Species of the genus Siparuna Aublet are found in Neotropical regions, mainly in the Andes. In the Brazilian folk medicine, some Siparuna species are used to combat fever, inflammation, pain, and infections. This paper presents a review of phytochemical studies and biological activities of species of this genus. Phytochemical studies of 18 species led to the isolation of mainly flavonoids (quercetin and kaempferol derivatives) as well as alkaloids (aporphinic derivatives). Essential oils were reported for 8 species among which S. guianensis is the most studied species. Numerous reports provide evidence of antimicrobial, antiplasmodic, larvicidal, cytotoxic, and antioxidant activities for some species of Siparuna genus. The reports of phytochemical studies and biological activities motivate the continued research of other species of the genus, remembering that a large part of the identified species are unknown from the natural products chemistry point of view. Manuscript profile