Abstract: Danshensu(DSS) is one of the most important water-soluble components, has been widely used for the treatment of angina pectoris. Numerous studies have shown that DSS can improve microcirculation and protect endothelial cells from damage, and it has antioxidant, anti-inflammatory, anti-platelet aggregation and other pharmacological activities. The study show that DSS plays a cardiac protective effect on ischemia reperfusion(I/R) injury mainly through the activation of AKT/ERK1/2/Nrf2 signaling pathway. The phenolic hydroxyl group and hydroxy carboxylic acid in DSS structure hinder its further development and clinical application. The development and synthesis of DSS derivatives with higher pharmacological activity, better stability and lipid solubility have become a research hotspot in recent years. In this paper, the advances in pharmacological action, molecular mechanism, derivative research and dosage form application of DSS in recent years were reviewed to make a more comprehensive and in-depth understanding of DSS, in order to provide reference for its application and clinical research.