Efficacy of Dibenzoylmethane Derivatives in Protecting against Endoplasmic Reticulum Stress and Inhibiting Nuclear Factor Kappa B on Dextran Sulfate Sodium Induced Colitis in Mice

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We recently reported that some dibenzoylmethane (DBM) derivatives have a protective effect against endoplasmic reticulum (ER) stress and inhibit nuclear factor kappa B (NF-κB). The aim of this study was to evaluate the effect of DBM derivatives against dextran sulfate sodium (DSS)-induced colitis in mice. The DBM derivatives used in this study were 4,4′-dibromodibenzoylmethane that protects against ER stress, and, 4,4′-dichlorodibenzoylmethane that protects against ER stress and inhibits NF-κB. In each group, the presence of faecal occult blood, the disease activity index score (DAI score) and intestinal length were examined. Both of the DBM derivatives with protective effects against ER stress significantly improved occult bleeding of the colitis induced by DSS. The 4,4′-dichlorodibenzoylmethane significantly reduced the DAI score and inhibited the shortening of colon length, but the 4,4′-dibromodibenzoylmethane did not. These findings suggest that both the protective effect against ER stress and inhibitory effect on NF-κB are needed in the treatment of DSS-induced colitis. Therefore, the effect of 4,4′-dichlorodibenzoylmethane maybe beneficial in the therapeutic regulation of ulcerative colitis.
日本薬学会の論文