Faculty of Chemistry, University of Wrocław, ul. F. Joliot-Curie 14, 50-383 Wrocław, Poland.
Department of Analytical Chemistry, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211 A, 50-566 Wrocław, Poland.
Molecules. 2020 Feb 8;25(3):741. doi: 10.3390/molecules25030741.
A series of water-soluble copper(II) complexes based on 2,9-dimethyl-1,10-phenanthroline (dmphen) and mixed-ligands, containing PTA=O (1,3,5-triaza-7-phosphaadamantane-7-oxide) have been synthesized and fully characterized. Two types of complexes have been obtained, monocationic [Cu(NO)(O-PTA=O)(dmphen)][PF] (), [Cu(Cl)(dmphen)][PF] (), and neutral [Cu(NO)(dmphen)] (). The solid-state structures of all complexes have been determined by single-crystal X-ray diffraction. Magnetic studies for the complex - indicated a very weak antiferromagnetic interaction between copper(II) ions in crystal lattice. Complexes were successfully evaluated for their cytotoxic activities on the normal human dermal fibroblast (NHDF) cell line and the antitumor activity using the human lung carcinoma (A549), epithelioid cervix carcinoma (HeLa), colon (LoVo), and breast adenocarcinoma (MCF-7) cell lines. Complexes and revealed lower toxicity to NHDF than A549 and HeLa cells, meanwhile compound appeared to be more toxic to NHDF cell line in comparison to all cancer lines. Additionally, interactions between the complexes and human apo-transferrin (apo-Tf) using fluorescence and circular dichroism (CD) spectroscopy were also investigated. All compounds interacted with apo-transferrin, causing same changes of the protein conformation. Electrostatic interactions dominate in the / - apo- Tf systems and hydrophobic and ionic interactions in the case of .
一系列基于 2,9-二甲基-1,10-菲啰啉(dmphen)和混合配体的水溶性铜(II)配合物,含有 PTA=O(1,3,5-三氮杂-7-磷杂金刚烷-7-氧化物)已被合成并进行了全面的表征。得到了两种类型的配合物,分别是阳离子[Cu(NO)(O-PTA=O)(dmphen)]PF_6、[Cu(Cl)(dmphen)]PF_6和中性[Cu(NO)(dmphen)][3]。所有配合物的晶体结构均通过单晶 X 射线衍射确定。对配合物的磁性研究表明,晶格中铜(II)离子之间存在非常微弱的反铁磁相互作用。成功评估了这些配合物对正常人类真皮成纤维细胞(NHDF)细胞系的细胞毒性和对人肺癌(A549)、上皮样宫颈癌细胞(HeLa)、结肠(LoVo)和乳腺腺癌(MCF-7)细胞系的抗肿瘤活性。配合物[1]和[2]对 NHDF 的毒性比 A549 和 HeLa 细胞低,而配合物[3]对 NHDF 细胞系的毒性似乎比所有癌细胞系都高。此外,还使用荧光和圆二色性(CD)光谱研究了配合物与人类脱铁蛋白(apo-Tf)之间的相互作用。所有化合物都与 apo-转铁蛋白相互作用,导致蛋白质构象发生相同的变化。静电相互作用在/ - apo-Tf 体系中起主导作用,而在的情况下则是疏水和离子相互作用。