Abstract: AIM: To study the constituents and bioactivity of Illicium simonsii. METHODS: The extracts of the fruits of Illicium simonsii were submitted to a combination of chromatographic materials, silica gel, ODS column chromatography and finally preparative HPLC to obtain eight compounds which were further evaluated for their cytotoxicity by MTT method. RESULTS: A new phenylpropanoid glycolside, 2, 4-dihydroxy-allylbenzene-2-O--D-glucopyranoside (1), together with seven characteristic sesquiterpene lactones, oligandrumin B (2), oligandrumin D (3), anisatin (4), veranisatin D (5), pseudomajucin (6), 1-hydroxy-3-deoxy-pseudoanisatin (7), 8-hydroxy-10-deoxycyclomerrillianolide (8) were isolated. CONCLUSION: Compound 1 is new. Compounds 1, 2, 3, 58 were isolated from this plant for the first time. None of the isolates showed inhibitory effects on the growth of non-small cell lung tumor cell line A549.