Echinocystic acid, a metabolite of lancemaside A, inhibits TNBS-induced colitis in mice

Supriya R Hyam, Se-Eun Jang, Jin-Ju Jeong, Eun-Ha Joh, Myung Joo Han, Dong-Hyun Kim
International Immunopharmacology 2013, 15 (2): 433-41
The rhizome of Codonopsis lanceolata (CL, family Campanulaceae), of which the main constituent is lancemaside A, has been used for cough and bronchitis in traditional Chinese medicine. To evaluate anti-colitic effect of CL, we examined anti-inflammatory effect of CL extracts, lancemaside A and its metabolites in lipopolysaccharide (LPS)-stimulated peritoneal macrophages and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitic mice. Among CL extracts, CL BuOH extract inhibited LPS-induced IL-1β, IL-6 and TNF-α expression, as well as NF-κB activation most potently. CL BuOH extract also inhibited colon shortening and myeloperoxidase activity in TNBS-induced colitic mice. Among lancemaside A, a main constituent of CL BuOH extract, and its metabolites (lancemaside X, echinocystic acid-3-O-β-d-glucopyranoside and echinocystic acid), echinocystic acid inhibited the expression of the pro-inflammatory cytokines, IL-1β, IL-6, and TNF-α, as well as the phosphorylation of IKKβ and p65 in LPS-stimulated peritoneal macrophages most potently. Echinocystic acid also potently inhibited the binding of LPS to TLR4 on peritoneal macrophages. Lancemaside A and its metabolite, echinocystic acid, inhibited TNBS-induced colonic inflammation, including colon shortening, increased myeloperoxidase activity and pro-inflammatory cytokine expression, and NF-κB activation in mice. The anti-colitic effect of echinocystic acid was superior to that of lancemaside A. Based on these findings, orally administered lancemaside A may be metabolized to echinocystic acid, which may express anti-colitic effect by inhibiting the binding of LPS to TLR4 on the macrophages.

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