Phytoestrogenic activity of Aceriphyllum rossii and rapid identification of phytoestrogens by LC–NMR/MS and bioassay-guided isolation

Aceriphyllum rossii Engler (Saxifragaceae) has been used as a nutritious food in Korea, but only minimal studies on this plant have been undertaken. We have examined the estrogenic effect of A . rossii and have discovered its potent constituents. To identify the estrogenic activity of A . rossii , we measured the transactivation of the estrogen-responsive element (ERE) in MCF-7 cells transfected with an ERE-containing construct after treatment of the extract and fractions of A . rossii . A . rossii showed a potent estrogenic activity and gallic acid ethyl ester; quercetin and kaempferol were identified as major constituents of the active fractions by liquid chromatography–nuclear magnetic resonance spectroscopy/mass spectrometry. We confirmed quercetin and kaempferol are the major active constituents after activity-guided isolation of seven compounds: gallic acid ethyl ester (1) , quercetin (2) , kaempferol (3) , quercetin-3- O -(6″-galloyl)-β- d -glucopyranoside (4) , quercetin-3- O -β- d -glucopyranoside (5) , kaempferol-3- O -(6″-galloyl)-β- d -glucopyranoside (6) , and kaempferol-3- O -β- d -glucopyranoside (7) . These results show A. rossii could be a possible candidate for the treatment of postmenopausal symptoms.