A new ent –kaurane type diterpene glucoside, pulicarside (1), together with three known terpenoids, paniculoside IV (2, diterpene), ent–16, 17-dihydroxy-(-)-kauran-19–oic acid (3, diterpene), and 2α–hydroxy alantolactone (4, sesquiterpene) have been isolated from Pulicaria undulata L. Their structures were determined with the help of spectral studies. Pulicarside (1) showed α-glucosidase activator activity, whereas its hydrolyzed product ent-16, 17-dihydroxy-(-)-kauran-19-oic acid (3) exhibited strong α-glucosidase inhibitory activity. Paniculoside IV (2) also shows high inhibitory potency compared with the standard drug acarbose.