Parameters | 10-day | 22-day | ||||
---|---|---|---|---|---|---|
CON | HFD | DM | CON | HFD | DM | |
Intestinal transport | ||||||
REOatp1a5a | 1.00 | 0.86 ± 0.13 | 0.38 ± 0.13 | 1.00 | 1.48 ± 0.24 | 0.54 ± 0.20 |
REg P-pa | 1.00 | 0.79 ± 0.12 | 0.40 ± 0.13 | 1.00 | 0.76 ± 0.20 | 0.46 ± 0.21 |
REBcrpa | 1.00 | 0.98 ± 0.12 | 0.33 ± 0.14 | 1.00 | 1.21 ± 0.20 | 1.45 ± 0.21 |
Peff,Pas (×10−3cm/min) | 11.95 | 11.95 | 11.95 | 12.02 | 12.02 | 12.02 |
Peff,Oatp1a5 (×10−3cm/min)b | 0.80 | 0.69 ± 0.10 | 0.30 ± 0.10 | 0.77 | 1.14 ± 0.18 | 0.42 ± 0.15 |
Peff,P-gp (×10−3cm/min)b | 2.15 | 1.70 ± 0.26 | 0.86 ± 0.26 | 2.18 | 1.66 ± 0.44 | 1.00 ± 0.46 |
Peff,Bcrp (×10−3cm/min)b | 6.65 | 6.52 ± 0.79 | 2.19 ± 0.93 | 6.68 | 8.08 ± 1.34 | 9.69 ± 1.40 |
Pred Peff (×10−3cm/min)c | — | 4.42 ± 1.21 | 9.20 ± 1.32 | — | 3.42 ± 1.35 | 1.75 ± 1.37 |
Obs Peff (×10−3cm/min)d | 3.95 ± 0.67 | 4.81 ± 0.46 | 7.16**,##±0.72 | 3.92 ± 0.77 | 5.34 ± 0.83 | 1.53**,##±0.82 |
Hepatic uptake | ||||||
REOatp1b2a | 1 | 1.51 ± 0.20 | 1.97 ± 0.26 | 1 | 1.07 ± 0.25 | 1.93 ± 0.23 |
CLup,int,Pas (μl/min per 106 cells) | 5.69 | 5.69 | 5.69 | 6.13 | 6.13 | 6.13 |
Pred CLup,int, Oatp1b2 (μl/min per 106 cells)b | 58.42 | 87.63 ± 11.68 | 115.09 ± 15.19 | 82.13 | 87.88 ± 20.53 | 158.51 ± 18.89 |
Pred CLup,int (μl/min per 106 cells)e | — | 93.32 ± 11.71 | 120.78 ± 16.11 | — | 94.01 ± 21.32 | 164.64 ± 22.13 |
Obs CLup,int (μl/min per 106 cells)d | 64.12 ± 2.84 | 117.9 ± 4.29** | 150.28 ± 3.52**,## | 88.37 ± 2.98 | 127.82 ± 2.28** | 148.84 ± 9.37**,## |
↵a Pred, predicted; RE, relatve expression of protein to CON rats.
↵b Peff,i (/or CLup,i) = Peff,i (/or CLup,i) in normal rats × RE.
↵c Pred Peff = Peff,Pas + Peff,Oatp1a5 − Peff,P-gp − Peff,Bcrp.
↵d Data are expressed as mean ± S.D. (n = 5) of CON, HFD, and DM rats.
↵e Pred CLup,int = CLup,int,Pas + CLup,int,Oatp1b2.
↵* P < 0.05; **P < 0.01 vs. CON rats; #P < 0.05; ##P < 0.01 vs. HFD rats.