Department of Physiology (Neuroimmunophysiology and Chrononutrition Research Group), Faculty of Science, University of Extremadura, 06006, Badajoz, Spain.
Departament of Organic and Inorganic Chemistry (Chemistry of Coordination Research Group), Faculty of Science, University of Extremadura, Badajoz, Spain.
Sci Rep. 2020 Oct 7;10(1):16745. doi: 10.1038/s41598-020-73488-0.
Cisplatin is one of the most widely used chemotherapeutic agents in the treatment of different tumors but has high toxicity and side effects. Therefore, the synthesis of new chemotherapeutic agents is necessary, so that they are effective in the treatment of cancer while avoiding such toxicity. In this study, we have synthesized and characterized a palladium(II) complex, [PdCl(µ-PyTT)]Cl·4HO (PdPyTT), with 2-(2-pyridyl)imine-N-(2-thiazolin-2-yl)thiazolidine (PyTT) as a ligand; besides, its cytotoxicity and pro-apoptotic capacity was tested in human promyelocytic leukemia HL-60 cell line. Similar to cisplatin, PdPyTT produced a time- and dose-dependent decrease in cell viability. Additionally, the palladium complex increased both the proportion of cells with apoptotic morphology and the activation of caspase-3 and -9. PdPyTT, like cisplatin, also increased intracellular ROS production and DNA oxidative damage. Therefore, our findings demonstrated the promising application of palladium(II) complexes as novel anti-leukemic agents.
顺铂是治疗不同肿瘤的最广泛使用的化疗药物之一，但具有高毒性和副作用。因此，有必要合成新的化疗药物，使它们在治疗癌症的同时避免这种毒性。在这项研究中，我们合成并表征了一种钯 (II) 配合物 [PdCl(µ-PyTT)]Cl·4HO（PdPyTT），其配体为 2-(2-吡啶基)亚胺-N-(2-噻唑啉-2-基)噻唑烷（PyTT）；此外，还在人早幼粒细胞白血病 HL-60 细胞系中测试了其细胞毒性和促凋亡能力。与顺铂相似，PdPyTT 产生了时间和剂量依赖性的细胞活力下降。此外，钯配合物增加了具有凋亡形态的细胞比例以及 caspase-3 和 -9 的激活。与顺铂一样，PdPyTT 还增加了细胞内 ROS 的产生和 DNA 的氧化损伤。因此，我们的研究结果表明，钯 (II) 配合物作为新型抗白血病药物具有广阔的应用前景。
