TABLE 2

Effects of flavonoids and their glycosides 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.
(Percentage Change in Mean)
Mean ± S.D.
(Percentage Change in Mean)
Control 379 ± 49.3 100 ± 7.03
Rifampin 141 ± 16.1** (-62.9) 106 ± 8.16 (+5.75)
Daidzein 395 ± 109 (+4.34) 99.3 ± 6.27 (-0.67)
Daidzin 368 ± 38.1 (-2.94) 97.7 ± 8.48 (-2.34)
Diosmetin 301 ± 26.7* (-20.6) 159 ± 7.31** (+59.1)
Diosmin 374 ± 88.4 (-1.36) 106 ± 7.99 (+5.57)
EGC 354 ± 15.0 (-6.70) 83.9 ± 7.35** (-16.1)
EGCG 186 ± 24.6** (-51.0) 82.4 ± 6.39** (-17.6)
Genistein 146 ± 8.05** (-61.6) 99.5 ± 5.23 (-0.50)
Genistin 398 ± 13.9 (+4.88) 87.2 ± 4.62* (-12.8)
Hesperitin 292 ± 22.5** (-22.9) 127 ± 6.67** (+27.5)
Hesperidin 288 ± 16.2** (-24.0) 94.3 ± 5.53 (-5.67)
Naringenin 178 ± 17.9** (-53.1) 126 ± 9.23** (+26.0)
Naringin 167 ± 6.94** (-55.9) 90.7 ± 6.69 (-9.23)
Phloretin 230 ± 14.9** (-39.3) 90.7 ± 9.09 (-9.27)
Phloridzin 203 ± 17.0** (-46.6) 103 ± 18.7 (+3.23)
Quercetin 334 ± 28.4 (-11.8) 96.2 ± 5.77 (-3.85)
Rutin
686 ± 52.7**
(+81.1)
105 ± 12.5
(+5.24)