Berberine ameliorates TNBS-induced colitis by inhibiting lipid peroxidation, enterobacterial growth and NF-κB activation

Eur J Pharmacol. 2010 Dec 1;648(1-3):162-70. doi: 10.1016/j.ejphar.2010.08.046. Epub 2010 Sep 7.


Berberine, which is a major constituent of the rhizome of Coptidis japonica (CJ), inhibits IL-8 production in colonic epithelial cells and improves 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in mice. In our preliminary studies, berberine inhibited lipid peroxidation in liposomes prepared from l-α-phosphatidylcholine as well as TLR-4-linked NF-κB activation in HEK cells. Therefore, to clarify its anticolitic mechanism, we examined the inhibitory effects of berberine in TNBS-induced colitic C3H/HeN and C3H/HeJ mice. Its oral administration inhibited macroscopic score, body weight gain, colon shortening, myeloperoxidase activity, and lipid peroxidation in the colons of TNBS-treated C3H/HeN and C3H/HeJ mice. Berberine inhibited colonic expression of iNOS, COX-2, IL-1β, IL-6, and TNF-α, but increased IL-10 expression in the colons of TNBS-treated C3H/HeN and C3H/HeJ mice. Berberine also inhibited NF-κB activation in TNBS-treated C3H/HeN and C3H/HeJ mice, and inhibited TLR-4 expression in C3H/HeN, but not C3H/HeJ, mice. Treating C3H/HeN and C3H/HeJ mice with berberine significantly reduced the number of Enterobacteriaceae induced by TNBS, but restored the number of Bifidobacteria reduced by TNBS. Furthermore, berberine potently inhibited LPS-induced inflammation in peritoneal macrophages mainly via NF-κB and weakly via MAPKs. Based on these findings, berberine may improve colitis by inhibiting lipid peroxidation, enterobacterial growth and NF-κB activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Berberine / pharmacology*
  • Berberine / therapeutic use
  • Colitis / chemically induced
  • Colitis / drug therapy*
  • Colitis / metabolism
  • Colitis / microbiology
  • Enterobacteriaceae / drug effects*
  • Enterobacteriaceae / growth & development*
  • Enzyme Activation / drug effects
  • HEK293 Cells
  • Humans
  • Inflammation / chemically induced
  • Inflammation / metabolism
  • Intestinal Mucosa / metabolism
  • Intestines / drug effects
  • Intestines / enzymology
  • Intestines / microbiology
  • Lipid Peroxidation / drug effects*
  • Lipopolysaccharides / pharmacology
  • Macrophages, Peritoneal / drug effects
  • Macrophages, Peritoneal / immunology
  • Male
  • Mice
  • Mitogen-Activated Protein Kinases / metabolism
  • NF-kappa B / metabolism*
  • Trinitrobenzenesulfonic Acid / pharmacology*


  • Lipopolysaccharides
  • NF-kappa B
  • Berberine
  • Trinitrobenzenesulfonic Acid
  • Mitogen-Activated Protein Kinases