Since ancient times, Hibiscus species (Malvaceae) have been used as a folk remedy for the treatment of skin diseases, as an antifertility agent, antiseptic, and carminative. Some compounds isolated from the species, such as flavonoids, phenolic acids, and polysaccharides, are considered responsible for these activities. This review aims to summarize the worldwide reported biological activities and phytoconstituents associated with this genus for the past 40 years.