BACKGROUND: Alkylresorcinols are phenolic compounds that are present almost exclusively in rye and wheat fiber. Alkylresorcinols are absorbed and thereafter metabolized to 3,5-dihydroxybenzoic acid (DHBA) and 3-(3,5-dihydroxyphenyl)-1-propanoic acid (DHPPA), which have been detected in human urine and plasma. OBJECTIVE: The objective was to determine the plasma pharmacokinetics of DHBA and DHPPA in human subjects to estimate whether they show potential as biomarkers for whole-grain rye and/or wheat intake. DESIGN: Fifteen human volunteers followed a low-alkylresorcinol diet for 2 d before ingesting a single dose of high-fiber rye bread containing 100 mg alkylresorcinols [corrected]. Plasma samples were collected for 25 h, and the alkylresorcinol metabolites were quantified by HPLC with coulometric electrode array detection. RESULTS: Maximum concentrations were reached at approximately 6 h for both metabolites, although interindividual variation was found. The half-life was significantly (P < 0.0002) longer for DHPPA (16.3 h) than for DHBA (10.1 h). No significant differences were discovered between women and men in the half-life of each metabolite, which, from a pharmacokinetic point of view, is the most important parameter. The area under the curve differed significantly between DHBA and DHPPA (P < 0.0001) and between women and men (P = 0.03 for DHBA and P = 0.01 for DHPPA). However, when corrected for body weight, the difference between sexes was no longer significant. CONCLUSIONS: Our results suggest that DHBA and DHPPA are both good candidate biomarkers for whole-grain rye and/or wheat intake; however, DHPPA is the better indicator because of its longer half-life. This could provide a practical tool when investigating the association between diet and diseases.
BACKGROUND:Alkylresorcinols are phenolic compounds that are present almost exclusively in rye and wheat fiber. Alkylresorcinols are absorbed and thereafter metabolized to 3,5-dihydroxybenzoic acid (DHBA) and 3-(3,5-dihydroxyphenyl)-1-propanoic acid (DHPPA), which have been detected in human urine and plasma. OBJECTIVE: The objective was to determine the plasma pharmacokinetics of DHBA and DHPPA in human subjects to estimate whether they show potential as biomarkers for whole-grain rye and/or wheat intake. DESIGN: Fifteen human volunteers followed a low-alkylresorcinol diet for 2 d before ingesting a single dose of high-fiber rye bread containing 100 mg alkylresorcinols [corrected]. Plasma samples were collected for 25 h, and the alkylresorcinol metabolites were quantified by HPLC with coulometric electrode array detection. RESULTS: Maximum concentrations were reached at approximately 6 h for both metabolites, although interindividual variation was found. The half-life was significantly (P < 0.0002) longer for DHPPA (16.3 h) than for DHBA (10.1 h). No significant differences were discovered between women and men in the half-life of each metabolite, which, from a pharmacokinetic point of view, is the most important parameter. The area under the curve differed significantly between DHBA and DHPPA (P < 0.0001) and between women and men (P = 0.03 for DHBA and P = 0.01 for DHPPA). However, when corrected for body weight, the difference between sexes was no longer significant. CONCLUSIONS: Our results suggest that DHBA and DHPPA are both good candidate biomarkers for whole-grain rye and/or wheat intake; however, DHPPA is the better indicator because of its longer half-life. This could provide a practical tool when investigating the association between diet and diseases.
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