Madecassoside is a natural active component extracted from Centella asiatica. In recent years, a large number of studies have reported that madecassoside has a variety of biological activities, such as anticancer, anti-inflammatory and antibacterial effects, prevention and treatment of cardiovascular diseases, nerve damage, visceral damage and arthritis, and other pharmacological effects. In this paper, the pharmacological action and mechanism of madecassoside were reviewed to provide a theoretical basis for further research of madecassoside and drug development.