Consumption of Roasted Coffee Leads to Conjugated Metabolites of Atractyligenin in Human Plasma

Roasted coffee contains atractyligenin-2-O-β-d-glucoside and 3′-O-β-d-glucosyl-2′-O-isovaleryl-2-O-β-d-glucosylatractyligenin, which are ingested with the brew. Known metabolites are atractyligenin, atractyligenin-19-O-β-d-glucuronide (M1), 2β-hydroxy-15-oxoatractylan-4α-carboxy-19-O-β-d-glucuronide (M2), and 2β-hydroxy-15-oxoatractylan-4α-carboxylic acid-2-O-β-d-glucuronide (M3), but the appearance and pharmacokinetic properties are unknown. Therefore, first time-resolved quantitative data of atractyligenin glycosides and their metabolites in plasma samples from a pilot human intervention study (n = 10) were acquired. None of the compounds were found in the control samples and before coffee consumption (t = 0 h). After coffee, neither of the atractyligenin glycosides appeared in the plasma, but the aglycone atractyligenin and the conjugated metabolite M1 reached an estimated cmax of 41.9 ± 12.5 and 25.1 ± 4.9 nM, respectively, after 1 h. M2 and M3 were not quantifiable until their concentration enormously increased ≥4 h after coffee consumption, reaching an estimated cmax of 2.5 ± 1.9 and 55.0 ± 57.7 nM at t = 10 h. The data suggest that metabolites of atractyligenin could be exploited to indicate coffee consumption. © 2023 The Authors. Published by American Chemical Society.