Papyriflavonol A from Broussonetia papyrifera inhibits the passive cutaneous anaphylaxis reaction and has a secretory phospholipase A 2-inhibitory activity

초록

Papyriflavonol A, a new prenylated flavonol isolated from Broussonetia papyrifera, selectively inhibits recombinant human secretory phospholipase A<inf>2</inf>s (sPLA<inf>2</inf>s). Papyriflavonol A was found to inhibit human group IIA and V sPLA<inf>2</inf>s potently and irreversibly in a dose-dependent manner, with respective IC<inf>50</inf> values of 3.9 and 4.5 μM. The inhibitory effects of papyriflavonol A against bovine group IB (IC<inf>50</inf> of 76.9 μM) and the human group X (IC<inf>50</inf> of 225 μM) sPLA <inf>2</inf>s were weaker than those against human group IIA and V sPLA <inf>2</inf>, and human group IIF sPLA<inf>2</inf> was not inhibited. In addition, papyriflavonol A potently inhibited the stimulus-induced production of leukotriene C<inf>4</inf> with an IC<inf>50</inf> 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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