The invention relates to a method for extracting antitumor effective sites of selfheal, which comprises: using ethanol to soak spica of the selfheal in an extractor, and performing heating, reflux and extraction; concentrating an extracting solution into a dried extract, using chloroform and water or ethyl acetate and the water to extract the dried extract, respectively collecting an organic phase and an aqueous phase, and concentrating the organic phase and the aqueous phase to be dried; using the chloroform, methanol and the water to dissolve the organic phase, separating out superstratum after standing, and concentrating an upper solution to be dried; and adding a mobile phase to dissolve upper residue, performing reversed-phase column chromatography and elution, collecting 30 to 80 percent methanol eluent, concentrating eluent of various phases to be dried, and obtaining the antitumor effective sites. The in vitro experiments of the effective sites of the selfheal determined by the proposal of the method can obviously inhibit proliferation of Rajicells, Jurkat cells, K562 cells and 435S cells; and the in vivo experiments have tumor inhibitory efficacy on a He T lymphoma EL-4 cell mouse, and can prolong the life cycle of the He T lymphoma EL-4 cell mouse; and the antitumor effective sites of the selfheal have definite antitumor function and low toxicity.