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Bioorg Med Chem Lett ; 20(13): 3872-5, 2010 Jul 01.
Article in English | MEDLINE | ID: mdl-20627560

ABSTRACT

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 (FcepsilonRI), 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 FcepsilonRI more potently than the active flavonoids found previously. In addition, tectorigenin (1) was clarified to particularly reduce generation of gamma-chain subunit to suppress expression of FcepsilonRI among the three subunits.


Subject(s)
Genistein/pharmacology , Isoflavones/pharmacology , Plant Extracts/pharmacology , Pueraria/chemistry , Receptors, IgE/antagonists & inhibitors , Dose-Response Relationship, Drug , Flow Cytometry , Fluorescent Antibody Technique , Genistein/chemistry , Genistein/isolation & purification , Humans , Isoflavones/chemistry , Isoflavones/isolation & purification , Mast Cells/cytology , Mast Cells/drug effects , Mast Cells/immunology , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Receptors, IgE/biosynthesis , Receptors, IgE/immunology , Stereoisomerism , Structure-Activity Relationship
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