While searching for new anti-estrogenic compounds from plant kingdom, we investigated extracts of the rhizomes of Polygonatum falcatum and the aerial part of Allium schoenoprasum (Liliaceae). Four new spirostenol glycosides along with 9 known compounds have been isolated and characterized. Isolates were evaluated for their anti-estrogenic activity using estrogen responsive/unresponsive human breast cancer cell lines. Disogenin lycotetraosides (1, 2) were the most effective compounds and suppressed the estradiol (E2)-induced cell proliferation of MCF-7 and T47D at a concentration of 100 pM. Prazerigenin lycotetraosides (3 - 6) also showed the activity but needed 100 times higher concentration of the diosgenin lycotetraosides. Another diosgenin glycoside (9) which has rhamnose in its sugar chain suppressed not only E2-induced cell proliferation but also E2 unresponsive cell proliferation. To determine the estrogenic characteristics of the active constituents, the luciferase(luc) reporter assay using ERE-luc transfected MCF-7 (MCF-7/luc) and ERE-luc transfected T47D (T47D/luc) cells was carried out.