Transport of salvianolic acid B via the human organic anion transporter 1B1 in the liver.

Salvianolic acid B (SAB) has a high concentration in the liver, but the mechanism of its distribution in the liver is unclear. The aim of this study was to investigate the mechanisms of hepatic uptake of SAB. In this study, we first explored the uptake features of SAB in HepG2 cells and the effect of rifampicin on uptake. Then, we explored the effects of SAB on the uptake of pitavastatin in HepG2 cells. Finally, we established an HEK239T-OATP1B1 cell model to confirm whether OATP1B1 mediated the transport of SAB. Results showed that the uptake kinetic parameters Vmax and Km for SAB in HepG2 cells were 21.28 ± 2.06 pmol mg-1 per protein min-1 and 28.47 ± 7.36 μM, respectively. Rifampicin inhibited the uptake of SAB in HepG2 cells (IC50 was 5.85 ± 1.70 μM), and SAB affected the uptake of pitavastatin in HepG2 cells (IC50 was 27.67 ± 1.90 μM). The uptake kinetic parameters Vmax and Km for SAB in HEK239T-OATP1B1 were 60.03 ± 6.16 pmol mg-1 per protein min-1 and 87.24 ± 15.28 μM, respectively, whereas in EGFP-HEK293 cells were 14.04 ± 2.53 pmol mg-1 per protein min-1 and 56.53 ± 15.50 μM. The SAB had no effect of on the expression of OATP1B1 in HEK239T-OATP1B1 cells. In conclusion, this study demonstrated that OATP1B1 contributes to the transport and accumulation of SAB in the liver.