In order to explore the chemical composition and anti-tumor activity of Homalomena occulta,10 compounds were separated from the ethanol extract of Homalomena occulta by using normal phase silica gel,medium-pressure liquid chromatography,Sephadex LH-20 and other chromatographic separation methods.According to spectral analysis method,the obtained compounds include betulinic acid (1),3β-acetoxyolean-12-en-28-oic acid (2),ursolic acid (3),antriptolactone (4),cleo-lignan C (5),bullatantriol (6),pineapple coriander (7),mucrolidin (8),pinocembrin (9),and 3-(4-hydroxy-3-methoxyphenyl)-propenal (10).Except for compounds 7 and 8,the remaining compounds isolated in this experiment were isolated from Homalomena occulta for the first time.The in vitro cytotoxicity and single-cell gel electrophoresis comparison tests of compounds 2,4,and 9 with the anti-tumor drug methotrexate showed that the anti-tumor cell effects of compounds 2,4,and 9 were significant.The anti-tumor comparative test in mice also showed that it has a strong inhibitory effect on tumor tissue growth.The study of compounds 2,4,and 9 against 4 kinds of tumor cell lines including human lung cancer cells (A549) is reported for the first time.