Long-term kinetics of daidzein and its main metabolites in human equol-producers after soymilk intake: identification of equol-conjugates by UPLC-orbitrap-MS and influence of the number of transforming bacteria on plasma kinetics

Abstract

The main aim of the study was to establish in vivo a correlation between equol (EQU) production and a number of intestinal bacteria able to perform the transformation. Thus, healthy female volunteers were selected for their ability to convert slowly (n = 6, 10⁵-10⁹ cells/g wet feces) or quickly (n = 6, 10¹⁰-10¹² cells/g wet feces) daidzein (DAI) in EQU. After oral administration of 100 mg DAI in soymilk, plasma (0-99 h) and urine (0-96 h) samples were collected. DAI and its metabolites were determined by LC-MS/MS and EQU -conjugates by UPLC-High Resolution-MS. Only for EQU a direct correlation was found between the number of transforming microorganisms and parameters such as t_max and t_1/2 (p = 0.027). Peak serum concentration time, C_max, AUC_{0-72 h} and t_1/2 for total EQU (n = 12) were 36 ± 10 h, 89 ± 78 nM, 2.4 ± 1.7 (μmol × h/L) and 15.6 ± 3.3 h, respectively. In plasma and urine EQU was found mainly as 7-O-glucuronide.

Keywords: Daidzein; equol; human; mass spectrometry; metabolism; pharmacokinetics.