Table 2.
Maximal or minimal activity and EC50 or IC50 of progestins on HG5LN-hPXR and HG5LN-zfPXR.
| Compound | hPXR agonism | zfPXR agonism | zfPXR antagonism | |||
|---|---|---|---|---|---|---|
| EC50 (µM) | Max (%) | EC50 (µM) | Max (%) | IC50 (µM) | Min (%) | |
| DMSO | 19 ± 6 | 28 ± 1.7 | ||||
| Chlormadinone acetate | n.a. | - | n.a. | - | n.a. | - |
| Desogestrel* | 4.2 ± 0.2 | 54 | 0.13 ± 0.01 | 99 | n.a. | - |
| 17α,20β-Dihydroxy-4-pregnen-3-one | n.a. | - | n.a. | - | n.a. | - |
| Drospirenone | 18 ± 1.4 | 44 | n.a. | - | 3.6 ± 0.4 | 52 |
| Dydrogesterone | n.m. | 27 | n.a. | - | n.a. | - |
| Ethisterone | n.a. | - | n.a. | - | n.a. | - |
| Etynodiol diacetate* | n.a. | - | 0.32 ± 0.02 | 92 | n.a. | - |
| Etonogestrel | 24 ± 4.6 | 27 | 2.3 ± 0.2 | 90 | n.a. | - |
| Gestodene* | n.a. | - | 0.18 ± 0.01 | 81 | n.a. | - |
| Gestonorone | n.a. | - | n.a. | - | n.a. | - |
| Levonorgestrel | n.a. | - | 1.4 ± 0.2 | 74 | n.a. | - |
| Lynestrenol* | 41 ± 7.7 | 30 | 0.23 ± 0.01 | 98 | n.a. | - |
| Medroxyprogesterone | 18 ± 2.4 | 50 | n.a. | - | n.a. | - |
| Megestrol acetate | 19 ± 4.3 | 50 | n.a. | - | n.a. | - |
| Mifepristone* | 5.9 ± 0.2 | 39 | n.a. | - | 0.08 ± 0.003 | 10 |
| Nestorone | n.a. | - | n.a. | - | n.a. | - |
| Nomegestrol acetate | n.a. | - | n.a. | - | n.a. | - |
| Norethisterone | n.a. | - | 2.2 ± 0.4 | 54 | n.a. | - |
| Progesterone | 9.1 ± 2.2 | 72 | n.a. | - | 0.64 ± 0.03 | 14 |
| Promegestone | n.a. | - | n.a. | - | n.a. | - |
| Tibolone* | n.a. | - | 0.56 ± 0.04 | 96 | n.a. | - |
n.a., not active; max, maximal activity of the chemicals obtained at 10 µM except for compounds that were not tested above 3 µM because of toxicity*; min, minimal activity of the chemicals obtained at 10 µM except for compounds that were not tested above 3 µM because of toxicity*.
Maximal activities of the chemicals obtained at 10 µM are expressed as a percentage of the maximal induced by 3 µM SR 12813 and 1 µM clotrimazole for HG5LN-hPXR and HG5LN-zfPXR, respectively. Antagonism assays were performed in coexposure with 0.3 µM SR 12813 in HG5LN-hPXR cells and 0.03 µM clotrimazole in HG5LN-zfPXR cells. Minimal activities of the chemicals obtained at 10 µM are expressed as a percentage of the maximal induced by 3 µM SR 12813 and 1 µM clotrimazole for HG5LN-hPXR and HG5LN-zfPXR, respectively.