Biflavonoid is one of unique classes of naturally-occurring bioflavono
ids. Certain biflavonoids including amentoflavone were previously repo
rted to have inhibitory effect on the group II phospholipase A(2) acti
vity. Amentoflavone was also found to inhibit cyclooxygenase from guin
ea-pig epidermis without affecting lipoxygenase. In this study, anti-i
nflammatory and analgesic activities of amentoflavone were evaluated.
When amentoflavone was administered intraperitoneally, it showed a pat
ent anti-inflammatory activity as determined by amelioration of croton
-oil induced mouse ear edema. It also showed a potent anti-inflammator
y activity in the rat carrageenan paw edema model (ED50=42 mg/kg) comp
ared to the activity of prednisolone (35 mg/kg) and indomethacin (10 m
g/kg). However, amentoflavone did not show a significant inhibitory ac
tivity against rat adjuvant-induced arthritis, a chronic inflammatory
model. In addition, amentoflavone was found to possess a potent analge
sic activity in the acetic acid writhing test (ED50=9.6 mg/kg) compare
d to the activity of indomethacin (3.8 mg/kg). These results suggest t
hat amentoflavone may be a potential lead for a new type of anti-infla
mmatory agents having dual inhibitory activity of group II phospholipa
se A(2) and cyclooxygenase.