Zinnia genus contains annual and perennial plants belonging to family Asteraceae and comprising about 20 species native to South America. Zinnia species are used in folk medicine for the treatment of malaria and stomach pain and are used as hepatoprotective, antiparasitic, antifungal and antibacterial agents. Zinnia plants are well known ornamental plants with large, beautiful and attractive flowers. This review is first attempt for assembling the published papers about the isolated phytochemical components and pharmacological actions of this genus. Many studies reported that Zinnia contains numerous secondary metabolites of different classes including sterols, flavonoids, sesquiterpenes, diterpenes and hydrocarbons. Zinnia plants also are reported to possess a wide range of biological effects such as antioxidant, hepatoprotective, cytotoxic, antibacterial, antifungal and insecticidal activities. This review potentiates the researchers for carrying out further studies on this genus to isolate and develop new drugs from natural sources with wide margin of safety and understanding their effects and possible mechanism of actions.