The scientific basis for the statement that plants and their active constituents play an important role in the prevention of chronic and degenerative diseases is continuously advancing. In fact, the origin of many therapeutic substances is due to secondary metabolism in the plant. The genus Hibiscus contains 220 species distributed around the world. It is an interesting source of potential bioactive molecules, as phenolic compounds, triterpene derivatives, phytosteroids, with antioxidant, cardioprotective, antihypertensive and antiproliferative activities. This work reviews the pharmacological evidence of extracts of plants from the genus Hibiscus, giving an overview of the most studied biological effects and the known phytochemical composition. Although more studies are necessary, Hibiscus spp. exhibits proven potential to become of important pharmacological interest.