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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
【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.
- 【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