Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Papyriflavonol A from Broussonetia papyrifera Inhibits the Passive Cutaneous Anaphylaxis Reaction and Has a Secretory Phospholipase A2-Inhibitory Activity
Wie Jong Kwak, Tae Churl Moon, Chang Xiu Lin, Hyeun Gee Rhyn, Hyejin Jung, Eunkyung Lee, Dong Yeul Kwon, Kun Ho Son, Hyun Pyo Kim, Sam Sik Kang, Makoto Murakami, Ichiro Kudo, Hyeun Wook Chang
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Keywords: papyriflavonol A, phospholipase A2, leukotriene C4, passive cutaneous anaphylaxis
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2003 Volume 26 Issue 3 Pages 299-302

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Abstract

Papyriflavonol A, a new prenylated flavonol isolated from Broussonetia papyrifera, selectively inhibits recombinant human secretory phospholipase A2s (sPLA2s). Papyriflavonol A was found to inhibit human group IIA and V sPLA2s potently and irreversibly in a dose-dependent manner, with respective IC50 values of 3.9 and 4.5 μM. The inhibitory effects of papyriflavonol A against bovine group IB (IC50 of 76.9 μM) and the human group X (IC50 of 225 μM) sPLA2s were weaker than those against human group IIA and V sPLA2s, and human group IIF sPLA2 was not inhibited. In addition, papyriflavonol A potently inhibited the stimulus-induced production of leukotriene C4 with an IC50 value of approximately 0.64 μM 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.

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© 2003 The Pharmaceutical Society of Japan
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