Selagin-7-O-(6''-O-acetyl-)-ß-D-glycoside, a new
flavone glycoside isolated from Cancrinia discoidea, is known to exhibit anti-inflammatory activity in vivo. This study aimed to investigate the protection of this
flavone glycoside on
inflammation in
lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. The effects of selagin-7-O-(6''-O-acetyl-)-ß-D-glycoside on inflammatory
cytokines and signaling pathways were analyzed by
enzyme-linked
immunosorbent assay, reverse transcription-polymerase chain reaction, and western blot. Results show that selagin-7-O-(6''-O-acetyl-)-ß-D-glycoside protected LPS-induced macrophage RAW 264.7 cells from injury. The
flavone glycoside markedly inhibited the LPS-induced production of
tumor necrosis factor-α, interleukin-1ß, and
interleukin-6 and increased
interleukin-10 release in a concentration-dependent manner. Furthermore, treatment with the
flavone glycoside decreased
nitric oxide and
prostaglandin E2 in LPS-challenged RAW 264.7 cells. These decreases were associated with the down-regulation of
inducible nitric oxide synthase (iNOS),
cyclooxygenase (COX-2), and
nuclear factor kappa B (NF-κB) activity. These findings suggest that the anti-inflammatory effects of selagin-7-O-(6''-O-acetyl-)-ß-D-glycoside were associated with the adjustment of inflammatory
cytokines, and attributed to the down-regulation of NF-κB and consequent suppression of the expression of iNOS and COX-2.