title: Inhibition by berberine of cyclooxygenase-2 transcriptional activity in human colon cancer cells.
abstract: The enzyme cyclooxygenase-2 (COX-2) is abundantly expressed in colon cancer cells and plays a key role in colon tumorigenesis. Compounds inhibiting COX-2 transcriptional activity have therefore potentially a chemopreventive property against colon tumor formation. An assay method for estimating COX-2 transcriptional activity in human colon cancer cells was established using a beta-galactosidase reporter gene system, and examination was made of various medicinal herbs and their ingredients for an inhibitory effect on COX-2 transcriptional activity. We found that berberine, an isoquinoline alkaloid present in plants of the genera Berberis and Coptis, effectively inhibits COX-2 transcriptional activity in colon cancer cells in a dose- and time-dependent manner at concentrations higher than 0.3 microM. The present findings may further explain the mechanism of anti-inflammatory and anti-tumor promoting effects of berberine.
authors.affiliation: Department of Oriental Medicine, Gifu University School of Medicine, Japan. kfukuda@cc.gifu-u.ac.jp
authors.forename: K
authors.initials: K
authors.lastname: Fukuda
authors.forename: Y
authors.initials: Y
authors.lastname: Hibiya
authors.forename: M
authors.initials: M
authors.lastname: Mutoh
authors.forename: M
authors.initials: M
authors.lastname: Koshiji
authors.forename: S
authors.initials: S
authors.lastname: Akao
authors.forename: H
authors.initials: H
authors.lastname: Fujiwara
mesh_terms: D001599:Berberine / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D003110:Colonic Neoplasms / Q000201:enzymology* / Q000235:genetics; D003513:Cycloheximide / Q000494:pharmacology; D051546:Cyclooxygenase 2; D017930:Genes, Reporter / Q000187:drug effects; D006801:Humans; D007527:Isoenzymes / Q000096:biosynthesis* / Q000235:genetics; D008565:Membrane Proteins; D010957:Plasmids; D011451:Prostaglandin-Endoperoxide Synthases / Q000096:biosynthesis* / Q000235:genetics; D011500:Protein Synthesis Inhibitors / Q000494:pharmacology; D014158:Transcription, Genetic / Q000187:drug effects*; D014162:Transfection; D014407:Tumor Cells, Cultured
chemical_list: D007527:Isoenzymes; D008565:Membrane Proteins; D011500:Protein Synthesis Inhibitors; D001599:Berberine; D003513:Cycloheximide; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases