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Vol. 30, Issue 5, 531-533, May 2002
Department of Biochemistry and Molecular Biology, University of
Arkansas for Medical Sciences, Little Rock, Arkansas
Linoleic acid has recently been shown to be glucuronidated
in vitro by human liver and intestinal microsomes and recombinant UGT2B7. In the present study, the dietary fatty acids (FA), phytanic acid (PA), and docosahexaenoic acid (DHA) have been used as substrates for human UDP-glucuronosyltransferases (UGTs). Both compounds were
effectively glucuronidated by human liver microsomes (HLM; 1.25 ± 0.36 and 1.12 ± 0.32 nmol/mg × min for PA and DHA,
respectively) and UGT2B7 (0.71 and 0.53 nmol/mg × min). Kinetic
analysis produced relatively low Km values
for PA with both HLM and UGT2B7 (149 and 108 µM, respectively). The
Km for DHA glucuronidation by HLM (460 µM)
was considerably higher than that for UGT2B7 (168 µM), suggesting the
involvement in microsomes of other UGT isoforms in addition to UGT2B7.
Glucuronidation of PA and DHA by gastrointestinal microsomes from 16 human subjects was determined. In general, both PA and DHA were
glucuronidated by gastric and intestinal microsomes, and activity
toward both substrates was lowest in the stomach, increased in the
small intestine, and lower in the colon. However, there were large
interindividual variations in UGT activity toward both substrates in
all segments of the intestine, as has been seen with other substrates.
Thus, PA and DHA are effective in vitro substrates for human liver,
gastric and intestinal microsomes, and glucuronidation may play a role
in modulating the availability of these FA as ligands for nuclear receptors.
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