Abstract: As a traditional Chinese medicine, Agrimoniapilosa Ledeb has astringent hemostatic, detoxicative, and deficiency-restoring effects.Agrimonolides with isocoumarin skeleton, the active ingredients of Agrimoniapilosa Ledeb, have various pharmacological activities including liver protection and detoxification, anti-inflammation, anti-diabetes andantitumor.In this paper, the discovery, chemical synthesis and pharmacological activitiesof agrimonolides with isocoumarin skeleton and their glycoside derivatives were reviewed, so as to provide reference for further research and development of the title compounds.