Department of Medical and Clinical Biochemistry, P. J. Šafárik University in Košice, Trieda SNP 1, SK-04011 Košice, Slovakia.
Department of Ecology, University of Prešov, Ulica 17. novembra 1, SK-08116 Prešov, Slovakia.
J Inorg Biochem. 2020 Sep;210:111160. doi: 10.1016/j.jinorgbio.2020.111160. Epub 2020 Jun 25.
Two novel Co(II) fenamato complexes containing bathocuproine (bcp), namely [Co(bcp)(flu)] (1) and [Co(bcp)(nif)] (2) (flu = flufenamato, nif = niflumato) were synthesized and characterized by elemental analysis, single-crystal X-ray structure analysis as well as absorption and fluorescence spectroscopy. Investigation of their molecular structure revealed that both complexes are isostructural and form analogous complex molecules, with a Co(II) atom hexacoordinated by two nitrogen atoms of bcp and four oxygen atoms of two chelate bonded flu (1) and nif (2) ligands in a distorted octahedral arrangement. Surprisingly, the results of cytotoxicity experiments on four cancer cell lines (HeLa, HT-29, PC-3 and MCF-7) have revealed that despite similar structure of the complexes, the nif complex exhibits significantly higher activity, being the most effective against the PC-3 cell line (IC (MTT) = 6.11 ± 1.95 μM). Further studies performed on PC-3 cell line have shown that the mechanism of the cytotoxic action of nif complex (2) might involve activation of autophagic processes and apoptosis, while for its flu analogue (1) apoptosis was detected.
两种新型含双（邻-氨基苯甲酰肟）合钴（Ⅱ）配合物[Co(bcp)(flu)]（1）和[Co(bcp)(nif)]（2）（flu = 氟苯甲酰肟，nif = 尼氟灭酸）被合成并通过元素分析、单晶 X 射线结构分析以及吸收和荧光光谱进行了表征。对它们的分子结构的研究表明，这两种配合物是同构的，并形成类似的配合物分子，其中 Co(II)原子被 bcp 的两个氮原子和两个螯合键合的 flu（1）和 nif（2）配体的四个氧原子以扭曲的八面体排列方式六配位。令人惊讶的是，对四种癌细胞系（HeLa、HT-29、PC-3 和 MCF-7）进行的细胞毒性实验结果表明，尽管配合物的结构相似，但 nif 配合物表现出显著更高的活性，对 PC-3 细胞系的抑制作用最为有效（IC（MTT）= 6.11 ± 1.95 μM）。在 PC-3 细胞系上进行的进一步研究表明，nif 配合物（2）的细胞毒性作用机制可能涉及自噬过程和细胞凋亡的激活，而其 flu 类似物（1）则检测到细胞凋亡。
