| 管惠峰,谭小芳,宫 平,吴百川,侯丽娜,李 娟.多靶点抗AD bis-MEP-乙二酰胺杂合物ZLA抑制神经元型AChE活性及促智作用研究[J].现代生物医学进展英文版,2020,(7):1206-1210. |
| 多靶点抗AD bis-MEP-乙二酰胺杂合物ZLA抑制神经元型AChE活性及促智作用研究 |
| A Multifunctional Bis-MEP-oxadiamide Hybrid Inhibits Neuronal AChE Activity and Improves Cognitive Deficits Caused by Central Cholinergic Dysfunction |
| Received:October 31, 2019 Revised:November 27, 2019 |
| DOI：10.13241/j.cnki.pmb.2020.07.002 |
| 中文关键词: 阿尔茨海默病（AD） 多靶点抗AD 药物 AChE抑制 认知改善 |
| 英文关键词: Alzheimer's disease Multi-target directed ligand AChE inhibition Cognitive amelioration |
| 基金项目:国家自然科学基金项目（81503044，81373417，30973538） |
| Author Name | Affiliation | E-mail | | GUAN Hui-feng | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | 2468118848@qq.com | | TAN Xiao-fang | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | | | GONG Ping | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | | | WU Bai-chuan | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | | | HOU Li-na | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | | | LI Juan | Department of Pharmacology, Shanghai Jiaotong University School of Medicine, Shanghai, 200025, China | |
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| 中文摘要: |
| 摘要 目的：探究ZLA对神经元型AChE的抑制活性及其对中枢胆碱能神经功能障碍导致的学习记忆功能减退的改善作用。方法：通过体外实验观察ZLA对神经元型AChE活性的影响；通过ex vivo实验观察ZLA体内AChE抑制活性；利用Morris水迷宫行为学实验探讨ZLA对东莨菪碱诱发的小鼠学习记忆功能障碍的改善作用。结果：ZLA明显抑制人SH-SY5Y神经元细胞和小鼠海马神经元来源的AChE活性。另外，ZLA腹腔注射后以剂量依赖性方式抑制小鼠脑内AChE活性。 Morris水迷宫实验结果显示，ZLA显著改善东莨菪碱引起的学习和记忆功能障碍。结论：ZLA能够抑制神经元型AChE活性并具有促智作用。 |
| 英文摘要: |
| ABSTRACT Objective: The purpose of this study was to observe the inhibition activity of ZLA on neuron-derived AChE activity and its improving effect on learning and memory dysfunction caused by central cholinergic dysfunction. Methods: Inhibition of ZLA on neuron-derived AChE activity was detected through in vitro experiments. The in vivo effect of ZLA on AChE activity was observed through ex vivo experiments. The improvement effect of ZLA on learning and memory dysfunction induced by scopolamine was examined in Morris water maze task in mice. Results: ZLA inhibited activity of AChE derived from human SH-SY5Y and mouse hippocampal neurons. In addition, systematically injected ZLA inhibited AChE activity in the brains of mice in a dose-dependent manner. The results of Morris water maze test showed that ZLA significantly ameliorated the learning and memory dysfunction caused by scopolamine. Conclusion: ZLA can inhibit the activity of neuron-derived AChE. Moreover, ZLA can effectively ameliorate dementia caused by central cholinergic dysfunction. |
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