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ETHNOPHARMACOLOGICAL RELEVANCE: Erigeron multiradiatus (Lindl.) Benth., an herb that grows in the alpine and subalpine meadow of Qinghai-Tibet plateau, has been widely used as a folk remedy by the native people for treatment of various inflammatory ailments.AIM OF THE STUDY: In order to isolate and identify the active components of Erigeron multiradiatus for anti-inflammatory activity, a preliminary phytochemical study and a bioassay-guided fractionation and purification process was performed. MATERIAL AND METHODS: The dry whole plant Erigeron multiradiatus was extracted with 50% ethanol and then separated into CHCl(3), n-BuOH, and aqueous fractions. The anti-inflammatory activities of each fraction were investigated using two in vivo inflammation models. RESULTS: These results exhibited varying degrees of anti-inflammatory activities and the n-BuOH fraction showed the strongest anti-inflammatory activities. The n-BuOH fraction was then subjected to separation and purification using macroporous resins column chromatography and Sephadex LH-20 leading to two flavonoids glucuronides identified as scutellarein-7-O-beta-glucuronide and apigenin-7-O-beta-glucuronide. Furthermore, LC-MS/MS identification and quantification of isolated compounds were also performed. CONCLUSION: Scutellarein-7-O-beta-glucuronide and apigenin-7-O-beta-glucuronide were considered as major components and principally responsible for the anti-inflammatory activity of Erigeron multiradiatus. Thus the results of our study provide a scientific basis for the utilization of Erigeron multiradiatus in traditional Tibetan medicine.