OBJECTIVE: To investigate the effects of active constituents extracted from Cortex Acanthopanacis Radicison improving the impaired memory in mice models. METHODS: The mice models of memory impairment were established using scopolamine. Ameliorating effects of the fractions and constituents on scopolamine-induced memory impairment in vivo were investigated using passive avoidance and Morris water-maze task tests, and their anti-acetylcholinesterase (AChE) and antioxidant activities in vitro examined. The isolation of constituents was performed by chromatographic methods and their structures were identified on the basis of instrumental analysis. RESULTS: Among the fractions tested, ethylacetate fraction exhibited the anti-AChE activity (25.83% +/- 0.23%) properly and excellent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and superoxide anion scavenging capacity (87.50%. +/- 0.83% and 60.22% +/- 0.43%, respectively). However, the methylene chloride fraction was much more active than the ethylacetate fraction in the passive avoidance task test (167.5% increase of step-through latency time) and Morris water-maze task test (33.3% decrease of escape latency time): Four constituents, beta-sitosterol, stigmasterol, sesamin, and hyperin were isolated from the methylene chloride fraction, among them, hyperin showed anti-acetylcholinesterase and anti-oxidant activities remarkably. Moreover, hyperin exerted a potent effect (146 +/- 38) s on memory improvement in terms of passive avoidance task test compared with the reference compound tacrine (162 +/- 43) s at a dose of 2.5 mg/kg. CONCLUSION: Hyperin, a flavonoid glucoside isolated from Cortex Acanthopanacis Radicis, inhibited AChE activity and potently ameliorated scopolamine-induced memory impairment, and its action may be partially mediated by the acetylcholine-enhancing cholinergic nervous system. (C) 2014 JTCM. All rights reserved.