The genus Cephalaria, belonging to the Caprifoliaceae family, is a rich source of interesting secondary metabolites, including mainly saponins which display a variety of biological activities, such as immunomodulatory, antimicrobial and hemolytic effects. Besides these compounds, flavonoids and phenolic acids were identified in Cephalaria species. Cephalaria is employed in traditional medicine e.g., to cure cardiac and lung diseases, rheumatism, and regulate menstruation. In this review we focus on the phenolic compound composition and antioxidative activity of Cephalaria species. The antioxidant effect can be explained by flavonoids present in all parts of these plants. However, future efforts should concentrate more on in vitro and in vivo studies and also on clinical trials in order to confirm the possibility of using these plants as natural antioxidants for the pharmacology, food or cosmetic industries.