The chromatographic separation of methanol extract from Acer tegmentosum twigs led to the isolation of one phytosterol and five phenolic compounds. Using spectroscopic methods, the structures of these compounds were determined as β-sitosterol 3-O-β-D-glucopyranoside (1), ρ-hydroxyphenylethyl-O-β-D-glucopyranoside (Salidroside) (2), ρ-hydroxyphenylethyl alcohol (tyrosol) (3), 6’-O-galloylsalidroside (4), Quercetin 3-O-β-D-glucopyranoside (5), Quercetin (6). Compounds 1, 3, 4, 5 and 6 were isolated from the plant for the first time, but we also found that 2 and 4 were major compounds (high contents). We measured the antioxidant activity (radical/superoxide scavenging activity) and anti-inflammatory activity (nitric oxide (NO) scavenging activity in RAW 264.7, BV2 cell lines). The ethyl acetate fraction and compounds 4, 6 had both activities, but the hexane fraction and 2 had only anti-inflammatory activity. Together, all data indicate that A. tegmentosum extract is a source of functional food and treatments for neurodegenerative diseases. Key words: Acer tegmentosum, antioxidant activity, anti-inflammatory activity, compound.