Cancer Letters
Volume 203, Issue 2 , Pages 127-137, January 2004

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

  • Chi-Li Kuo

      Affiliations

    • Institute of Pharmacology, National Yang-Ming University, Taipei, Taiwan, ROC
    • ,
  • Chin-Wen Chi

      Affiliations

    • Institute of Pharmacology, National Yang-Ming University, Taipei, Taiwan, ROC
    • Department of Medical Research and Education, Taipei Veterans General Hospital, Rm. 822, Taipei, Taiwan, ROC
    • ,
  • Tsung-Yun Liu

      Affiliations

    • Institute of Pharmacology, National Yang-Ming University, Taipei, Taiwan, ROC
    • Department of Medical Research and Education, Taipei Veterans General Hospital, Rm. 822, Taipei, Taiwan, ROC
    • Corresponding Author InformationCorresponding author. Address: Department of Medical Research and Education, Taipei Veterans General Hospital, Rm. 822, Taipei, Taiwan, ROC. Tel.: +886-2-2874-7848; fax: +886-2-2875-1562

Received 16 May 2003; received in revised form 8 September 2003; accepted 8 September 2003.

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 μM) reduced prostaglandin E2 (PGE2) production dose-dependently with or without 12-O-tetradecanoylphorbol-13-acetate (TPA, 10nM) 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.

Keywords: Inflammation, Berberine, Prostaglandin E2, Cyclooxygenase-2, Activator protein 1

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PII: S0304-3835(03)00594-9

doi:10.1016/j.canlet.2003.09.002

Cancer Letters
Volume 203, Issue 2 , Pages 127-137, January 2004

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