新型2,2′-联吡啶衍生物金属配合物的合成、结构解析、DNA结合、裂解及胆碱酯酶抑制活性研究。

IF 1.3 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Ebenezer Bonpandi, Caroline John, Pechiammal Arumugam
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引用次数: 0

摘要

为了获得有效的抑制胆碱酯酶活性,开发了具有2,2'-联吡啶基框架[M-L]的Cu(II)、Ni(II)、Co(II)和Zn(II)的金属(II)配合物(L = 2,2'-联吡啶基衍生物,含有芳香族中心和一个吸e -NO2基团)。通过光谱和分析研究确定了其结构特征。评价了所制备的配体和金属(II)配合物对细菌和真菌的抑菌活性。用琼脂糖凝胶电泳研究了合成的金属(II)配合物在puc18 DNA上的DNA片段化能力。铜(II)配合物(Kb=4.11 × 105 M-1)对DNA的结合亲和力高于溴化乙啶(EB) (Kb=3.3 × 105 M-1)和金属(II)配合物。化学合成的2,2′-联吡啶衍生物对乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BuChE)的抑制作用最强,IC50值分别小于标准化合物(0.34µM和3.42µM)。我们的研究结果可以帮助创造新的药物分子,特别是治疗神经系统疾病,如阿尔茨海默病和由糖尿病引起的神经系统疾病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, structural elucidation, DNA binding, cleavage, cholinesterase inhibitory activity of metal complexes of novel 2,2'-bipyridyl derivative.

To achieve efficient cholinesterase inhibitory activity of metal(II) complexes of Cu(II), Ni(II), Co(II), and Zn(II) with 2,2'-bipyridyl framework [M-L] (L = 2,2'-bipyridyl derivative containing an aromatic center and an e--withdrawing -NO2 group) was developed. The structural characteristics were identified through spectroscopic and analytical studies. The antibacterial activity of the produced ligand and metal(II) complexes against bacteria and fungi was evaluated. The synthesized metal(II) complexes ability to fragment DNA has been studied on pUC 18 DNA using agarose gel electrophoresis. The copper(II) complex (Kb=4.11 × 105 M-1) is stronger binding affinity for DNA than ethidium bromide (EB) (Kb=3.3 × 105 M-1) and metal(II) complexes. The chemically produced 2,2'-bipyridyl derivative had the strongest inhibitory effects against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values that were less than the standard compounds (0.34 and 3.42 µM, respectively). Our research results could aid in the creation of novel drug molecules, especially for the treatment of neurological conditions like Alzheimer's disease and neurological disorders occurring through diabetes.

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来源期刊
Nucleosides, Nucleotides & Nucleic Acids
Nucleosides, Nucleotides & Nucleic Acids 生物-生化与分子生物学
CiteScore
2.60
自引率
7.70%
发文量
91
审稿时长
6 months
期刊介绍: Nucleosides, Nucleotides & Nucleic Acids publishes research articles, short notices, and concise, critical reviews of related topics that focus on the chemistry and biology of nucleosides, nucleotides, and nucleic acids. Complete with experimental details, this all-inclusive journal emphasizes the synthesis, biological activities, new and improved synthetic methods, and significant observations related to new compounds.
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