Abstract: Streptocaulon griffithii belongs to family Asclepiadaceae, and its major constituents are cardiac glycosides. Streptocaulon griffithii has attracted great attention for its antitumor effect in recent years. This review summarized the research progress in the chemical structures, antitumor effects, structure-activity relationship and mechanisms of action of cardiac glycosides from Streptocaulon griffithii, so as to provide reference for further investigation on the bioactive components with anti-tumor potential in Streptocaulon griffithii.