Net transport ratios of in vitro transports of ginsenosides by various human and rat hepatic transporters
| Hepatic transporter | Positive control (10 μM) | Ppt-type | Ppd-type | ||||
|---|---|---|---|---|---|---|---|
| Ginsenoside Rg1 (50 μM) | Ginsenoside Re (50 μM) | Notoginsenoside R1 (50 μM) | Ginsenoside Rb1 (50 μM) | Ginsenoside Rc (50 μM) | Ginsenoside Rd (50 μM) | ||
| Human hepatic SLC transporters | |||||||
| OATP1B1 | 97.7 ± 7.1 (E217βG) | 1.11 ± 0.02 | 1.20 ± 0.04 | 1.29 ± 0.06 | 1.04 ± 0.12 | 1.02 ± 0.14 | 0.914 ± 0.077 |
| OATP1B3 | 73.2 ± 10.9 (E217βG) | 15.1 ± 0.8 | 107 ± 15 | 37.2 ± 4.1 | 0.921 ± 0.135 | 0.892 ± 0.044 | 0.922 ± 0.006 |
| OATP2B1 | 88.6 ± 5.2 (E1S) | 0.918 ± 0.036 | 0.844 ± 0.021 | 1.02 ± 0.16 | 0.933 ± 0.266 | 1.14 ± 0.06 | 1.03 ± 0.19 |
| Human hepatic ABC transporters | |||||||
| MRP2 | 10.2 ± 0.9 (E217βG) | 10.9 ± 1.8 | 16.8 ± 2.3 | 23.9 ± 3.0 | 1.20 ± 0.20 | 0.921 ± 0.087 | 0.911 ± 0.075 |
| BCRP | 12.1 ± 1.4 (MTX) | 6.81 ± 0.8 | 4.12 ± 1.11 | 6.72 ± 0.22 | 1.51 ± 0.14 | 0.833 ± 0.074 | 1.04 ± 0.15 |
| BSEP | 4.22 ± 0.12 (TCA) | 3.12 ± 0.09 | 5.13 ± 0.45 | 5.31 ± 0.15 | 1.82 ± 0.08 | 0.842 ± 0.050 | 0.907 ± 0.078 |
| MDR1 | 4.67 ± 0.57 (VER) | 5.91 ± 0.17 | 5.99 ± 0.56 | 22.0 ± 1.3 | 1.49 ± 0.07 | 1.40 ± 0.23 | 1.24 ± 0.23 |
| Rat hepatic SLC transporters | |||||||
| Oatp1a1 | 7.61 ± 1.1 (E217βG) | 1.13 ± 0.00 | 1.21 ± 0.02 | 0.614 ± 0.005 | 1.11 ± 0.10 | 1.03 ± 0.01 | 0.916 ± 0.092 |
| Oatp1b2 | 63.0 ± 7.4 (E217βG) | 10.9 ± 1.44 | 9.92 ± 1.19 | 5.50 ± 0.23 | 0.912 ± 0.123 | 1.02 ± 0.03 | 1.17 ± 0.05 |
| Ntcp | 21.9 ± 3.9 (TCA) | 1.21 ± 0.37 | 0.927 ± 0.201 | 0.836 ± 0.023 | 0.813 ± 0.106 | 1.11 ± 0.12 | 1.03 ± 0.26 |
| Rat hepatic ABC transporters | |||||||
| Mrp2 | 13.1 ± 3.2 (E217βG) | 12.5 ± 0.12 | 10.2 ± 2.00 | 19.8 ± 4.1 | 1.21 ± 0.29 | 1.39 ± 0.06 | 1.11 ± 0.04 |
| Bcrp | 43.0 ± 7.6 (MTX) | 4.03 ± 0.32 | 4.01 ± 0.79 | 3.31 ± 0.24 | 1.03 ± 0.07 | 1.41 ± 0.08 | 1.21 ± 0.01 |
| Bsep | 10.5 ± 0.7 (TCA) | 5.91 ± 0.27 | 3.93 ± 0.14 | 4.32 ± 0.67 | 0.923 ± 0.105 | 1.22 ± 0.16 | 1.03 ± 0.00 |
| Mdr1a | 4.23 ± 0.06 (VER) | 1.52 ± 0.12 | 1.32 ± 0.07 | 1.52 ± 0.09 | 0.912 ± 0.012 | 1.20 ± 0.01 | 1.41 ± 0.09 |
| Mdr1b | 3.60 ± 0.04 (VER) | 1.22 ± 0.07 | 1.28 ± 0.04 | 1.28 ± 0.06 | 1.11 ± 0.13 | 0.922 ± 0.065 | 1.03 ± 0.04 |
E217βG, oestradiol-17β-D-glucuronide; E1S, oestrone-3-sulfate; MTX, methotrexate; TCA, taurocholic acid; VER, verapamil. The functions of human MDR1, rat Mdr1a and rat Mdr1b were verified with veripamil by ATPase assay according to the manufacturers' protocols and using the ratio of vesicular transport in the absence of sodium vanadate to that in the presence of sodium vanadate. Values represent the means ± SDs (n = 3). For those with net transport ratios greater than three, the differences between TransportTC and TransportMC or between TransportATP and TransportAMP were statistically significant (P < 0.05).