Abstract: The phytochemical studies on the leaves of Anisopus mannii led to the isolation of seven compounds by silica gel, ODS, DIAION HP-20, Sephadex LH-20 colunmn chromatographer, their structures were elucidated on the basis of the spectroscopic analyses(NMR, HRMS)and the comparisons with the literatures as 3β-acetoxylup-20(29)-ene( 1 ), 1-acetoxy-2-isopropyl-1-tridecene( 2 ), rutin( 3 ), 3, 6′-diferuloylsucrose( 4 ), 3-O-β-D-glucopyranosyl-3-β-hydroxyolean-12-en-28-oic acid 28-O-［α-L-rhamnopyra- nosyl-(1→2)-β-D-glucopyranosyl］ ester( 5 ), conduritol A( 6 ), hoyacarnoside I( 7 ). Meanwhile, the isolated compounds were evaluated for their inhibitory activities against melanogensis in B16 melanoma cells, as the results, all compounds exhibited melanogenesis-inhibitory activity and compound 5 showed a strongest activity(Melanin content: (27. 4±3. 5)%, Cell Viability: (54. 9±5. 6)% with a concentration of 30 μmol/L)which could be further developed.