Table 3.
Summary of in vitro, in situ, and in vivo experiments describing genistein-sulfate as a substrate of BCRP/Bcrp.
| Experiment type | Model | Genistein concentration | Detection Method | Time | BCRP Inhibitor | References |
|---|---|---|---|---|---|---|
| In Vitro | ||||||
|
| ||||||
| Transcellular transport | Caco-2 | 2–10 μM | UPLC-MS/MS | 4 h | 5 μM Ko143 | [73] |
|
| ||||||
| Vesicle uptake | Sf9-BCRP vesicles | Chow (Amount unknown; mouse urine) | HPLC/MS | 40 s | - | [98] |
| Sf9-BCRP vesicles | 35S-genistein-sulfate | LSC | 40 s | - | [98] | |
|
| ||||||
| In Situ Intestinal Perfusion | ||||||
|
| ||||||
| SI and colon excretion | FVB Bcrp −/− mice | 10 μM | UPLC-DAD-MS/MS | 120 min | - | [72] |
| Biliary excretion | FVB Bcrp −/− mice | 10 μM | UPLC-MS/MS | 2.5 h | - | [73] |
|
| ||||||
| In Vivo Pharmacokinetics | ||||||
|
| ||||||
| Oral (p.o.) | ||||||
|
| ||||||
| Plasma | FVB Bcrp −/− mice | 50 mg/kg | HPLC-DAD-MS/MS | 3 h | - | [70] |
| FVB Bcrp −/− mice | 2–20 mg/kg | UPLC-MS/MS | 24 h | - | [73] | |
| FVB Bcrp −/− mice | Chow (Amount unknown) | HPLC/MS | - | - | [98] | |
|
| ||||||
| Intraperitoneal (i.p.) | ||||||
|
| ||||||
| Plasma | FVB Bcrp −/− mice | 20 mg/kg | UPLC/MS/MS | 24 h | - | [73] |