Chair and Department of Biochemistry, Medical University of Warsaw, 02-097 Warszawa, Poland.
Laboratory of X-ray and Electron Microscopy Research, Institute of Physics, Polish Academy of Sciences, 02-668 Warszawa, Poland.
Int J Mol Sci. 2021 Oct 22;22(21):11415. doi: 10.3390/ijms222111415.
A series of eight copper (II) complexes with 3-(4-chloro-3-nitrophenyl)thiourea were designed and synthesized. The cytotoxic activity of all compounds was assessed in three human cancer cell lines (SW480, SW620, PC3) and human normal keratinocytes (HaCaT). The complexes , , , and were cytotoxic to the studied tumor cells in the low micromolar range, without affecting the normal cells. The complexes , , and induced lactate dehydrogenase (LDH) release in all cancer cell lines, but not in the HaCaT cells. They provoked early apoptosis in pathological cells, especially in SW480 and PC3 cells. The ability of compounds , , and to diminish interleukin-6 (IL-6) concentration in a cell was established. For the first time, the influence of the most promising Cu (II) complexes on intensities of detoxifying and reactive oxygen species (ROS) scavenging the enzymes of tumor cells was studied. The cytotoxic effect of all copper (II) conjugates against standard and hospital bacterial strains was also proved.
设计并合成了一系列八个铜（II）配合物与 3-（4-氯-3-硝基苯基）硫脲。所有化合物的细胞毒性活性在三种人癌细胞系（SW480、SW620、PC3）和人正常角质形成细胞（HaCaT）中进行了评估。配合物 、 、 、 对研究的肿瘤细胞具有低微摩尔范围内的细胞毒性，而对正常细胞没有影响。配合物 、 、 诱导所有癌细胞系中乳酸脱氢酶（LDH）的释放，但在 HaCaT 细胞中没有。它们在病态细胞中诱导早期细胞凋亡，特别是在 SW480 和 PC3 细胞中。还确定了化合物 、 、 降低细胞内白细胞介素-6（IL-6）浓度的能力。首次研究了最有前途的 Cu（II）配合物对肿瘤细胞解毒和活性氧（ROS）清除酶强度的影响。还证明了所有铜（II）缀合物对标准和医院细菌菌株的细胞毒性作用。
