Medicinal plants are vital sources of modern and traditional Chinese medicines. Sesquiterpene lactones (SLs) consist of a large group of plant secondary metabolites and belong to C15 terpenoid group. SLs have shown various biological activities including antitumor and anti‐inflammatory activities. Santamarine (STM), C15H20O3, is a kind of sesquiterpene lactone, whose molecular weight is 248.322 g/mol. Santamarine has been isolated from several plants species and has shown eminent biological activities, such as anticancer activity and anti‐inflammatory activity. In this mini‐review, we summarize the studies on the effects and the mechanisms of STM, and explore the avenues of application.