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Vol. 28, Issue 10, 1210-1216, October 2000
Departments of Biochemistry and Molecular Biology (P.J.C., J.M.L.,
A.R.-P.), Surgery (G.W.B.), and Internal Medicine (J.-P.R.),
University of Arkansas for Medical Sciences, Little Rock, Arkansas
We have recently shown that, in human intestine, glucuronidation of
androsterone and testosterone was on the nanomolar level and increased
from proximal to distal intestine. In the present study, we have
characterized estrogen UDP-glucuronosyltransferase activity in
microsomes from intestine of seven human subjects. Intestinal
microsomes from all segments of intestine from both males and females
(except for one male) glucuronidated estrone (0.2-2.6 nmol/mg × min) and estradiol (0.5-3.1 nmol/mg × min) at levels 2 to 15 times higher than found with human liver microsomes (0.04-0.1 and
0.16-0.25 nmol/mg × min, for estrone and estradiol, respectively). Only with estriol were there significant hepatic glucuronidation (2.2-4.5 nmol/mg × min) and intestinal
glucuronidation activities (0.2-2.2 nmol/mg × min) that were
lower than those in liver. All-trans-retinoic acid was
glucuronidated by all segments of intestine from both sexes at levels
50 to 80% of those found with human liver but quite low compared with
estrogen glucuronidation. In the two subjects for whom stomach was
available, there was no measurable activity in stomach microsomes
toward any of the substrates. UGT2B RNA expression was examined in
mucosa from stomach to colon from two subjects. There was significant
expression of UGT2B7, but not of UGT2B4 or UGT2B15, in all segments of
intestine. To our knowledge, this is the first direct demonstration of
glucuronidation of estrogens by human intestinal microsomes. Thus, in
humans, the intestine may be considered as part of the overall
mechanism of detoxification via glucuronidation.
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