title: Effects of flavone derivatives on antigen-stimulated degranulation in RBL-2H3 cells.
abstract: Mast cells are primarily responsible for IgE-mediated allergic responses. The activation level of mast cells is reflected in their degree of degranulation. This can in turn be determined by measuring the amount of β-hexosaminidase release, a key parameter in degranulation. In this study, 40 flavone derivatives, including flavone, 14 methoxyflavones, 13 hydroxyflavones, and 12 hydroxymethoxyflavones, were evaluated for their inhibition of degranulation in rat basophilic leukemia RBL-2H3 cells. 3',7-Dihydroxyflavone inhibited degranulation (IC(50) = 13.56 μM), which was comparable to PP2 (3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine) used as a control. In addition, we report quantitative relationships between the structural properties of flavones and their inhibitory effects on degranulation.
authors.affiliation: Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 143-701, Korea            National Institute of Animal Science, Rural Development Administration, Suwon 441-706, Korea            Cell Activation Research Institute, Gyeonggi-do 464-870, Korea.
authors.forename: Doseok
authors.initials: D
authors.lastname: Hwang
authors.forename: Hye-Jin
authors.initials: HJ
authors.lastname: Park
authors.forename: Eun-Kyung
authors.initials: EK
authors.lastname: Seo
authors.forename: Joo Y
authors.initials: JY
authors.lastname: Oh
authors.forename: Sang Y
authors.initials: SY
authors.lastname: Ji
authors.forename: Dong K
authors.initials: DK
authors.lastname: Park
authors.forename: Yoongho
authors.initials: Y
authors.lastname: Lim
mesh_terms: D000818:Animals; D000941:Antigens / Q000378:metabolism*; D001665:Binding Sites; D015550:Cell Degranulation / Q000187:drug effects; D045744:Cell Line, Tumor; D047309:Flavones / Q000737:chemistry / Q000494:pharmacology*; D006860:Hydrogen Bonding; D007073:Immunoglobulin E / Q000276:immunology; D008407:Mast Cells / Q000187:drug effects* / Q000502:physiology; D051381:Rats; D013329:Structure-Activity Relationship; D001619:beta-N-Acetylhexosaminidases / Q000378:metabolism
chemical_list: D000941:Antigens; D047309:Flavones; D007073:Immunoglobulin E; D001619:beta-N-Acetylhexosaminidases