Antiinflammatory effects of chiisanoside and chiisanogenin obtained from the leaves of Acanthopanax chiisanensis in the carrageenan- and Freund's complete adjuvant-induced rats.

To find the antiinflammtory constituents of Acanthopanax chiisanensis (Araliaceae) leaves, phytochemical isolation procedures were performed by activity-guided fractionation in carrageenan- and Freund's complete adjuvant (FCA) reagent-induced rat models, respectively. In the two assay system, the MeOH extract (100 and 250 mg/kg, p.o.) showed significant antiinflammtory effects. Since BuOH extract among the fractionated extracts exhibited the most potent effect, it was subjected to column chromatography to yield a main triterpene glycoside, chiisanoside (1). This compound was hydrolyzed in alkaline solution to find the biological activity of produced aglycone, chiisanogenin (1a). Oral treatment with compounds 1 and 1a produced significant antiinflammtory effects at 10 and 30 mg/kg dose, and 1a was more potent than 1. The antiiflammtory effects of the two compounds were supported by the reduction of carrageenan-induced lipid peroxidation and hydroxy radical in serum. Furthermore, treatment with 1 and 1a significantly reduced rheumatoid arthritis (RA) and C-reactive protein (CRP) factors in the rat induced by Freund's complete adjuvant reagent. Compounds, 1 and 1a, inhibited xanthine oxidase activity and increased superoxide dismutase (SOD), glutathione peroxidase and catalase indicating that both compounds scavenged reactive oxygen species (ROS).