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
