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Isolation and anti‐inflammatory activity of the sesquiterpene lactone dihydrolactucopicrin

Many sesquiterpene lactones have demonstrated anti‐inflammatory properties. Dihydrolactucopicrin (DP), a sesquiterpene lactone from Chicorium species, has a unique guainanolide ester structure, but has never before been reported for anti‐inflammatory activity. Therefore, DP was isolated from Chicorium intybus using liquid‐liquid partitioning, preparative HPLC, and LC‐MS. Anti‐inflammatory activity was determined by measuring nitric oxide production and pro‐inflammatory gene expression in RAW macrophages. DP inhibited nitric oxide production in a dose‐dependant manner (IC50 = 13 μM) and had higher activity than aspirin and other sesquiterpene lactones isolated from Chicorium intybus. DP also inhibited expression of the pro‐inflammatory genes TNF‐α, IL1β, and iNOS, which may partially account for the reduction in nitric oxide production. Overall, DP shows promise as a potent botanical anti‐inflammatory agent.