Table 1.
Effective concentration (EC50 in nM), IC50 in nM), relative estrogenic potency (REP) and maximal activity (%) of 17β-E2, 16α-LE2, BPA and the bisphenol analogues on the zfERs.
| zfERα | zfERβ1 | zfERβ2 | ||||
|---|---|---|---|---|---|---|
| Basal activity | 18.8 ± 0.3 | 16.5 ± 0.7 | 20.2 ± 0.6 | |||
| Agonism | ||||||
| Ligand | EC50 (REP) | Maximal activity | EC50 | Maximal activity | EC50 | Maximal activity |
| E2 | 0.08 ± 0.03 (1) | 100 | 0.04 ± 0.01 (1) | 100 | 0.12 ± 0.03 (1) | 100 |
| 16α-LE2 | 0.65 ± 0.1 (1.2 10−1) | 100 | 271 ± 45 (1.5 10−4) | 100 | 69.5 ± 17.5 (1.7 10−3) | 100 |
| BPA | 469 ± 42 (1.7 10−4) | 79 | 3326 ± 381 (1.2 10−5) | 53.1 | 2800 ± 562 (4.3 10−5) | 56.1 |
| BPAF | 84 ± 27 (9.5 10−4) | 89.3 | 758 ± 131 (5.3 10−5) | 89.6 | 897 ± 268 (1.3 10−4) | 79.6 |
| BPC | 25 ± 7.5 (3.2 10−3) | 31 | 316 ± 110 (1.3 10−4) | 36.1 | 167 ± 72 (7.2 10−4) | 58.5 |
| Antagonism | ||||||
| IC50 | IC50 | IC50 | ||||
| BPC | 46 ± 6.4 | 160 ± 42 | 136 ± 75 | |||
Values are the mean ± standard deviations from three separate experiments. Maximal activity is expressed as percentage of luciferase activity induced by 10 nM E2. REPs were determined as the ratio of E2 EC50 to that of bisphenol.