Background: Croton species are widely spread around the world, and present a varied chemical composition distributed in many classes of secondary metabolites, such as terpenoides, alkaloids, phenolic compounds and phenylpropanoids. These compounds can be obtained by different extraction methods, and more recently, with supercritical fluids. The crude and isolated extracts may have applications due to their biological activities in animals and humans. Methods: The text was written based on literature data from 1996 onwards. Results: The research showed in a concise way the botanical and taxonomic aspects of Croton and the success of its application is in studies related to the biological activities of the plant parts. It was also related to the chemical composition of its extracts and isolated compounds, obtained by many methods. Conclusion: In summary, the review feature studies reported the use of extracts and isolated Croton compounds due to their biological effects with antioxidant, antimicrobial, anti-inflammatory, neuroprotective, antitumor, anticancer, cytotoxic, insecticidal and allelopathic activities, with potential application in food, cosmetics, pharmaceuticals, and agrochemicals products.