Uptake and metabolism of enterolactone and enterodiol by human colon epithelial cells

Jansen, Guus H E, Arts, Ilja C W, Nielen, Michel W F, Müller, Michael, Hollman, Peter C H and Keijer, Jaap (2005) Uptake and metabolism of enterolactone and enterodiol by human colon epithelial cells. Archives of Biochemistry and Biophysics, 435 (1). pp. 74-82. ISSN 0003-9861

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Abstract

The enterolignans enterolactone and enterodiol are phytoestrogens that are formed from plant lignans by microorganisms in the human colon. Enterolignans circulate in plasma as conjugates. We hypothesized that conjugation of enterolignans takes place in colon epithelial cells, and studied the time course of uptake and metabolism of enterolactone and enterodiol in three human colon epithelial cell lines. In addition, the conjugates were identified by mass spectrometry with accurate mass measurement (LC/QTOFMS/MS). Intracellular levels of conjugated enterolactone and enterodiol in HT29 cells rose immediately after starting the exposure. This was accompanied by a rapid decrease in free enterolactone and enterodiol in the exposure medium of HT29 and (un)differentiated CaCo-2 but not of CCD841CoTr cells. Conjugation and excretion of enterolactone and enterodiol was complete within 8 h, except for enterodiol in CaCo-2 cells ( approximately 48 h). Enterolactone appears to be more rapidly metabolized and/or excreted than enterodiol, and also the appearance of conjugated enterolactone in medium is less affected by the presence of enterodiol than vice versa. Total (free plus conjugated) enterolignan concentrations remained constant throughout the experiments. Three conjugates were identified in exposure medium of HT29 cells: enterolactone-sulfate, enterolactone-glucuronide, and enterodiol-glucuronide. Taken together, our data suggest that phase II metabolism of enterolactone and enterodiol already may take place during uptake in the colon and that colon epithelial cells may be responsible for this metabolism.

Item Type: Article
Uncontrolled Keywords: 4-butyrolactone,caco-2 cells,cell line,colon,ht29 cells,humans,intestinal mucosa,lignans,metabolic clearance rate
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Depositing User: Pure Connector
Date Deposited: 07 Jul 2014 12:04
Last Modified: 21 Apr 2020 22:53
URI: https://ueaeprints.uea.ac.uk/id/eprint/47738
DOI: 10.1016/j.abb.2004.12.015

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