当前位置: X-MOL 学术Inorg. Chem. Commun. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design, Synthesis, characterization, DNA binding, acetyl and butyryl cholinesterase activities of metal chelates with 1,10-Phenanthroline derivative
Inorganic Chemistry Communications ( IF 3.8 ) Pub Date : 2020-12-01 , DOI: 10.1016/j.inoche.2020.108232
E.H. Edinsha Gladis , K. Nagashri , J. Joseph

Abstract Metal chelates comprised of highly conjugated planar 1,10-Phenanthroline derivative, [ML] where L is ligand (1,10-Phenanthroline derivative); M = Cu2+, Co2+, Ni2+ & Zn2+, were prepared. They were subjected to the composition measurement and different spectroscopic techniques for structural elucidation. Based on spectroscopic and analytical measurements confirmed that a distorted square planar arrangement for the Cu2+, Co2+, Ni2+ & Zn2+ chelates. The antimicrobial efficacy of prepared complexes were assessed against C. albicans, E. coli, B. subtilis, A. flavus, S. aureus, and A. niger. The anti-mycobacterial efficacy of ligand title chelates was evaluated against H37Rv and related to standard with the aid of MABA assay. The acetylcholinesterase (AChE) inhibitory effect of the ligand was examined to find out the beneficial efficiency of compound in the management of neurodegenerative syndromes. The synthesized ligand exhibited selective inhibition (AChE & BuChE), IC50 values of 0.20 and 3.20 µM as compared to standard, Rivastigmine and Galantamine. Further, the in vitro anti-inflammatory efficiency of metal chelates were performed with the help of egg albumin method. The α-glucosidase inhibition activity was also carried out for the prepared metal chelates. The inherent binding constants of metal chelates with DNA was calculated based molar extinction coefficient (Kb), 4.11, 3.62, 3.85 and 2.9 × 105 mol−1 for Cu2+, Co2+, Ni2+ & Zn2+ chelates, respectively, demonstrating that the metal chelates intensely bound to DNA. Studies of DNA cleavage were also conducted on pUC 18 DNA.

中文翻译:

1,10-菲咯啉衍生物金属螯合物的设计、合成、表征、DNA结合、乙酰和丁酰胆碱酯酶活性

摘要 金属螯合物由高度共轭的平面 1,10-菲咯啉衍生物 [ML] 组成,其中 L 是配体(1,10-菲咯啉衍生物);制备 M = Cu2+、Co2+、Ni2+ 和 Zn2+。他们接受了成分测量和不同的光谱技术以进行结构阐明。基于光谱和分析测量证实,Cu2+、Co2+、Ni2+ 和 Zn2+ 的扭曲方形平面排列螯合。对制备的复合物对白色念珠菌、大肠杆菌、枯草芽孢杆菌、黄曲霉、金黄色葡萄球菌和黑曲霉的抗菌功效进行了评估。配体标题螯合物的抗分枝杆菌功效针对 H37Rv 进行评估,并在 MABA 测定的帮助下与标准相关。检查了配体的乙酰胆碱酯酶 (AChE) 抑制作用,以发现化合物在治疗神经退行性综合征中的有益效果。合成的配体表现出选择性抑制(AChE 和 BuChE),与标准品、卡巴拉汀和加兰他敏相比,IC50 值为 0.20 和 3.20 µM。此外,金属螯合物的体外抗炎效率是在卵白蛋白方法的帮助下进行的。对制备的金属螯合物也进行了α-葡萄糖苷酶抑制活性。根据摩尔消光系数 (Kb) 计算金属螯合物与 DNA 的固有结合常数,Cu2+、Co2+、Ni2+ 和 Zn2+ 螯合物的摩尔消光系数分别为 4.11、3.62、3.85 和 2.9 × 105 mol-1,表明金属螯合物强烈结合到 DNA。
更新日期:2020-12-01
down
wechat
bug