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1,10-菲啰啉骨架金属配合物的合成、结构解析、DNA 结合、切割、AChE 和 BuChE 胆碱酯酶活性。

Synthesis, structural elucidation, DNA binding, cleavage, AChE and BuChE cholinesterase efficiencies of metal complexes with 1,10-phenanthroline scaffold.

机构信息

Department of Chemistry, Manonmaniam Sundaranar University, Tirunelveli, Tamil Nadu, India.

Department of Chemistry, Noorul Islam Centre for Higher Education, Kumaracoil, Tamil Nadu, India.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2022;41(3):285-313. doi: 10.1080/15257770.2021.2011915. Epub 2022 Jan 26.

DOI:10.1080/15257770.2021.2011915
PMID:35080488
Abstract

A series of metal complexes containing a 1,10-phenanthroline scaffold [ML] (L-1,10-Phenanthroline derivative comprises conjugated aromatic core and electron withdrawing -NO group); M = Cu(II), Zn(II), Co(II), and Zn(II) ions were designed and synthesized to obtain effective anti-cholinesterase efficiencies of metal chelates. Analytical and spectroscopic studies were used to determine the structural features. An octahedral structure with moderate distortion was attributed to the above metal chelates based on spectroscopic data. were used to test the antibacterial efficacy of the synthesized ligands and metal complexes. Using agarose gel electrophoresis, the DNA fragmentation proficiency of prepared metal complexes was tested on pUC 18 DNA. The distorted octahedral geometry of the copper(II) complex to DNA ( = 4.11 × 10 M) is stronger than that of ethidium bromide (EB) to DNA ( = 3.3 × 10 M) and other metal complexes, respectively. The synthesized 1,10-phenanthroline derivative had the best inhibitory effects against acetylcholinesterase and butyrylcholinesterase, with IC values of 0.45 and 3.6 M, respectively, which were lower than the reference molecules. Our experimental results may contribute to the development of new drug molecules particularly in the treatment of neurological disorders including glaucoma, Alzheimer's disease and diabetes. The actions of inhibitors on the glycosidase enzyme help to delay the breakdown and release of sugar molecules into the bloodstream, and they can be used as therapeutic factors in the treatment of diabetes.

摘要

一系列含有 1,10-菲啰啉骨架[ML]的金属配合物(L-1,10-菲啰啉衍生物包含共轭芳香核和吸电子-NO 基团);M = Cu(II)、Zn(II)、Co(II) 和 Zn(II)离子被设计和合成,以获得金属配合物有效的抗胆碱酯酶效率。分析和光谱研究用于确定结构特征。基于光谱数据,将上述金属配合物归因于具有中等扭曲的八面体结构。合成的配体和金属配合物用于测试其抗菌功效。使用琼脂糖凝胶电泳,在 pUC 18 DNA 上测试了制备的金属配合物对 DNA 的片段化能力。铜(II)配合物与 DNA 的扭曲八面体几何形状( = 4.11 × 10 M)强于溴化乙锭(EB)与 DNA( = 3.3 × 10 M)和其他金属配合物,分别。合成的 1,10-菲啰啉衍生物对乙酰胆碱酯酶和丁酰胆碱酯酶具有最佳的抑制作用,IC 值分别为 0.45 和 3.6 M,均低于参考分子。我们的实验结果可能有助于开发新的药物分子,特别是在治疗包括青光眼、阿尔茨海默病和糖尿病在内的神经紊乱方面。抑制剂对糖苷酶的作用有助于延缓糖分子在血液中的分解和释放,并且可以作为治疗糖尿病的治疗因素。

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