Table 1.
Compounds | ERα | ERβ | RBA β/α | ||
---|---|---|---|---|---|
% RBAb | % RREc | % RBAb | % RREc | ||
17β-Estradiol | 100 | 100 | 100 | 100 | --- |
Flavanones, Flavones | |||||
8-PN | 30 | 94.7 | 9 | 51.2 | 0.3 |
8-PA | 18 | 43.2 | 48 | 47.2 | 2.7 |
NRG | <0.002 | 12.6 | 0.05 | 23.0 | --- |
API | <0.002 | 15.4 | 0.6 | 32.8 | --- |
Flavonols | |||||
DMI | <0.002 | 9.1 | 0.5 | 16.6 | --- |
ICT | <0.002 | 10.2 | <0.002 | 11.9 | --- |
KFL | <0.002 | 31.1 | 0.2 | 18.8 | --- |
Isoflavonoids | |||||
GEN | 5.6 | 62.7 | 19.4 | 50.2 | 3.5 |
DGN | <0.002 | 25.1 | 14 | 38.7 | --- |
8-PG | <0.002 | 33.5 | 0.9 | 17.2 | --- |
Values are expressed as the mean of at least three independent analytical determinations in triplicate. Method details for the ERα and ERβ competitive binding assay and for the (TR-FRET) assay are described in the Experimental Section.
% relative binding affinity (RBA)= (IC50 E2/ IC50 (iso)flavonoid))*100,
% relative recruitment efficacy (RRE) = (max FRET efficacy (iso)flavonoid) / max FRET efficacy E2)*100, E2 arbitrarily set at 100%.