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首页> 外文期刊>Nucleosides, nucleotides and nucleic acids >Synthesis, structural elucidation, DNA binding, cleavage, AChE and BuChE cholinesterase efficiencies of metal complexes with 1,10-phenanthroline scaffold
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Synthesis, structural elucidation, DNA binding, cleavage, AChE and BuChE cholinesterase efficiencies of metal complexes with 1,10-phenanthroline scaffold

机译:1,10-菲咯啉支架金属配合物的合成、结构解析、DNA结合、切割、AChE和BuChE胆碱酯酶效率

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A series of metal complexes containing a 1,10-phenanthroline scaffold ML (L-1,10-Phenanthroline derivative comprises conjugated aromatic core and electron withdrawing -NO2 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. S. aureus, A. niger, C. albicans, B.subtilis, A. flavus, and E. coli 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 (K-b = 4.11 x 10(5) M-1) is stronger than that of ethidium bromide (EB) to DNA (K-b = 3.3 x 10(5) M-1) and other metal complexes, respectively. The synthesized 1,10-phenanthroline derivative had the best inhibitory effects against acetylcholinesterase and butyrylcholinesterase, with IC50 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.
机译:含有1,10-菲咯啉支架[ML]的一系列金属配合物(L-1,10-菲咯啉衍生物包括共轭芳香族核心和吸电子-NO2基团);设计合成了M = Cu(II)、Zn(II)、Co(II)和Zn(II)离子,以获得有效的金属螯合物抗胆碱酯酶效率。通过分析和光谱研究确定结构特征。基于光谱数据,上述金属螯合物具有中等畸变的八面体结构。以金黄色葡萄球菌、黑曲霉、白色念珠菌、枯草芽孢杆菌、黄曲霉和大肠杆菌为研究对象,对合成的配体和金属配合物进行抑菌效果测试。使用琼脂糖凝胶电泳,在pUC 18 DNA上测试所制备的金属配合物的DNA片段化能力。铜(II)配合物对DNA的扭曲八面体几何形状(K-b = 4.11 x 10(5) M-1)分别强于溴化乙锭(EB)对DNA(K-b = 3.3 x 10(5) M-1)和其他金属配合物的变形。合成的1,10-菲咯啉衍生物对乙酰胆碱酯酶和丁酰胆碱酯酶的抑制效果最好,IC50值分别为0.45和3.6 M,均低于对照分子。我们的实验结果可能有助于开发新药物分子,特别是在治疗神经系统疾病方面,包括青光眼、阿尔茨海默病和糖尿病。抑制剂对糖苷酶的作用有助于延缓糖分子分解和释放到血液中,可作为治疗糖尿病的治疗因子。

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