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DOI: 10.1055/s-2006-959361
© Georg Thieme Verlag Stuttgart · New York
Biological and Pharmacological Effects of Pinusolide, a Novel Platelet Activating Factor Antagonist
Publication History
1995
1995
Publication Date:
04 January 2007 (online)
Abstract
Pinusolide, a potent platelet activating factor (PAF) receptor binding antagonist, inhibited PAF-induced aggregation of rabbit platelets with an IC50 value of 5 µM, whereas no inhibitory effects on the aggregation induced by ADP, thrombin, and collagen were observed. Pinusolide protected the mice from PAF-induced lethality with ED50 values of 1.1 mg/kg, i.v. and 69 mg/kg, p.o. Topically given pinusolide at 2 mg/ear effectively inhibited croton oil induced mouse ear edema. All the pinusolide treated ears recovered to normal healthy appearance in a sharp contrast to totally necrotized untreated ears. These results indicated that pinusolide is a potent and specific PAF antagonist in all experimental models as shown in vitro, in vivo, and in animal tests.
Key words
Platelet activating factor (PAF) antagonist - Biota orientalis - Cupressaceae - pinusolide - PAF-induced lethality - croton oil - topical anti-inflammatory activity