Received for publication June 7, 2007.
Revised September 6, 2007.
Accepted for publication September 6, 2007.

Incensole Acetate, a Novel anti-inflammatory compound Isolated from Boswellia Resin, Inhibits Nuclear Factor (NF)-kappa B Activation

Abstract

Boswellia resin is a major anti-inflammatory agent in herbal medical tradition, as well as a common food supplement. Its anti-inflammatory activity has been attributed to boswellic acid and its derivatives. Here, we re-examined the anti-inflammatory effect of the resin, using IB degradation in TNF-stimulated HeLa cells as a read-out for a bioassay-guided fractionation. We thus isolated two novel NF-B inhibitors from the resin, their structures elucidated as incensole acetate (IA) and its non-acetylated form, incensole (IN). IA inhibited TAK/TAB-mediated IB kinase (IKK) activation loop phosphorylation, resulting in the inhibition of cytokine and LPS mediated NF-B activation. It had no effect on IKK activity in vitro, nor did it suppress IB phosphorylation in costimulated T-cells, indicating that the kinase inhibition is neither direct, nor is it affecting all NF-B activation pathways. The inhibitory effect appears specific as IA did not interfere with TNF-induced activation of JNK and p38 MAPK. IA treatment had a robust anti-inflammatory effect in a mouse inflamed paw model. Cembrenoid diterpenoids, and specifically IA and its derivatives may thus constitute a potential novel group of NF-B inhibitors, originating from an ancient anti-inflammatory herbal remedy.

Key words: Tumor necrosis factor, NFkappaB, NMR

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