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Immunochemical identification of UGT isoforms in human small bowel and in caco-2 cell monolayers.

Abstract：

:Previous work had suggested the presence of significant levels of UDP-glucuronosyltransferase 1A1 (UGT1A1) catalytic activity in human small intestinal microsomes, with undetectable to low UGT1A6 and 2B7 activities. To confirm the presence of UGT1A1 isoform in human small bowel, to explore the possible absence of UGT1A6 and 2B7 in the organ, and to examine induced Caco-2 cells as a potential model for human intestinal metabolism, Western blot analysis was performed using specific antibodies to the relevant UGT isoforms. Significant expression of UGT1A1 protein was observed in all samples of human small intestinal microsomes, while UGT1A6 expression was undetectable to faint and UGT2B7 immunoreactivity was faint to detectable. Caco-2 cells treated with typical enzyme-inducing agents resulted in low UGT2B7 expression but failed to mimic the UGT1A1 levels found in human small bowel. Further work needs to be performed to develop a comprehensive in vitro model for human small intestinal first-pass metabolism.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Paine MF,Fisher MB

doi

10.1006/bbrc.2000.3064

subject

Has Abstract

pub_date

2000-07-14 00:00:00

pages

1053-7

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(00)93064-X

journal_volume

273

pub_type

杂志文章

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