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New heteroleptic lanthanide complexes as multimodal drugs: Cytotoxicity studies, apoptosis, cell cycle analysis, DNA interactions, and protein binding
Applied Organometallic Chemistry ( IF 3.7 ) Pub Date : 2020-10-18 , DOI: 10.1002/aoc.6062 Alexandra‐Cristina Munteanu 1 , Mihaela Georgiana Musat 2 , Mirela Mihaila 3 , Mihaela Badea 4 , Rodica Olar 4 , George Mihai Nitulescu 5 , Flavian Ștefan Rădulescu 6 , Lorelei Irina Brasoveanu 3 , Valentina Uivarosi 1
Applied Organometallic Chemistry ( IF 3.7 ) Pub Date : 2020-10-18 , DOI: 10.1002/aoc.6062 Alexandra‐Cristina Munteanu 1 , Mihaela Georgiana Musat 2 , Mirela Mihaila 3 , Mihaela Badea 4 , Rodica Olar 4 , George Mihai Nitulescu 5 , Flavian Ștefan Rădulescu 6 , Lorelei Irina Brasoveanu 3 , Valentina Uivarosi 1
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We report herein the synthesis and characterization of four new heteroleptic complexes of Sm(III), Eu(III), Gd(III), and Tb(III) with the natural flavonoid 5‐hydroxyflavone (primuletin) and 1,10‐phenanthroline. According to the physicochemical characterization, the mononuclear complexes correspond to the general formula [Ln(OH)2L1L2]·nH2O, where L1 = C15H9O3 (deprotonated 5‐hydroxyflavone) and L2 = C12H8N2 (1,10‐phenanthroline), Ln is the lanthanide cation, and n = 4 for Sm(III), 3.5 for Eu(III), 2 for Gd(III), and 3 for Tb(III). A six‐coordinated distorted octahedron geometry was proposed for the complexes, and density functional theory (DFT) studies were used to calculate their optimized geometry. Cytotoxicity was studied using MTS assay on cervical, colorectal, colon, breast, and ovarian adenocarcinoma cell lines. Flow cytometry data were consistent with apoptotic cell death and disruption of the cell cycle in cervical and colon cancer cells. As a means to investigate the mechanism underlying the cytotoxic effects, the abilities of the complexes to interact with calf thymus DNA, human serum albumin, and transferrin have also been assessed. According to experimental and computational studies, the four lanthanide complexes act as DNA intercalators and bind strongly to serum proteins.
中文翻译：
作为多峰药物的新型杂合镧系元素复合物：细胞毒性研究，细胞凋亡，细胞周期分析，DNA相互作用和蛋白质结合
我们在此报告了Sm（III），Eu（III），Gd（III）和Tb（III）与天然类黄酮5-羟基黄酮（primuletin）和1,10-菲咯啉的四种新的杂配物的合成和表征。根据理化特性，单核配合物对应于通式[Ln（OH）2 L 1 L 2 ]· n H 2 O，其中L 1 = C 15 H 9 O 3（去质子化的5-羟基黄酮）和L 2 = C 12 H 8 N 2（1,10-菲咯啉），Ln是镧系阳离子，n对于Sm（III）= 4，对于Eu（III）为3.5，对于Gd（III）为2，对于Tb（III）为3。为配合物提出了六坐标失真的八面体几何形状，并使用密度泛函理论（DFT）研究来计算其最佳几何形状。使用MTS分析法对宫颈，结肠直肠，结肠，乳腺癌和卵巢腺癌细胞系进行了细胞毒性研究。流式细胞仪数据与宫颈癌细胞和结肠癌细胞中的凋亡细胞死亡和细胞周期破坏一致。作为研究细胞毒性作用机理的手段，还评估了复合物与小牛胸腺DNA，人血清白蛋白和转铁蛋白相互作用的能力。根据实验和计算研究，四种镧系元素络合物可充当DNA嵌入剂，并与血清蛋白牢固结合。
更新日期：2020-12-22
中文翻译：
作为多峰药物的新型杂合镧系元素复合物：细胞毒性研究，细胞凋亡，细胞周期分析，DNA相互作用和蛋白质结合
我们在此报告了Sm（III），Eu（III），Gd（III）和Tb（III）与天然类黄酮5-羟基黄酮（primuletin）和1,10-菲咯啉的四种新的杂配物的合成和表征。根据理化特性，单核配合物对应于通式[Ln（OH）2 L 1 L 2 ]· n H 2 O，其中L 1 = C 15 H 9 O 3（去质子化的5-羟基黄酮）和L 2 = C 12 H 8 N 2（1,10-菲咯啉），Ln是镧系阳离子，n对于Sm（III）= 4，对于Eu（III）为3.5，对于Gd（III）为2，对于Tb（III）为3。为配合物提出了六坐标失真的八面体几何形状，并使用密度泛函理论（DFT）研究来计算其最佳几何形状。使用MTS分析法对宫颈，结肠直肠，结肠，乳腺癌和卵巢腺癌细胞系进行了细胞毒性研究。流式细胞仪数据与宫颈癌细胞和结肠癌细胞中的凋亡细胞死亡和细胞周期破坏一致。作为研究细胞毒性作用机理的手段，还评估了复合物与小牛胸腺DNA，人血清白蛋白和转铁蛋白相互作用的能力。根据实验和计算研究，四种镧系元素络合物可充当DNA嵌入剂，并与血清蛋白牢固结合。
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