Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos

Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (FcεRI), the key molecule triggering the allergic reactions, on human mast cells. As a result of analysis of structure–activity relationship of the naturally occurring and synthesized isoflavones, 7-O-methyl glycitein (11) was disclosed as the more potent inhibitor than tectorigenin (1). These isoflavone ingredients suppressed expression of FcεRI more potently than the active flavonoids found previously. In addition, tectorigenin (1) was clarified to particularly reduce generation of γ-chain subunit to suppress expression of FcεRI among the three subunits.

Graphical abstractTectorigenin was disclosed as the inhibitor for expression of IgE receptor on human mast cells from the medicinal plant, Puerariae Flos. Furthermore, survey for synthesized analogs brought about more potent 7-O-methyl glycitein.Figure optionsDownload full-size imageDownload as PowerPoint slide