Sida szechuensis is a traditional medicine used by Dai people to treat various diseases such as furuncle, pruritus, bruise and wounds, in Xishuangbanna, Southwest, China. The chemical constituents from the aerial parts of S. szechuensis and their anti-inflammatory activities in vitro was investigated in this study. Multiple techniques, such as column chromatography on silica gel, Sephadex LH-20, semi-preparative HPLC, were used to isolate and purify compounds. Their structures were identified by physicochemical properties and NMR spectral data. All isolated compounds were evaluated for their nitric oxide(NO) inhibitory effects in lipopolysaccharide(LPS)-induced RAW 264.7 cells. The results were as follows: A total of 16 compounds were isolated from the ethanol extract and identified as kaempferol-3-O-β-D-glucopyranoside(1), kaempferol-3-O-rutinoside(2), quercetin(3), 20-hydroxyecdysone(4), α-ecdysone(5), 22-deoxyecdysterone(6), abutasterone(7), pterosterone(8), icariside E5 (9), icariside E3 (10),(+)-syringaresinol(11), pinringaresinol(12), balanophonin B(13), N-trans-feruloyl tyramine(14),(-)-loliolide(15), and palmitic acid(16). Compounds 1-3, 9-13, and 16 were isolated from this plant for the first time. The anti-inflammatory results showed that except for compounds 1, 4 and 5, all other tested compounds had NO inhibitory activities at the concentration of 50 μmol·L-1. Especially, compounds 2, 3, 11-14 demonstrated significant anti-inflammatory activities, with fifty percent NO inhibition concentration(IC50) at 18.63, 40.76, 21.46, 14.32, 16.82, 42.31 μmol·L-1, respectively. The results enrich the chemical constituents of S. szechuensis, clary the material basis of its anti-inflammatory effect, verify the scientificity of its traditional usage, and provide new insight and scientific evidence for its further development and utilization in medicine industry. [ABSTRACT FROM AUTHOR]