Acanthopanax species (Araliaceae) are used in traditional medicines in Eastern cultures. In vitro and in vivo experimental studies have demonstrated that many Acanthopanax species exhibit multiple biological effects against oxidative stress, inflammation, cancer, and obesity. Additionally, analytical studies have identified compounds from Acanthopanax and described their biological mechanisms of action. One of such active compounds suppresses extracellular signal regulated kinase 1/2 phosphorylation and its kinase activity through direct binding. This compound also suppresses the activities of activator protein-1 and nuclear factor ${kappa}$-light-chain-enhancer of B cells in vitro and in vivo. Thus, further studies of the use of compounds from Acanthopanax species and more details of their mechanisms of action may help in broadening the use of Acanthopanax species in functional foods and pharmacological agents.