Effects of flavonoids and their glycosides on the uptake of [14C]PAH in both OAT1-expressing and OAT1-negative LLC-PK1 cells
The uptake of [14C]PAH (0.5 μM) in both OAT1-expressing and OAT1-negative LLC-PK1 cells in the absence or presence of flavonoids (50 μM) was performed as described in Materials and Methods. Probenecid (200 μM) was used as a positive control. The uptake of [14C]PAH is expressed as the percentage of control (uptake in OAT1-negative cells). The data are expressed as mean ± S.D. The values in the “Change in Mean” columns represent the percentage of decrease or increase in means relative to the control value for either OAT1-expressing or OAT1-negative cells.
| Flavonoids | Chemical Structure | ||||
|---|---|---|---|---|---|
| OAT1-Expressing Cells | OAT1-Negative Cells | ||||
| Mean ± S.D. | Change in Mean | Mean ± S.D. | Change in Mean | ||
| Percentage | |||||
| Control | 1432 ± 119 | 100 ± 3.31 | |||
| Probenecid | 75.5 ± 4.29*** | −94.7% | 92.3 ± 7.96 | −7.72% | |
| Diosmetin |  | 396 ± 7.69*** | −72.3% | 107 ± 12.7 | +6.64% |
| Diosmin |  | 2525 ± 104*** | +76.4% | 139 ± 4.92* | +38.8% |
| EGC |  | 1276 ± 57.3 | −10.9% | 94.1 ± 13.3 | −5.95% |
| EGCG |  | 1478 ± 77.9 | +3.28% | 108 ± 25.1 | +8.16% |
| Genistein |  | 684 ± 64.1*** | −52.2% | 131 ± 1.70* | +31.4% |
| Genistin |  | 1474 ± 169 | +3.00% | 129 ± 29.0 | +28.5% |
| Quercetin |  | 198 ± 17.6*** | −86.2% | 124 ± 13.2 | +22.3% |
| Rutin |  | 1237 ± 57.5 | −13.6% | 87.0 ± 1.25 | −13.7% |
| Phloretin |  | 1232 ± 264 | −13.9% | 122 ± 6.26 | +23.9% |
| Phloridzin |  | 1172 ± 94.4* | −18.1% | 114 ± 1.7 | +13.0% |
↵* P < 0.05; ***P < 0.001 versus the control of either OAT1-expressing or OAT1-negative cells.