Table 2.
Binding affinity of the coregulator SRC3 to ERα and ERβ complexes with E2 and BEs expressed as RCA values
BE | ERα |
ERβ |
β/α | ||
---|---|---|---|---|---|
EC50 (nM) | RCA | EC50 (nM) | RCA | ||
E2 | 0.13 ± 0.004 | [100] | 0.12 ± 0.002 | [100] | [1.0] |
Genistein | 1.1 ± 0.1 | 11.30 ± 0.7 | 0.20 ± 0.01 | 61 ± 0.9 | 5.4 |
Daidzein | 14.2 ± 1.1 | 0.88 ± 0.05 | 0.22 ± 0.02 | 54.4 ± 2.1 | 61.8 |
S-equol | 16.7 ± 0.6 | 0.73 ± 0.01 | 0.18 ± 0.01 | 78.5 ± 4.2 | 108.0 |
R-equol | 33.9 ± 1.8 | 0.36 ± 0.008 | 0.33 ± 0.1 | 43 ± 2.1 | 119.0 |
(±)-Equol | 25.9 ± 4.2 | 0.47 ± 0.02 | 0.25 ± 0.11 | 56 ± 4.2 | 119.0 |
Biochanin A | 88.8 ± 6.4 | 0.14 ± 0.02 | 0.26 ± 0.01 | 46.7 ± 1.5 | 334.0 |
Formononetin | ND | ND | 0.53 ± 0.02 | 22.9 ± 1.7 | — |
Liquiritigenin | 2.2 ± 0.4 | 4.60 ± 0.5 | 0.13 ± 0.01 | 88.9 ± 6.7 | 19.3 |
RCA = (EC50 E2/EC50 BE) × 100. β/α = RCAERβ/RCAERα. ND, not detectable.