The aim of our study was to evaluate the in vitro and in vivo anti-proliferative potential of complex (2) [Cu (L1)Cl]Cl.2H₂O, where L1 = 1-[2-hydroxybenzyl(2-pyridylmethyl)amino]-3-(1-naphthyloxy)-2-propanol on lung carcinoma cell NCI-H460. Cell viability assay determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) colorimetric assay demonstrated that the complex (2) exhibits higher activity against the NCI-H460 cell, with an IC₅₀ value lower than cisplatin (26.5 μM ± 1.1 and 203 ± 1.2 μM respectively). Cell death by apoptosis was investigated by flow cytometer analysis of sub-G1 populations in the cell cycle and Annexin V/Propidium Iodide assay. Changes on the cell surface and ultrastructure were detected by scanning and transmission electron microscopy. Our work revealed that complex (2) induced changes associated with apoptosis, such as plasma membrane blebbing and a lower microvilli amount, fragmentation and condensation of chromatin, alterations in mitochondria, and enlargement of the endoplasmic reticulum. Mitochondrial function of NCI-H460 cells evaluated by 5,5′,6,6′-tetrachloro 1,1′,3,3′ tetraethylbenzimidazolylcarbocyanine iodide (JC-1) probes showed high loss of mitochondrial membrane potential when treated with complex (2). Moreover, caspase-12 measurement showed an expressive activation level, which is related to endoplasmic reticulum stress. In vivo assay using the murine model of human lung cancer cell showed that complex (2) and cisplatin has similar antineoplastic activity.

我们研究的目的是评估复合物（2）[Cu（L1）Cl] Cl.2H ₂ O的体外和体内抗增殖潜力，其中L1 = 1- [2-羟基苄基（2-吡啶基甲基）氨基] -3-（1-萘氧基）-2-丙醇对肺癌细胞NCI-H460的影响。用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四氮唑（MTT）比色法测定的细胞活力测定表明，复合物（2）对NCI-H460细胞表现出更高的活性， IC ₅₀该值低于顺铂（分别为26.5μM±1.1和203±1.2μM）。通过流式细胞仪分析亚G1群体在细胞周期中的凋亡和膜联蛋白V /碘化丙啶检测细胞凋亡所致的细胞死亡。通过扫描和透射电子显微镜检测细胞表面和超微结构的变化。我们的工作表明，复合物（2）诱导了与凋亡相关的变化，例如质膜起泡微绒毛数量少，染色质破碎和凝集，线粒体改变以及内质网扩大。5,5'，6,6'-四氯1,1'，3,3'四乙基苯并咪唑基碳菁碘化物（JC-1）探针评估的NCI-H460细胞的线粒体功能显示，当用复合物处理时，线粒体膜电位有很大损失（2 ）。此外，caspase-12测定显示了表达激活水平，这与内质网应激有关。使用人肺癌细胞的鼠模型进行的体内分析表明，复合物（2）和顺铂具有相似的抗肿瘤活性。