TABLE 1

Effects of flavonoids on the uptake of [3H]DHEAS in both OATP1B1-expressing and OATP1B1-negative cells

The uptake of [3H]DHEAS (0.5 μM) in both OATP1B1-expressing and OATP1B1-negative cells in the absence or presence of flavonoids (50 μM) was performed as described under Materials and Methods. Rifampicin (100 μM) was used as a positive control. The uptake of [3H]DHEAS was expressed as the percentage of control (uptake in OATP1B1-negative cells in the presence of 0.3% DMSO). The data are expressed as mean ± S.D., n ≥ 6. * p < 0.05, ** p < 0.01 compared with the control of either OATP1B1-expressing or OATP1B1-negative cells. The values in parentheses represent the percentage of decrease or increase in means relative to the control value for either OATP1B1-expressing or OATP1B1-negative cells.



OATP1B1-Expressing Cells

OATP1B1-Negative Cells

Mean ± S.D.
(Perceentage Change in Mean)
Mean ± S.D.
(Percentage Change in Mean)
Control 452 ± 105 100 ± 7.93
Rifampicin 195 ± 78.5** (-56.8) 97.1 ± 10.9 (-2.88)
Apigenin 362 ± 49.8* (-19.8) 193 ± 42.3** (+92.8)
Biochanin A 142 ± 35.0** (-68.6) 90.1 ± 19.6 (-9.95)
Benzoflavone 445 ± 29.3 (-1.53) 112 ± 4.48 (+11.9)
Chrysin 477 ± 77.0 (+5.53) 117 ± 10.6** (+17.5)
Fisetin 197 ± 22.8** (-56.5) 138 ± 13.0** (+37.9)
Galangin 391 ± 19.6 (-13.5) 118 ± 9.49* (+17.8)
Kaempferol 378 ± 68.8 (-16.5) 85.9 ± 3.75 (-14.1)
Luteolin 217 ± 44.6** (-52.0) 118 ± 6.41** (+17.8)
Morin 252 ± 20.0** (-44.2) 87.7 ± 11.8 (-12.3)
Myricetin 305 ± 24.0** (-32.5) 94.0 ± 10.5 (-6.03)
Silibinin 152 ± 15.2** (-66.5) 114 ± 5.70* (+13.9)
Silymarin
140 ± 11.6**
(-68.9)
96.0 ± 12.8
(-3.96)