This paper describes the cytotoxic and antitumoral activities of kaempferol 3-O-(6”-O-E-pcoumaroyl)-β-D-glucopyranoside (tiliroside), kaempferol 3,7-di-O-α-L-rhamnoside (dhiramnoside) and of the mixture of sitosteryl-3-O-β-D-glucopyranoside and stigmasteryl-3-O-β-D-glucopyranoside (GM) isolated of the Herissantia crispa. The compounds did not present cytotoxic activity against NCI-H292, HEp-2 and KB cells. In vivo, dhiramnoside did not present significant inhibitory activity of the growth of sarcoma 180 when compared with the control group; however, tiliroside and GM-treated animals showed a high inhibition rate in the growth of the tumor. Tiliroside inhibits significantly the growth of the carcinoma of Ehrlich. In conclusion, tiliroside exhibited promising antitumor effects without an expressive toxicity.Colegio de Farmacéuticos de la Provincia de Buenos Aire