Cycloartane triterpenoids are widely distributed in the plant kingdom, and there have been reports of hundreds of families containing cycloartane triterpenoids. But the types and content of cycloartane are different among various plants. In recent years, a large amount of cycloartane triterpenoids have been extracted and studied from different plants, and some types of cycloartane triterpenoids exhibit great pharmacological activities in terms of antiaging, antioxidant, anti-inflammatory, anticancer, antiarrhythmic effects, and so on. Herein, we have systematically reviewed these research on the structure of naturally occurring, synthetic, and semisynthetic cycloartane triterpenoids, with particular emphasis on their pharmacological activities.