Objective:To investigate the pharmacological activity of ent-11α-hydroxy-15-oxo-kaur-1b-en-19-oic-acid (5F)

a compound isolated from Pteris semipinnata

in vitro and in vivo inflammatory conditions. Method: The in vitro inflammation model was established using lipopolysaccharides(LPS)-induced RAW264.7 cell and different concentration of 5F was added in the culture medium. The cytotoxicity of 5F was measured by CCK-8 method. The contents of nitric oxide (NO) was examined by Griess method

tumor necrosis factor-α (TNF-α)

interleukin-1β (IL-1β)

interleukin-6 (IL-6) and prostaglandin E2(PGE2) were determined by ELISA method. The expression of inducible nitric oxide synthase (iNOS) and cyclo-oxygen-ase-2 (COX-2) were assayed by Western blot. The in vivo anti-inflammatory effect of 5F was evaluated with croton oil or arachidonic acid-induced mouse ear edema models. Result: 5F showed no cytotoxicity on RAW264.7 cells at the concentrations from 0 to 40 mg ·L-1. 5F (10

20

40 mg · L-1) could markedly decreased secretions of NO

TNF-α and IL-1β (P<0.01) in LPS-induced RAW264.7 cells. 5F(20

40 mg · L-1) exhibited the inhibitory effects on PGE2 and IL-6 releases (P<0.01). 5F (40 mg · L-1) could inhibit iNOS and COX-2 expression (P<0.05). Similarly

oral administration of 5F (100 mg · kg-1) for 1 week diminished mouse ear edema induced by croton oil or arachidonic acid (P<0.05). Conclusion: 5F has anti-inflammtory effects

which might be mediated by inhibiting the expression of iNOS and COX-2

decreasing the inflammatory factors such as TNF-α

IL-1β

IL-6

NO and PGE2.