Objective To explore the anti-inflammatory effect and mechanism of the ethyl acetate extracted fraction of baliospermum solanifolium (bsea) in vitro and in vivo. Methods Forty-eight female mice were randomly divided into the normal group, model group, positive control group, and the high-, medium-, and low-dose BSEA groups, respectively. Mice in the positive control group were treated with aspirin (400 mg/kg) by gavage. BSEA (176, 88, and 44 mg/kg, respectively) was given to mice in the high-, medium-, and low-dose groups, and equal volume of 0. 5% sodium carboxymethyl cellulose was given to the mice in the normal group by gavage. All of the above administration groups were given relevant medicine once a day, for consecutive 5 d. Except for the normal group, the acute inflammatory models were established. The carrageenan-induced paw edema in mice was used to explore the anti-inflammatory effects of the BSEA, and the corresponding activity was evaluated via the degree of the foot swelling and the inhibition rate. Chemical constituents were isolated and purified by chromatographic techniques, such as silica gel, MCI, Sephadex LH-20, and semipreparative HPLC, and their structures were identified by analysis of spectral data; Compound 2 was tested for the inhibitory activity against nitric oxide( NO) production in lipopolysaccharide( LPS)-stimulated RAW264. 7 cells and the mechanism of action was investigated by the molecular docking technology. Results After intragastrical administration for consecutive 5 d, no anomaly was observed for the mice, indicating that the tested sample had no effect on the normal vital activity of mice in the corresponding dosage conditions. The swelling degree of feet in the positive control group, and the high- and mediumdose BSEA groups was lower than that in the model group (P˂0. 05). Compared with the positive control group, the swelling degree of feet in the medium- and low-dose BSEA groups was higher (P˂0. 05). There were no significant differences in the swelling degree of feet between the positive control group and the high-dose BSEA group (P>0. 05). The swelling inhibition rates of the positive control group, and the high-, medium-, and low-dose BSEA groups were 45. 56%, 35. 57%, 27. 24% and 14. 19%, respectively. Four compounds were isolated and identified as 2,3-trans-6,7,4′-trimethoxyflavan- 3-ol (1), α-linolenic acid (2), methyl linolenate (3), and 1-linolenoyl glycerol (4). Compound 2 exhibited moderate inhibitory activity against LPS-induced NO production with half-maximal inhibitory concentration (IC50) value of (22. 79±1. 48) μmol/L, and had good affinity to five targets relating to inflammation, inducible nitric oxide synthase (iNOS), peroxisome proliferator-activated receptor α (PPARα), nuclear factor-κB (NF-κB), interleukin-1β (IL-1β), and tumour necrosis factor-α( TNF-α), with the docking binding energy of -7. 3, -6. 7, -6. 4, -6. 2, and -5. 9 kCal/mol, respectively. Conclusion BSEA exhibits anti-inflammatory activity; Compounds 1-4 are isolated from Baliospermum solanifolium for the first time; Compound 2 exhibits potential anti-inflammatory activity, and it may exert the effect by acting on inflammation-related targets such as iNOS, PPARα, NF-κB, IL-1β, and TNF-α. [ABSTRACT FROM AUTHOR]