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提取物及其活性成分对阿尔茨海默病的多功能性。

Multifunctionality of Extract and Its Active Constituents against Alzheimer's Disease.

作者信息

Boonyarat Chantana, Yenjai Chavi, Monthakantirat Orawan, Kaewamatawong Rawiwun, Poonsawas Pattaporn, Wangboonskul Jinda, Chaiwiwatrakul Suchada, Waiwut Pornthip

机构信息

Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.

Center for Research and Development of Herbal Health Products, Khon Kaen University, Khon Kaen 40002, Thailand.

出版信息

Curr Issues Mol Biol. 2022 Aug 15;44(8):3681-3694. doi: 10.3390/cimb44080252.

Abstract

This study was designed to investigate the effects of the root-bark extract of (CH) and its active constituents (nordentatin and 7-methoxyheptaphylline) on pharmacological activities regarding selected targets associated with AD, namely, its antioxidant activity, inhibition of Aβ aggregation, acetylcholinesterase (AChE) activity, and neuroprotective effects. The effect of the CH extract on the cognitive impairment induced by scopolamine was also evaluated in mice. The effects of the CH extract and its active constituents on radical scavenging, Aβ aggregation, and AChE activity were investigated with a 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid (ABTS) assay, a thioflavin-T assay, and Ellman's method. The neuroprotective effects of the extract against hydrogen-peroxide and Aβ toxicity were evaluated with a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. In addition, the effects on cognitive impairment induced by scopolamine in mice were evaluated using Morris-water-maze and modified-Y-maze test models. The results of the present study demonstrate that the root-bark extract of CH shows multimodal actions relevant to the AD pathological cascade, including antioxidant effects, the inhibition of Aβ aggregation, the inhibition of AChE function, and neuroprotection against oxidative stress and Aβ toxicity. The extracts could improve both the short- and long-term memory deficits induced by scopolamine in mice.

摘要

本研究旨在探讨[植物名称]根皮提取物(CH)及其活性成分(去甲橙皮苷和7-甲氧基七叶苷)对与阿尔茨海默病(AD)相关的选定靶点的药理活性的影响,即其抗氧化活性、对β淀粉样蛋白(Aβ)聚集的抑制作用、乙酰胆碱酯酶(AChE)活性以及神经保护作用。还评估了CH提取物对东莨菪碱诱导的小鼠认知障碍的影响。采用2,2'-联氮-双-(3-乙基苯并噻唑啉-6-磺酸)(ABTS)法、硫黄素-T法和埃尔曼法研究了CH提取物及其活性成分对自由基清除、Aβ聚集和AChE活性的影响。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)法评估了该提取物对过氧化氢和Aβ毒性的神经保护作用。此外,使用莫里斯水迷宫和改良Y迷宫试验模型评估了其对东莨菪碱诱导的小鼠认知障碍的影响。本研究结果表明,CH根皮提取物表现出与AD病理级联相关的多模式作用,包括抗氧化作用、对Aβ聚集的抑制作用、对AChE功能的抑制作用以及对氧化应激和Aβ毒性的神经保护作用。该提取物可以改善东莨菪碱诱导的小鼠短期和长期记忆缺陷。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/25ee/9406758/99dbbaef11d6/cimb-44-00252-g001.jpg

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