This research aimed to optimize the extraction condition, and to identify and investigate the bioactivities of triterpenoids from Crataegus cuneata. The optimum extraction conditions for recovering triterpenoids from hawthorn were ultrasound-assisted extraction with 80% methanol at 30 degrees C, 400 W for 20 min, which resulted in the recovery of total triterpenoids of 28.47 mg/g dry material. Further isolation work led to the isolation and identification of six triterpenoids: ursolic acid (1), maslic acid (2), corsolic acid (3), pomolic acid (4), euscaphic acid (5), and 2, 19-dihydroxy-3-oxo-urs-12-en-28-oic acid (6) from the triterpenoid-enriched C. cuneata fruits extracts (TCFE). Among which pomolic acid and euscaphic acid were firstly found in genus Crataegus. Biological evaluation revealed that all of the isolated triterpenoids and TCFE showed considerable xanthine oxidase and tyrosinase inhibitory activities, while some of isolates exhibited considerable acetylcholinesterase inhibitory activities. Practical applicationsTriterpenoids are one class of the major compounds with broad biological activities in hawthorn species. Crataegus cuneata is one of the two major hawthorn species found in China. But, there is few data on the constituents and bioactivity of triterpenoids present in C. cuneata. This research indicated that ultrasound-assisted extraction is the suitable method for extracting triterpenoids from C. cuneata, and TCFE could be potentially used for against xanthine oxidase and tyrosinase-induced diseases, which could provide useful information for the further development of C.cuneata fruits.