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Humulus scanden, rich in flavonoids, is a traditional Chinese medicine. It is widely used in China to treat tuberculosis, dysentery and chronic colitis. In this study, Humulus scandens (H.S) was extracted in different solvents (water, n-butanol, acetic ether and chloroform) and the antioxidant, anti-inflammatory activities of extracts were investigated by four assays including DPPH, reducing power, xylene-induced mouse ear edema and cotton pellet-induced granuloma methods. And then, the acute oral toxicity of extracts and biochemical parameters such as superoxide dismutase (SOD) and catalase (CAT) in blood serum and edematous tissue of rats were also evaluated. Moreover, the active compounds were identified by LC-ESI-QTOF-MS-MS. Results showed that ethyl acetate and n-butanol extracts had the stronger antioxidant activities, while water extract appeared to be weakest among them. The anti-inflammatory test showed that the extract of n-butanol and chloroform had significant anti-inflammatory effects and could improve the activity of SOD and CAT in mice. In general, the site of n-butanol has a stronger antioxidant and anti-inflammatory activity, and 15 compounds were analyzed by LC/Q-TOF-MS/MS technology. The present study confirms the ethnobotanical use of H.S extracts as natural antioxidant, anti-inflammatory, and the composition of the active compound was preliminarily identified. [ABSTRACT FROM AUTHOR]