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水杨醛氨基硫脲双核铜配合物的合成、抗肿瘤活性及其机制研究(英文)

Synthesis of binuclear copper (Ⅱ) complex with salicylaldehyde thiosemicarbazone: structure,anticancer properties and anticancer mechanism

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【作者】 江名苟峄齐金旭张展周祖平梁士楚杨峰

【Author】 JIANG Ming;GOU Yi;QI Jin-xu;ZHANG Zhan;ZHOU Zu-ping;LIANG Shi-chu;YANG Feng;Key Laboratory of Ecology of Rare an Endangered Species and Environmental Protection,Ministry of Education of the People ’s Republic of China,Guangxi Normal University;State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources,Ministry of Science and Technology of China,Guanxi Normal University;

【机构】 广西师范大学珍稀濒危动植物生态与环境保护省部共建教育部重点实验室广西师范大学药用资源化学与药物分子工程国家重点实验室培育基地

【摘要】 目的合成铜类抗肿瘤金属药物并探讨其作用机制。方法合成了水杨醛氨基硫脲双核铜配合物[(CuⅡ)2(L)2(H2O)(MeOH)](NO3-)——2,利用X-ray单晶衍射、元素分析和红外光谱确证其结构。结果与结论该配合物对人肝癌细胞株BEL-7704具有很强的抑制活性,并且能使细胞周期停滞在S期。谷胱甘肽、活性氧、线粒体膜电位和蛋白质印迹实验结果显示该化合物是通过ROS介导的线粒体通路诱导癌细胞凋亡,同时伴随着Bcl-2家族蛋白的表达量的变化。

【Abstract】 One binuclear copper[Cu(Ⅱ)]complex of the Schiff base ligand(salicylaldehyde thiosemicarbazone,HL),namely[(CuⅡ)2(L)2(H2O)(MeOH)](NO3-2,was synthesized and well characterized by single crystal X-ray diffraction,elemental analysis and infrared(IR)spectroscopic analysis.The Cu(Ⅱ)complex strongly promoted the apoptosis of BEL-7404 cells and had a capacity to arrest the cell cycle at S phase of the cells.Furthermore,glutathione/oxidized glutathione(GSH/GSSG)assay,reactive oxygen species(ROS),mitochondrial membrane potential and western blot analyses revealed that the Cu(Ⅱ)complex exerts its cytotoxicity through an ROS-mediated intrinsic mitochondrial pathway accompanied by the regulation of Bcl-2 family proteins.

【基金】 National Natural Science Foundation of China(31460232)
  • 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2017年01期
  • 【分类号】R914.5;R96
  • 【被引频次】1
  • 【下载频次】298
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