Background: Inflammatory bowel disease is a chronic and idiopathic gastrointestinal inflammation mediated by disregulated immune responses. Artemisinin (a chemical from a traditional Chinese herbal medicine Artemisia annua L.) and its derivatives have been proven to exhibit anti-inflammatory
and immunomodulatory effects in the treatment of systemic lupus erythematosus and rheumatoid arthritis with low side-effects. This study is aimed to evaluate the potential therapeutic value of artesunate for inflammatory bowel disease. Methods: Murine colitis was induced by either oral administration
of dextran sulfate sodium salt (DSS) or intrarectal delivery of 2,4,6- trinitrobenzene sulfonic acid (TNBS) or oxazolone. Mice were treated with artesunate (150mg/kg/day). Peritoneal macrophages were stimulated with lipopolysaccharide (LPS) in the presence or absence of artesunate. Changes
in cytokines or proteins of interests were analyzed by enzyme-linked immunosorbent assay (ELISA) or SDS-PAGE/Western blot. Results: Artesunate significantly ameliorated DSS colitis and TNBS colitis (but not oxazolone colitis), including reduced weight loss and disease activity, as well as
macroscopic and microscopic colonic injury. The expression of NF-κBp65 and p-IκB-α were reduced in artesunate treated TNBS colitis compared with untreated. The levels of IFN-γ, IL-17, and TNF-α were significantly decreased in artesunate treated TNBS colitis or DSS
colitis. Furthermore, in vitro artesunate treatment significantly inhibited TNF-α production by LPS-activated macrophages. Conclusions: Artesunate suppresses TNF-α expression in vitro and in vivo as well as T-helper (Th)1/Th17 responses in TNBS colitis model. Our data suggest a novel
clinical application of artesunate as a potential therapy for Crohn's disease.
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