Anti-inflammatory effects of ß-sitosterol-ß-D-glucoside from Trachelospermum jasminoides (Apocynaceae) in lipopolysaccharide-stimulated RAW 264.7 murine macrophages.

Trachelospermum jasminoides (Apocynaceae) has pharmacological effects that include anti-inflammatory, anti-bacterial and anti-viral activities, which have been observed from various studies. Of these pharmacological effects, the anti-inflammatory capacity of compounds from T. jasminoides is not yet known exactly. In this study, we investigated the compound that can be used for the suppression of lipopolysacchaide (LPS) stimulated inflammatory responses in macrophages among the five isolated compounds. ß-sitosterol-ß-D-glucoside (1) was found to reduce nitric oxide (NO) production from LPS-induced RAW 264.7 cells the most. In addition, compound 1 strongly inhibited the interleukin 6 (IL-6) activities of stimulated macrophages. Treatment of RAW 264.7 cells with compound 1 reduced secretion of inflammatory elements including tumour necrosis factor - alpha (TNF-α) and interleukin 1 beta (IL-1ß). Thus, compound 1 may be a useful candidate for the development of new drugs to treat endotoxemia and inflammation accompanied by the overproduction of NO.

Bioassay-guided isolation of novel compound from Paeonia suffruticosa Andrews roots as an IL-1ß inhibitor.

The inhibition of Interleukin-1beta (IL-1ß) is of substantial interest for the treatment of rheumatoid arthritis. Using an in vitro assay with RAW 264.7 cells, oxo-acetic acid 2-ethoxy-4-(3-hydroxy-2-oxopropyl) phenyl ester (1) was isolated from the roots of Paeonia suffruticosa Andrews as an inhibitor of IL-1ß with an IC(50) value of 56 µM. Compound 1 is a novel phenylesteric compound from P. suffruticosa Andrews. Compound 1 was shown to inhibit the production of pro-inflammatory cytokines in RAW 264.7 cells. Thus, a possible new action of novel compound is provided explaining the anti-rheumatoid arthritic properties of P. suffruticosa Andrews.