The anti-inflammatory potential of berberine in vitro and in vivo

Cancer Lett. 2004 Jan 20;203(2):127-37. doi: 10.1016/j.canlet.2003.09.002.

Abstract

Berberine, an isoquinoline alkaloid, has a wide range of pharmacological effects, including anti-inflammation, yet the exact mechanism is unknown. Because cyclooxygenase-2 (COX-2) plays a key role in prostaglandins (PGs) synthesis, which is elevated in inflammation, we examined whether the anti-inflammatory mechanism of berberine is mediated through COX-2 regulation. In oral cancer cell line OC2 and KB cells, a 12 h berberine treatment (1, 10, and 100 microM) reduced prostaglandin E2 (PGE2) production dose-dependently with or without 12-O-tetradecanoylphorbol-13-acetate (TPA, 10 nM) induction. This berberine induced effect occurred rapidly (3 h) as a result of reduced COX-2 protein, but not enzyme activity. The electrophoretic mobility shift assay revealed that activator protein 1 (AP-1) binding was decreased in oral cancer cells treated with berberine for 2 h. Further analysis showed that berberine inhibited AP-1 binding directly. These anti-inflammatory effects paralleled to the in vivo results where berberine pretreatment of Wistar rat inhibited the production of exudates and PGE2 in carrageenan induced air pouch.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Berberine / pharmacology*
  • Blotting, Western
  • Cell Line, Tumor
  • Cell Nucleus / metabolism
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / pharmacology
  • Dinoprostone / metabolism
  • Dose-Response Relationship, Drug
  • Gene Expression Regulation, Enzymologic
  • Gene Expression Regulation, Neoplastic
  • Humans
  • In Vitro Techniques
  • Indomethacin / pharmacology
  • Isoenzymes / metabolism
  • Membrane Proteins
  • Mouth Neoplasms / metabolism
  • Mouth Neoplasms / pathology
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Protein Binding
  • Rats
  • Rats, Wistar
  • Tetradecanoylphorbol Acetate / pharmacology
  • Time Factors
  • Transcription Factor AP-1 / metabolism
  • Up-Regulation

Substances

  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Transcription Factor AP-1
  • Berberine
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Dinoprostone
  • Tetradecanoylphorbol Acetate
  • Indomethacin