Rhizoma Picrorhizae (RP) is a traditional Chinese medicine, which has always been used to treat many diseases like infantile epilepsy and malnutrition. In modern applications, it has been used to treat hepatitis B and various liver injuries with remarkable curative effects. So far, more than 90 chemical components have been reported in RP, mainly including iridoid glycosides, cucurbitacins, phenylethanoid glycosides, and phenolic glycosides. Among these, iridoid glycosides are the most important active ingredients, and about 30 such compounds have been isolated at present. In pharmacology, RP is beneficial to the choleresis, liver protection, anti-inflammation, asthma relief, immune regulation, and protection of heart, brain, kidney, and other organs. There have been many investigations on this medicinal herb in recent years, and it has attracted much attention in the medicine domain. In this paper, through systematically consulting the relevant books and electronic databases, we analyzed, arranged, and summarized the available information on this herb to provide reference for its further research.