Pharmacokinetics of Equol, a Soy Isoflavone Metabolite, Changes with the Form of Equol (Dietary versus Intestinal Production) in Ovariectomized Rats

Abstract

Recent findings indicate that soy isoflavones and their metabolites may play a role in mitigating postmenopausal bone loss. Equol, a metabolite of the soy isoflavone daidzein produced by intestinal bacteria, has shown some potential, but only 30–50% of the U.S. population is capable of converting dietary daidzein to equol. There are limited data on the pharmacokinetics of dietary racemic equol and its metabolites. This study was conducted to assess the levels of equol and its conjugates in plasma for a 24 h period resulting from oral administration of dietary daidzein and racemic equol in ovariectomized Sprague–Dawley rats. Plasma samples were analyzed for conjugated and free forms of equol using LC-MS/MS. The maximum plasma concentration (Cmax) and time to reach it (tmax) for total equol (conjugated and unconjugated) were 8815 ± 2988 nmol/L and 2.17 ± 2.91 h and 3682 ± 2675 nmol/L and 20.67 ± 4.67 h, for dietary equol and daidzein, respectively. Although the majority of equol metabolites present were glucuronide conjugates (≥99%), there were low levels of equol monosulfate present. The changes in equol metabolism, specifically equol conjugates, due to the form of equol may play a role in the potential health benefits of equol.