Qi Jinxu, Liang Shichu, Gou Yi, Zhang Zhenlei, Zhou Zuping, Yang Feng, Liang Hong
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, Guilin, Guangxi, China; State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, Ministry of Science and Technology of China, Guanxi Normal University, Guilin, Guangxi, China.
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, Guilin, Guangxi, China.
Eur J Med Chem. 2015;96:360-8. doi: 10.1016/j.ejmech.2015.04.031. Epub 2015 Apr 14.
Copper (Cu) compounds are a promising candidate for next generation metal anticancer drugs and have been extensively studied. Therefore, four binuclear copper(II) compounds derived from Schiff base thiosemicarbazones (L1-L4), namely [CuCl(L1)]2 (C1), [CuNO3(L2)]2 (C2), [Cu(NCS) (L3)]2 (C3) and [Cu(CH3COO) (L4)]2 (C4) were synthesized and characterized. Four of these compounds showed very high cytotoxicity to cancer cell lines in vitro. These Cu(II) compounds strongly promoted the apoptosis of BEL-7404 cells. The formation of reactive oxygen species (ROS), change in mitochondrial membrane potential and western blot analysis revealed that Cu compounds could induce cancer cell apoptosis through the intrinsic ROS-mediated mitochondrial pathway accompanied by the regulation of Bcl-2 family proteins.
铜（Cu）化合物是下一代金属抗癌药物的一个有前景的候选物，并且已经得到了广泛研究。因此，合成并表征了四种源自席夫碱硫代氨基脲（L1-L4）的双核铜（II）化合物，即[CuCl(L1)]2（C1）、[CuNO3(L2)]2（C2）、[Cu(NCS)(L3)]2（C3）和[Cu(CH3COO)(L4)]2（C4）。这些化合物中的四种在体外对癌细胞系表现出非常高的细胞毒性。这些铜（II）化合物强烈促进了BEL-7404细胞的凋亡。活性氧（ROS）的形成、线粒体膜电位的变化以及蛋白质免疫印迹分析表明，铜化合物可通过内在的ROS介导的线粒体途径并伴随Bcl-2家族蛋白的调节来诱导癌细胞凋亡。
