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Synthesis, spectroscopic, thermal analysis and in vitro cytotoxicity, anticholinesterase and antioxidant activities of new Co(II), Ni(II), Cu(II), Zn(II), and Ru(III) complexes of pyrazolone-based Schiff base ligand
Journal of Molecular Structure ( IF 4.0 ) Pub Date : 2023-07-16 , DOI: 10.1016/j.molstruc.2023.136225
Reşit Çakmak , Burak Ay , Ercan Çınar , Eyüp Başaran , Senem Akkoç , Mehmet Boğa , Eşref Taş

Metal-based drugs have gained significant importance in medicine in recent years. In this research, a series of new Co(II), Ni (II), Cu (II), Zn(II), and Ru(III) complexes of a Schiff base ligand, (1,5-dimethyl-4-((1-(3-nitrophenyl)ethylidene) amino)-2-phenyl-1,2-dihydro-3H-pyrazol-3-one), were prepared for the first time in excellent yields, and characterized by elemental analysis, FT-IR, 1H-NMR, 13C NMR, ICP-OES, and thermal analysis. The in vitro antiproliferative, anticholinesterase, and antioxidant properties of complexes 1-5 were evaluated. The cytotoxic effects of complexes 1-5 on the viability of colon cancer (DLD-1), breast cancer (MDA-MB-231), and healthy lung (Wl-38) cell lines were investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method in vitro. The anticancer activities of the ligand and its metal complexes were lower than those of the reference drug, cisplatin. In anticholinesterase activity studies, complex 4 (88.46±0.45% inhibition) in butyrylcholinesterase (BChE) assay showed a higher inhibitory effect than the standard compound galanthamine with 78.14±0.55 % inhibition. In antioxidant assays, some complexes showed higher antioxidant activities than standard antioxidant butylated hydroxytoluene (BHT). Among the prepared complexes, complex (4) (IC50=5.91±0.17 µM) in ABTS assay showed the highest antioxidant activity compared to BHT (IC50=16.19±0.17 µM). Also, this complex (IC50=10.17±0.36 µM) showed the best antioxidant activity in CUPRAC assay compared to BHT (IC50=39.37±0.12 µM).



中文翻译:

吡唑啉酮基希夫碱配体新型 Co(II)、Ni(II)、Cu(II)、Zn(II) 和 Ru(III) 配合物的合成、光谱、热分析以及体外细胞毒性、抗胆碱酯酶和抗氧化活性

近年来,金属药物在医学领域变得非常重要。在本研究中,席夫碱配体(1,5-二甲基-4-(首次以优异的收率制备了(1-(3-硝基苯基)亚乙基)氨基)-2-苯基-1,2-二氢-3H-吡唑-3-酮),并通过元素分析、FT进行了表征-IR、1 H-NMR、13 C NMR、ICP-OES 和热分析。评估了复合物1-5的体外抗增殖、抗胆碱酯酶和抗氧化特性。配合物1-5的细胞毒性作用使用 3-(4,5-二甲基噻唑-2-基)- 研究了结肠癌 (DLD-1)、乳腺癌 (MDA-MB-231) 和健康肺 (Wl-38) 细胞系活力的影响体外2,5-二苯基溴化四唑(MTT)法。该配体及其金属配合物的抗癌活性低于对照药顺铂。在抗胆碱酯酶活性研究中,丁酰胆碱酯酶(BChE)测定中的复合物4 (88.46±0.45%抑制)显示出比标准化合物加兰他敏(78.14±0.55%抑制)更高的抑制效果。在抗氧化剂测定中,一些复合物表现出比标准抗氧化剂丁基羟基甲苯 (BHT) 更高的抗氧化活性。在所制备的配合物中,配合物( 4 )(IC 50ABTS 测定中 =5.91±0.17 µM)与 BHT 相比显示出最高的抗氧化活性(IC 50 =16.19±0.17 µM)。此外,与 BHT (IC 50 =39.37±0.12 µM) 相比,该复合物(IC 50 =10.17±0.36 µM)在 CUPRAC 测定中显示出最佳的抗氧化活性。

更新日期:2023-07-16
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