With the accelerated aging of human society, Alzheimer’s disease (AD) is becoming one of the biggest threats to human health. Since multiple pathogenetic factors are implicated in the disease, the current hitting-one-target therapeutic strategy has proved inefficient to AD. As a result, finding multipotent agents that aim at multiple targets is attracting more and more attention. Although multifunc-tional anti-AD agents can be created by incorporating two or more pharmacophores in one scaffold, naturally occurring multipotent agents also attracted much attention. In this review, we first describe the functions of some typical naturally originated multipotent anti-AD compounds, then summarize their structural fea-tures and reveal that phenolics with certain flexibility predominate in these agents, which are of significance to find novel multipotent drugs to combat AD and other neurodegenerative diseases as well.