Abstract: The potential antitumor principles, maytansine and maytanprine were isolated from the overground parts of Gymnosporia diversifolia for the first time. The method of separation was modified by application of dry column chromatography, low pressure column chromatography and other separation techniques. Besides, six known compounds were also isolated and identificated as dulcitol, friedelin, β-amyrin, β-sitosterol, kaempferitrin and kaempferol-7-O-rhamnoside respectively. The latter two flavonoids were not reported in this genus before.