AIM: To examine the effects of berberine, an isoquinoline alkaloid with a long history used as a tonic remedy for liver and heart, on ion channels of isolated rat hepatocytes.METHODS: Tight-seal whole-cell patch-clamp...AIM: To examine the effects of berberine, an isoquinoline alkaloid with a long history used as a tonic remedy for liver and heart, on ion channels of isolated rat hepatocytes.METHODS: Tight-seal whole-cell patch-clamp techniques were performed to investigate the effects of berberine on the delayed outward potassium currents (Ik), inward rectifier potassium currents (Ik1) and Ca^2+ release-activated Ca^+ currents (ICRAC) in enzymatically isolated rat hepatocytes.RESULTS: Berbenne 1-300 μmol/L reduced/K in a concentration-dependent manner with EC50 of 38.86=1=5.37 μmol/L and nH of 0.82±0.05 (n = 8). When the bath solution was changed to tetraethylammonium (TEA) 8 retool/L,IK was inhibited.Berberine 30 μmol/L reduced/K at all examined membranepote ntials, especially at potentials positive to +60 mV (n = 8,P<0.05 or P<0.01 vs control). Berberine had mild inhibitory effects on IK1 in rat hepatocytes. Berberine 1-300 μmol/L also inhibited ICRAC in a concentration-dependent fashion. The fitting parameters were EC50 = 47.20±10.86 μmol/L,nH= 0.71±0.09 (n = 8). The peak value of/CRAC in the I-Vrelationship was decreased by berberine 30 μmol/L at potentialnegative to -80 mV (n = 8, P<0.05 vscontrol). But the reverse potential of/CRAC occurred at voltage 0 mV in all cells.CONCLUSION: Berberine has inhibitory effects on potassium and calcium currents in isolated rat hepatocytes, which may be involved in hepatoprotection.展开更多
文摘AIM: To examine the effects of berberine, an isoquinoline alkaloid with a long history used as a tonic remedy for liver and heart, on ion channels of isolated rat hepatocytes.METHODS: Tight-seal whole-cell patch-clamp techniques were performed to investigate the effects of berberine on the delayed outward potassium currents (Ik), inward rectifier potassium currents (Ik1) and Ca^2+ release-activated Ca^+ currents (ICRAC) in enzymatically isolated rat hepatocytes.RESULTS: Berbenne 1-300 μmol/L reduced/K in a concentration-dependent manner with EC50 of 38.86=1=5.37 μmol/L and nH of 0.82±0.05 (n = 8). When the bath solution was changed to tetraethylammonium (TEA) 8 retool/L,IK was inhibited.Berberine 30 μmol/L reduced/K at all examined membranepote ntials, especially at potentials positive to +60 mV (n = 8,P<0.05 or P<0.01 vs control). Berberine had mild inhibitory effects on IK1 in rat hepatocytes. Berberine 1-300 μmol/L also inhibited ICRAC in a concentration-dependent fashion. The fitting parameters were EC50 = 47.20±10.86 μmol/L,nH= 0.71±0.09 (n = 8). The peak value of/CRAC in the I-Vrelationship was decreased by berberine 30 μmol/L at potentialnegative to -80 mV (n = 8, P<0.05 vscontrol). But the reverse potential of/CRAC occurred at voltage 0 mV in all cells.CONCLUSION: Berberine has inhibitory effects on potassium and calcium currents in isolated rat hepatocytes, which may be involved in hepatoprotection.