研究芦荟大黄素在体外对胆碱酯酶的抑制活力，及其对阿尔茨海默病模型动物脑内胆碱酯酶水平和空间识别障碍与学习记忆能力的影响。通过体外Ellman比色法检测其胆碱酯酶抑制活力；采用东莨菪碱所致小鼠记忆获得性障碍模型，随机分为4组，即空白组、模型组、石杉碱甲阳性对照组与芦荟大黄素组。以行为学实验（水迷宫法）和大脑皮层胆碱酯酶活性作为观测指标，检测芦荟大黄素的改善作用。芦荟大黄素在体外能有效抑制胆碱酯酶活性，其IC50为18.53 μg/mL；与模型组相比，芦荟大黄素能显著缩短逃避潜伏期、延长目标象限游泳时间，降低动物大脑皮层内胆碱酯酶活力，改善模型动物的学习记忆能力。因此，芦荟大黄素对东莨菪碱所引起的小鼠学习记忆能力障碍有改善作用，其作用机制可能与抑制胆碱酯酶活性有关。

The aim of this study was to investigate the in vitro inhibitory activity of aloe-emodin on cholinesterase and the in vivo effect of aloe-emodin on cholinesterase activity in the brain, extent of spatial and object recognition, as well as learning and memory ability in a mouse model of Alzheimer's disease (AD). In vitro cholinesterase inhibitory activity was measured by the Ellman’s colorimetric method, while in vivo effect was assessed by using a mouse model of scopolamine-induced dysmnesia. Mice were randomly divided into four groups: normal group, model group, huperzine A positive-control group, and aloe-emodin group. The learning and memory ability was measured by using the Morris water-maze. The ameliorating effect due to aloe-emodin was measured by using behavioral experimentation (water-maze task) and brain cholinesterase activity as indicators. Aloe-emodin was found to effectively inhibit cholinesterase activity in vitro (IC50 = 18.37 μg/mL). Compared with the model group, aloe-emodin showed a significant decrease in escape latency, an increase in swimming time in the target quadrant, a reduction in brain cholinesterase activity, and an improvement in the learning and memory ability of the animal model. Thus, aloe-emodin was shown to ameliorate learning and memory deficit induced by scopolamine in mice, and the underlying mechanism may be related to inhibition of cholinesterase activity.

国家自然科学基金（81273523）