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Antiproliferative Activities of Diimine-Based Mixed Ligand Copper(II) Complexes.
ACS Combinatorial Science Pub Date : 2020-01-08 , DOI: 10.1021/acscombsci.9b00202 Nazanin Kordestani 1 , Hadi Amiri Rudbari 1 , Alexandra R Fernandes 2 , Luís R Raposo 2 , Pedro V Baptista 2 , Daniela Ferreira 2 , Giuseppe Bruno 3 , Giovanni Bella 3 , Rosario Scopelliti 4 , Jason D Braun 5 , David E Herbert 5 , Olivier Blacque 6
ACS Combinatorial Science Pub Date : 2020-01-08 , DOI: 10.1021/acscombsci.9b00202 Nazanin Kordestani 1 , Hadi Amiri Rudbari 1 , Alexandra R Fernandes 2 , Luís R Raposo 2 , Pedro V Baptista 2 , Daniela Ferreira 2 , Giuseppe Bruno 3 , Giovanni Bella 3 , Rosario Scopelliti 4 , Jason D Braun 5 , David E Herbert 5 , Olivier Blacque 6
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A series of Cu(diimine)(X-sal)(NO3) complexes, where the diimine is either 2,2'-bipyridine (bpy) or 1,10-phenanthroline (phen) and X-sal is a monoanionic halogenated salicylaldehyde (X = Cl, Br, I, or H), have been synthesized and characterized by elemental analysis and X-ray crystallography. Penta-coordinate geometries copper(II) were observed for all cases. The influence of the diimine coligands and different halogen atoms on the antiproliferative activities toward human cancer cell lines have been investigated. All Cu(II) complexes were able to induce a loss of A2780 ovarian carcinoma cell viability, with phen derivatives more active than bpy derivatives. In contrast, no in vitro antiproliferative effects were observed against the HCT116 colorectal cancer cell line. These cytotoxicity differences were not due to a different intracellular concentration of the complexes determined by inductively coupled plasma atomic emission spectroscopy. A small effect of different halogen substituents on the phenolic ring was observed, with X = Cl being the most highly active toward A2780 cells among the phen derivatives, while X = Br presented the lowest IC50 in A2780 cells for bpy analogs. Importantly, no reduction in normal primary fibroblasts cell viability was observed in the presence of bpy derivatives (IC50 > 40 μM). Mechanistically, complex 1 seems to induce a stronger apoptotic response with a higher increase in mitochondrial membrane depolarization and an increased level of intracellular reactive oxygen species (ROS) compared to complex 3. Together, these data and the low IC50 compared to cisplatin in A2780 ovarian carcinoma cell line demonstrate the potential of these bpy derivatives for further in vivo studies.
中文翻译：
基于二亚胺的混合配体铜 (II) 配合物的抗增殖活性。
一系列 Cu(diimine)(X-sal)(NO3) 络合物，其中二亚胺是 2,2'-联吡啶 (bpy) 或 1,10-菲咯啉 (phen)，X-sal 是单阴离子卤化水杨醛 ( X = Cl、Br、I 或 H)，已通过元素分析和 X 射线晶体学合成和表征。在所有情况下都观察到五坐标几何形状的铜 (II)。已经研究了二亚胺聚配体和不同卤素原子对人类癌细胞系抗增殖活性的影响。所有 Cu(II) 复合物都能够诱导 A2780 卵巢癌细胞活力的丧失，其中 phen 衍生物比 bpy 衍生物更具活性。相反，没有观察到对 HCT116 结肠直肠癌细胞系的体外抗增殖作用。这些细胞毒性差异不是由于通过电感耦合等离子体原子发射光谱法确定的复合物的不同细胞内浓度。观察到不同卤素取代基对酚环的小影响，在苯酚衍生物中，X = Cl 对 A2780 细胞的活性最高，而 X = Br 在 A2780 细胞中对 bpy 类似物的 IC50 最低。重要的是，在 bpy 衍生物（IC50 > 40 μM）的存在下，没有观察到正常原代成纤维细胞活力的降低。从机制上讲，与复合物 3 相比，复合物 1 似乎诱导更强的凋亡反应，线粒体膜去极化增加更多，细胞内活性氧 (ROS) 水平增加。
更新日期：2020-01-23
中文翻译：
基于二亚胺的混合配体铜 (II) 配合物的抗增殖活性。
一系列 Cu(diimine)(X-sal)(NO3) 络合物，其中二亚胺是 2,2'-联吡啶 (bpy) 或 1,10-菲咯啉 (phen)，X-sal 是单阴离子卤化水杨醛 ( X = Cl、Br、I 或 H)，已通过元素分析和 X 射线晶体学合成和表征。在所有情况下都观察到五坐标几何形状的铜 (II)。已经研究了二亚胺聚配体和不同卤素原子对人类癌细胞系抗增殖活性的影响。所有 Cu(II) 复合物都能够诱导 A2780 卵巢癌细胞活力的丧失，其中 phen 衍生物比 bpy 衍生物更具活性。相反，没有观察到对 HCT116 结肠直肠癌细胞系的体外抗增殖作用。这些细胞毒性差异不是由于通过电感耦合等离子体原子发射光谱法确定的复合物的不同细胞内浓度。观察到不同卤素取代基对酚环的小影响，在苯酚衍生物中，X = Cl 对 A2780 细胞的活性最高，而 X = Br 在 A2780 细胞中对 bpy 类似物的 IC50 最低。重要的是，在 bpy 衍生物（IC50 > 40 μM）的存在下，没有观察到正常原代成纤维细胞活力的降低。从机制上讲，与复合物 3 相比，复合物 1 似乎诱导更强的凋亡反应，线粒体膜去极化增加更多，细胞内活性氧 (ROS) 水平增加。
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