Anti-cancer effects of grailsine-al-glycoside isolated from Rhizoma Sparganii

BACKGROUND: An embryonic toxicity of Rhizoma sparganii was observed in mice. This study was aimed to evaluate the anticancer effects of Grailsine-Al-glycoside, the bioactive component of Rhizoma sparganii, on estrogen receptor-positive (ER(+)) and estrogen receptor-negative (ER(-)) cancer cell lines. METHODS: After A549, HeLa, HepG-2 and MCF-7 cells were treated with Grailsine-Al-glycoside, cell proliferation was analyzed by MTT, cell cycle and apoptosis by flow cytometry, and morphology with an immunofluorescence microscope. RESULTS: Grailsine-Al-glycoside strongly suppressed cell proliferation in a dose-dependent fashion in A549, MCF-7, HepG2, and HeLa cells, though this growth inhibitory effect on HepG2 cells was not as strong and long lasting. Compared to the control, Grailsine-Al-glycoside caused a significant increase of apoptosis in A549, MCF-7 and Hela cells. A549 and MCF-7 cells were arrested at the G2/S phase whereas HepG2 cells were arrested at the G1 phase by a high concentration of Grailsine-Al-glycoside . Cell shapes were also changed by the presence of Grailsine-Al-glycoside. CONCLUSIONS: Grailsine-Al-glycoside from Rhizoma sparganii inhibited the proliferation of ER(+) and some ER(-) cancer cells. Grailsine-Al-glycoside may be used as a chemotherapeutic agent against ER(+) and ERRα-expressing ER(-) cancers.