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DOI: 10.1055/s-1999-13959
Georg Thieme Verlag Stuttgart · New York
Pinusolide from the Leaves of Biota orientalis as Potent Platelet Activating Factor Antagonist
Publication History
February 20, 1998
July 19, 1998
Publication Date:
31 December 1999 (online)

Abstract:
We investigated the effect of a new PAF antagonist pinusolide, isolated from the leaves of Biota orientalis, on PAF-induced [3 H]serotinin release from rabbit platelets, hypotension and vascular permeability. Pinusolide (IC50, about 5 × 10-6 M) inhibited specifically [3 H]serotinin release from rabbit platelets when stimulated with PAF (5 × 10-8 M), but showed no effect when induced by ADP, collagen, and thrombin. It also inhibited PAF-induced hypotension in a dose-dependent manner in rats with no effect on the hypotension induced by acetylcholine, histamine and serotonin. The inhibitory effect of pinusolide on the PAF-induced vascular permeability is less specific than the induced hypotension. These results suggest that pinusolide may prove of therapeutic value in the treatment of hypotension and a molecular design of pinusolide analogues may provide the possibility of a new PAF specific antagonists.
Key words:
Biota orientalis - Cupressaceae - pinusolide - specific PAF antagonist - hypotension - vascular permeability in vivo