title: Excavation of lead compounds that inhibit mast cell degranulation by combinatorial chemistry and activity-guided.
abstract: An allergic reaction ensues after antigen binds to mast cell or basophil high affinity IgE receptor, Fc epsilonRI, resulting in degranulation of various inflammatory mediators that produce various allergic symptoms. In this study, i) we isolated the active component for the inhibition of mast cell degranulation from the extract of leaves of Castanea crenata and identified it as quercetin; ii) we established the total synthesis procedure of quercetin; iii) using quercetin as positive control, we excavated some lead compounds that possess inhibitory activities for mast cell degranulation by screening the chemical libraries of 1,3-oxazolidine derivatives prepared by solid phase combinatorial chemistry. Some of 1,3-oxazolidine compounds possessing acetyl and 3',4'-dichlorophenyl group displayed strong inhibitory activities on Fc epsilonRI-mediated mast cell degranulation, suggesting that they can be used as lead compounds for the development of anti-allergic agents.
authors.affiliation: College of Pharmacy, Drug Development Research Institute, Chonnam National University, Kwang-Ju, 500-757, Korea.
authors.forename: Hoh-Gyu
authors.initials: HG
authors.lastname: Hahn
authors.forename: Heong Sub
authors.initials: HS
authors.lastname: Oh
authors.forename: Seung Hoon
authors.initials: SH
authors.lastname: Cheon
authors.forename: Min Ho
authors.initials: MH
authors.lastname: Oak
authors.forename: Young-Ran
authors.initials: YR
authors.lastname: Kim
authors.forename: Kyeong-Man
authors.initials: KM
authors.lastname: Kim
mesh_terms: D000818:Animals; D015550:Cell Degranulation / Q000187:drug effects*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D029962:Fagaceae; D007854:Lead / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology*; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018515:Plant Leaves; D051381:Rats
chemical_list: D010936:Plant Extracts; D007854:Lead