title: Papyriflavonol A from Broussonetia papyrifera inhibits the passive cutaneous anaphylaxis reaction and has a secretory phospholipase A2-inhibitory activity.
abstract: Papyriflavonol A, a new prenylated flavonol isolated from Broussonetia papyrifera, selectively inhibits recombinant human secretory phospholipase A(2)s (sPLA(2)s). Papyriflavonol A was found to inhibit human group IIA and V sPLA(2)s potently and irreversibly in a dose-dependent manner, with respective IC(50) values of 3.9 and 4.5 microM. The inhibitory effects of papyriflavonol A against bovine group IB (IC(50) of 76.9 microM) and the human group X (IC(50) of 225 microM) sPLA(2)s were weaker than those against human group IIA and V sPLA(2)s, and human group IIF sPLA(2) was not inhibited. In addition, papyriflavonol A potently inhibited the stimulus-induced production of leukotriene C(4) with an IC(50) value of approximately 0.64 microM in mouse bone marrow-derived mast cells. In addition, papyriflavonol A significantly reduced IgE-dependent passive cutaneous anaphylaxis in rats. These results indicate that papyriflavonol A provides a basis for novel types of antiinflammatory drugs.
authors.affiliation: SK Chemicals, Suwon-Si, Kyungki-cho, Korea.
authors.forename: Wie Jong
authors.initials: WJ
authors.lastname: Kwak
authors.forename: Tae Churl
authors.initials: TC
authors.lastname: Moon
authors.forename: Chang Xiu
authors.initials: CX
authors.lastname: Lin
authors.forename: Hyeun Gee
authors.initials: HG
authors.lastname: Rhyn
authors.forename: Hyejin
authors.initials: H
authors.lastname: Jung
authors.forename: Eunkyung
authors.initials: E
authors.lastname: Lee
authors.forename: Dong Yeul
authors.initials: DY
authors.lastname: Kwon
authors.forename: Kun Ho
authors.initials: KH
authors.lastname: Son
authors.forename: Hyun Pyo
authors.initials: HP
authors.lastname: Kim
authors.forename: Sam Sik
authors.initials: SS
authors.lastname: Kang
authors.forename: Makoto
authors.initials: M
authors.lastname: Murakami
authors.forename: Ichiro
authors.initials: I
authors.lastname: Kudo
authors.forename: Hyeun Wook
authors.initials: HW
authors.lastname: Chang
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D016367:Baculoviridae; D001854:Bone Marrow Cells / Q000187:drug effects; D031623:Broussonetia; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004622:Embryo, Mammalian; D004625:Embryo, Nonmammalian; D044948:Flavonols / Q000096:biosynthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D007313:Insecta / Q000821:virology; D007668:Kidney; D017997:Leukotriene C4 / Q000032:analysis / Q000096:biosynthesis; D008297:Male; D008407:Mast Cells / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects* / Q000276:immunology; D010741:Phospholipases A / Q000037:antagonists & inhibitors / Q000145:classification / Q000235:genetics / Q000378:metabolism*; D054467:Phospholipases A2; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000893:Anti-Inflammatory Agents; D044948:Flavonols; C431929:papyriflavonol A; D017997:Leukotriene C4; D010741:Phospholipases A; D054467:Phospholipases A2