|
Activation of human and zebrafish PXRs by xenobiotics and vitamins |
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| Cmp. # |
Compound |
hPXR Activity |
hPXR Efficacy |
zfPXR Activity |
zfPXR Efficacy |
Toxicity |
|
|
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| MI1 |
Acetaminophen |
None |
None |
None |
||
| MI2 |
3-Aminobenzoic acid |
None |
None |
None |
||
| MI3 |
Benzo [a]pyren |
4.75 |
0.55 |
4.00 |
0.06 |
100 |
| MI4 |
n-Butyl-4-aminobenzoate |
4.88 |
1.35 |
4.86 |
0.69 |
100 |
| MI5 |
Butylbenzoate |
None |
None |
None |
||
| MI6 |
Caffeine |
None |
None |
None |
||
| MI7 |
Carbamazepine |
4.20 |
0.37 |
None |
200 |
|
| MI8 |
Carbamazepine epoxide |
4.09 |
0.57 |
None |
200 |
|
| MI9 |
β-Carotene |
5.46 |
0.67 |
None |
100 |
|
| MI10 |
Chlorpyrifos |
4.59 |
2.05 |
5.44 |
0.88 |
None |
| MI11 |
Chlorzoxazone |
None |
None |
500 |
||
| MI12 |
Cyclosporine |
None |
None |
20 |
||
| MI13 |
Ecdysone |
None |
None |
None |
||
| MI14 |
Ethyl-2-aminobenzoate |
None |
None |
None |
||
| MI15 |
Flurbiprofen |
4.10 |
1.59 |
4.10 |
0.53 |
None |
| MI16 |
Folic acid |
None |
None |
None |
||
| MI17 |
Guggulsterone |
None |
None |
None |
||
| MI18 |
GW3965 |
None |
None |
10 |
||
| MI19 |
Hyperforin |
7.22 |
1.29 |
None |
50 |
|
| MI20 |
Mevastatin |
5.23 |
0.51 |
None |
15 |
|
| MI21 |
Mycophenolic acid |
None |
None |
None |
||
| MI22 |
Nifedipine |
5.33 |
0.41 |
4.91 |
0.99 |
50 |
| MI23 |
Oxcarbazepine |
4.74 |
0.35 |
~4.70 |
~0.30 |
200 |
| MI24 |
Paclitaxel |
4.92 |
0.13 |
None |
100 |
|
| MI25 |
Phenobarbital |
3.43 |
1.19 |
3.49 |
0.10 |
None |
| MI26 |
Phenytoin |
4.26 |
0.52 |
None |
200 |
|
| MI27 |
n-Propyl-4-hydroxybenzoate |
4.51 |
0.32 |
4.28 |
0.31 |
100 |
| MI28 |
Provitamin D3 |
None |
None |
10 |
||
| MI29 |
Provitamin D2 |
None |
None |
20 |
||
| MI30 |
Reserpine |
4.91 |
0.72 |
None |
50 |
|
| MI31 |
Retinol |
5.80 |
0.20 |
None |
50 |
|
| MI32 |
Rifampicin |
7.00 |
1.00 |
None |
200 |
|
| MI33 |
SR12813 |
6.41 |
0.90 |
None |
10 |
|
| MI34 |
TCDD |
7.17 |
1.78 |
6.32 |
6.17 |
10 |
| MI35 |
TCPOBOP |
5.25 |
0.66 |
None |
200 |
|
| MI36 |
T-0901317 |
7.66 |
1.24 |
None |
100 |
|
| MI37 |
α-Tocopherol |
~4.30 |
~0.25 |
None |
100 |
|
| MI38 |
β-Tocopherol |
4.85 |
0.33 |
None |
100 |
|
| MI39 |
δ-Tocopherol |
5.14 |
0.64 |
None |
100 |
|
| MI40 |
γ-Tocopherol |
None |
None |
100 |
||
| MI41 |
1α,25-Dihydroxyvitamin D3 |
None |
None |
50 |
||
| MI42 |
1α-Hydroxyvitamin D2 |
None |
None |
50 |
||
| MI43 |
1α-Hydroxyvitamin D3 |
None |
None |
50 |
||
| MI44 |
Vitamin K1 |
4.99 |
0.13 |
None |
100 |
|
| MI45 |
Vitamin K2 |
5.04 |
0.80 |
None |
100 |
|
| MI46 |
Vitamin K3 |
~4.30 |
~0.15 |
None |
100 |
|
|
Activities are in -log(EC50), with EC50 in molar units for the activation of human or zebrafish PXR. Efficacy is relative to 10 μM rifampicin (human PXR) or 20 μM 5α-androstan-3α-ol (zebrafish PXR) which are assigned an efficacy of 1.0. Toxicity is the lowest concentration in micromolar that produced significant toxicity in the HepG2 cells. | ||||||
Ekins et al. BMC Evolutionary Biology 2008 8:103 doi:10.1186/1471-2148-8-103 |
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