Linarin down-regulates phagocytosis, pro-inflammatory cytokine production, and activation marker expression in RAW264.7 macrophages

Plant-extracted flavonoid glycosides have been reported to be bioactive compounds with pleiotropic functions, including antioxidant, anti-inflammatory, and anti-cancer effects. This study investigated the anti-inflammatory role of linarin (acacetin-7-rutinoside, which is found in Chrysanthemum indicum (Gam-Guk) and Dendranthema zawadskii (Gu-Jul-Cho)), on lipopolysaccharide-stimulated RAW264.7 macrophages. Linarin treatments exhibited no cytotoxicity up to a concentration of 30 mu M, as assessed by MTT assay. The production of nitric oxide, an inflammatory mediator, was decreased by addition of linarin. The secretion of pro-inflammatory cytokines, interleukin-1 beta and interleukin-6, was significantly decreased in a dose-dependent manner. Linarin also decreased the phagocytic ability of macrophages following co-culture with fluorescent beads. In addition, expression levels of antigen presenting surface markers, MHC II and CD80, were suppressed by linarin. Taken together, these results indicate that the flavonoid glycoside linarin has an anti-inflammatory effect, in part through the suppression of phagocytosis, cytokine production, and antigen presentation in macrophages.