Berberine inhibits ion transport in human colonic epithelia.
The effects of berberine on ion transport in both human colonic mucosal epithelia and an intestinal epithelial cell line (T84) were examined. Berberine (concentration range 0-500 microM) reduced both basal and stimulated ion transport responses in human colonic mucosae in a manner which was non-specific for Ca2+ -or cAMP-mediated signals. Similarly, in cultured intestinal epithelial monolayers, berberine inhibited Ca2+ -and cAMP-mediated responses indicating an inhibitory activity directly at the level of the epithelium rather than an indirect effect through other mucosal element(s). Berberine did not alter the rate of generation of cAMP by adenylyl cyclase or the activity of protein kinase A, the effector enzyme of the cAMP pathway. Berberine inhibited carbachol-stimulated 86Rb+ efflux from T84 monolayers. Berberine also inhibited K+ conductance in apically-permeabilised re-sected mucosae. These results indicate i) that berberine exerts an anti-secretory action directly upon epithelial cells and ii) the mechanism of action may be at the level of blockade of K+ channels.
Taylor
C T
CT
Department of Pharmacology, University College Dublin, Belfield, Ireland.
Winter
D C
DC
Skelly
M M
MM
O'Donoghue
D P
DP
O'Sullivan
G C
GC
Harvey
B J
BJ
Baird
A W
AW
D001599:Berberine / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D002217:Carbachol / Q000494:pharmacology; D002463:Cell Membrane Permeability / Q000187:drug effects; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D017868:Cyclic AMP-Dependent Protein Kinases / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D006801:Humans; D066298:In Vitro Techniques; D007413:Intestinal Mucosa / Q000187:drug effects* / Q000502:physiology; D017136:Ion Transport / Q000187:drug effects; D007476:Ionophores / Q000494:pharmacology; D008564:Membrane Potentials / Q000187:drug effects; D018721:Muscarinic Agonists / Q000494:pharmacology; D009761:Nystatin / Q000494:pharmacology; D015221:Potassium Channels / Q000187:drug effects / Q000502:physiology; D012414:Rubidium Radioisotopes; D014407:Tumor Cells, Cultured
D007476:Ionophores; D018721:Muscarinic Agonists; D015221:Potassium Channels; D012414:Rubidium Radioisotopes; D001599:Berberine; D009761:Nystatin; D005576:Colforsin; D002217:Carbachol; D000242:Cyclic AMP; D017868:Cyclic AMP-Dependent Protein Kinases; D002118:Calcium