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 (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.
Tamura
Satoru
S
Osaka University, Suita, Japan.
Yoshihira
Kunichika
K
Tokumaru
Mariko
M
Zisheng
Xu
X
Murakami
Nobutoshi
N
D004305:Dose-Response Relationship, Drug; D005434:Flow Cytometry; D005455:Fluorescent Antibody Technique; D019833:Genistein / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D007529:Isoflavones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008407:Mast Cells / Q000166:cytology / Q000187:drug effects / Q000276:immunology; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D029908:Pueraria / Q000737:chemistry*; D017455:Receptors, IgE / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000276:immunology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D007529:Isoflavones; D010936:Plant Extracts; D017455:Receptors, IgE; C120039:tectorigenin; D019833:Genistein