Activation effect of natural flavonoid compound baicalein on human wild cystic fibrosis transmembrane conductance regulator chloride channel / 吉林大学学报(医学版)

ABSTRACT

Objective To study activation effect of a natural compound baicalein on cystic fibrosis transmembrane conductance regulator(CFTR) chloride channel.Methods A cell-based fluorescence assay was used to determine CFTR-mediate iodide influx rate/dt(mmol?L-1?s-1)] activated by baicalein(the concentrations were 0.18,0.55,1.65,5,15,44,133 and 400 ?mol?L-1).Results The Ka of flavonoid baicalein stimulating CFTR was about 16 ?mol?L-1.The half of maximal activity was reached in ten minutes and the activation disappeared in 20 min after baicalein was washed out.The activation of baicalein was not affected obviously under different concentrations of Forsklin(0,20,50 and 100 nmol?L-1)and the activation could be totally inhibited by CFTRinh-172.Conclusion Baicalein can stimulate CFTR-mediated iodide influx in a dose-dependent way and its activity manifests a rapid and reversible characteristic.It might work in both elevating CFTR protein phosphorylation and direct binding way.