In this study, multifaceted targets of hispolon and its analogs No.6 and No.7 in free radical scavenging activities, anti-nitric oxide productions, inhibitions against AChE and Aβ1 − 42 aggregations, neurite outgrowth stimulated activities, and learning behavior improvements in scopolamine-induced cognitive impairment mouse models might be new routes for AD treatments. This evidence concerns the gene ACHE and Alzheimer disease.