Description:
<jats:p><jats:italic>Oplopanax horridus</jats:italic>, well-known as Devil’s club, is probably the most important ethnobotanical to most indigenous people living in the Pacific Northwest of North America. Compared with the long history of traditional use and widespread distribution in North America, the study of<jats:italic> O. horridus</jats:italic> is relatively limited. In the past decade, some exciting advances have been presented on the phytochemistry and pharmacological diversity and structure-activity relationship on anticancer effects of<jats:italic> O. horridus</jats:italic>. To date, no systematic review has been drafted on the recent advances of<jats:italic> O. horridus</jats:italic>. In this review, the different phytochemicals in<jats:italic> O. horridus</jats:italic> are compiled, including purified compounds and volatile components. Animal and in vitro studies are also described and discussed. Especially, the potential structural-activity relationship of polyynes on anticancer effects is highlighted. This review aimed to provide comprehensive and useful information for researching<jats:italic> O. horridus</jats:italic> and finding potential agents in drug discovery.</jats:p>