| English Summary: |
| Objective To investigate the mechanism of HeLa cell apoptosis-inducing by two cyclometalated Ru(II)-β -carboline complexes[Ru(dmb)2(NO2-Ph-βC)](PF6)(NO2-Ph-βC=NO2-phenyl-9H-pyrido[3,4-b]indole (RuβC-5) and [Ru(bpy)2(NO2-Ph-βC)](PF6) (RuβC-6). Methods The complexes were characterized by elemental analysis, ES-MS, 1H NMR and UV-Vis spectra.The oil-water partition coefficient of complexes were measured by using inductively coupled plasma mass spectrometry (ICP-MS). The cytotoxicity of RuβC-5 and RuβC-6 were assessed against A549, HeLa, NCI-H460, HepG-2 and MCF-7 cells. Their effects on apoptosis, cell cycle, mitochondrial membrane potential (MMP) and reactive oxygen species generation (ROS) of A549 were determined using flow cytometry.Western blot assay was used to detect the impact of Caspase signaling pathway and mitochondrial apoptosis pathway related proteins. Results The complexes RuβC-5 and RuβC-6 exhibited much higher cytotoxicity and good selectivity to normal cells, which can induce G0/ G1 phase arrest and apoptosis, decrease MMP and inhibit the production of intracellular ROS. Conclusion The new Ru(II)-β -carboline complexes can induce HeLa cells apoptosis. Furthermore, as an antioxidant, RuβC-5 tended to induce apoptosis in HeLa cells by scavenging intracellular ROS. |
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