Papyriflavonol A from Broussonetia papyrifera inhibits the passive cutaneous anaphylaxis reaction and has a secretory phospholipase A2-inhibitory activity.
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.
Kwak
Wie Jong
WJ
SK Chemicals, Suwon-Si, Kyungki-cho, Korea.
Moon
Tae Churl
TC
Lin
Chang Xiu
CX
Rhyn
Hyeun Gee
HG
Jung
Hyejin
H
Lee
Eunkyung
E
Kwon
Dong Yeul
DY
Son
Kun Ho
KH
Kim
Hyun Pyo
HP
Kang
Sam Sik
SS
Murakami
Makoto
M
Kudo
Ichiro
I
Chang
Hyeun Wook
HW
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
D000893:Anti-Inflammatory Agents; D044948:Flavonols; C431929:papyriflavonol A; D017997:Leukotriene C4; D010741:Phospholipases A; D054467:Phospholipases A2