Ipomoea tyrianthina has been used in Mexican traditional medicine as a mild purgative, for the treatment of nervous disorders, and against tumors. In this study, the effect of convolvulin (an ether-insoluble resin glycoside) from the root of Ipomoea tyrianthina on: Central Nervous System; as spasmolytic and vasodilator; cytotoxic against cancer cell lines is evaluated. Convolvulin isolated from the root of Ipomoea tyrianthina (IT-EM) was tested on pentylentetrazole induced seizures, pentobarbital-induced hypnosis, release of GABA and glutamic acid, isolated rat aorta and ileum rings, and against Caco-2 and KB cell lines. IT-EM increased the hypnotic effect induced by pentobarbital and the release of GABA in brain cortex of mice, but did not protect mice against pentylenetetrazole-induced convulsions. IT-EM produced a significant vasodilator effect in concentration- and endothelium-dependent manners on isolated rat aorta, but did not inhibit significantly contractions on rat ileum, colon, and jejune rings. IT-EM showed cytotoxic activity against nasopharyngeal carcinoma KB cell line. Convolvulin (IT-EM) from Ipomoea tyrianthina has sedative effect, vasorelaxant effect in concentration- and endothelium-dependent manners, and cytotoxic activity against nasopharyngeal carcinoma KB cell line. Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.