Abstract:In order to understand the chemical constituents of Osmanthus fragrans leaves, thirteen compounds were isolated from the 95% ethanol extract. On the basis of spectral data, their structures were identified as aromadendrin (1), genistein (2), lupinalbin A (3), methy oleanolate (4), 3-ketooleanolic acid (5), fouquierol (6), 19α-hydroxyl acetylursolic acid (7), betulin (8), stigmasta-3,5-dien-7-one (9), ciwujiatone (10), p-hydroxyaceto-phenone (11), entkaurane-3,16α-diol (12), and trigoflavidone A (13). All of compounds are isolated from the leaves of O. fragrans for the first time. The compounds 2, 3, 10 showed significant antitumor activities, and their activity determination to 4 kinds of tumor cells was reported for the first time.