Inhibitory effect of echinocystic acid on 12-O-tetradecanoylphorbol-13-acetate-induced dermatitis in mice.

The rhizome of Codonopsis lanceolata (family Campanulaceae), which contains lancemaside A as a main constituent, is frequently used in the traditional Chinese medicine for the treatment of inflammatory diseases. Lancemaside A exhibits anti-inflammatory effect in vitro and in vivo. However, orally administered lancemaside A is metabolized to echinocystic acid by the intestinal microflora and the metabolite is absorbed into the blood. Therefore, to understand whether echinocystic acid is effective against skin inflammatory diseases, we assessed its inhibitory effect against 12-O-tetra decanoylphorbol-13-acetate (TPA)-induced ear inflammation in mice. Topically administered echinocystic acid potently suppressed TPA-induced ear swelling. The suppression rates at 0.05 and 0.10 % concentrations were 65 and 73 %, respectively. Echinocystic acid also inhibited TPA-induced myeloperoxidase activity, as well as COX-2, iNOS, TNF-α and IL-1β expressions. Echinocystic acid inhibited NF-κB in TPA-treated mouse ears, as well as in lipopolysaccharide-stimulated peritoneal macrophages. Its potency is comparable with that of dexamethasone. These findings indicate that echinocystic acid may ameliorate inflammatory diseases, such as dermatitis.