Lipid peroxidation was determined using the FTC (ferric thiocyanate) and TBARS (thiobarbituric acid reactive substances) assays. LogP denotes the logarithm of n-octanol/water partition coefficient as a measure of lipophilicity with values predicted by the method incorporated into the BioMedCAChe program (version 6.1). Data are averages ± SEM (n = 3). n.i., no inhibition. IC50, median inhibitory concentration.
Compound | ER binding IC50 (nM) | Inhibition of lipid peroxidation: IC50 (μM) | Binding to human plasma proteins (%) | Lipophilicity (logPcalc) | Intrinsic water solubility at 25°C (μg/ml) | ||
ERα | ERβ | FTC | TBARS | ||||
E2 | 1.3 | 0.7 | 11.8 ± 1.6 | 3.9 ± 0.4 | 97.8 ± 0.3 | 4.01 | 4.2 ± 0.3 |
DHED | >10,000 | >10,000 | n.i. | n.i. | 58.0 ± 0.6 | 1.67 | 60.3 ± 1.7 |