Table 1. ER affinity, antioxidant potency, plasma protein binding, and selected physicochemical properties of E2 and DHED.

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.

CompoundER binding IC50 (nM)Inhibition of lipid peroxidation: IC50 (μM)Binding to human plasma proteins (%)Lipophilicity (logPcalc)Intrinsic water solubility at 25°C (μg/ml)
ERαERβFTCTBARS
E21.30.711.8 ± 1.63.9 ± 0.497.8 ± 0.34.014.2 ± 0.3
DHED>10,000>10,000n.i.n.i.58.0 ± 0.61.6760.3 ± 1.7