Biliary excretion characteristics of berberine, palmatine and jateorhizine in sandwich-cultured rat hepatocytes / 中国药理学通报

ABSTRACT

Aim To study the biliary excretion characteristics of berberine,palmatine and jateorhizine in rat hepatocytes.Methods Berberine,palmatine and jateorhizine were incubated with the sandwich-cultured rat hepatocytes (SCRH) in standard Ca2+ buffer or Ca2+ free buffer.The accumulation of the three compounds under different conditions were measured by UPLC-MS/MS.The biliary excretion index and biliary clearance were calculated,and the effect of P-gp or Mrp2 inhibitor on the transport of three compounds was also investigated.Results While the incubation time increased,the accumulation of the three compounds also increased.There were obvious differences in accumulation of berberine,palmatine and jateorhizine in incubations treated with standard buffer and calcium-free buffer.The P-gp inhibitors ciclosporin A and verapamil could inhibit the biliary excretion of berberine,palmatine and jateorhizine.However,the Mrp2 inhibitors MK571 and probenecid had no effect on biliary excretion of the three compounds.Conclusions The biliary excretion of berberine,palmatine and jateorhizine is mainly through an active process.They are all the P-gp substrates other than Mrp2 substrates.