Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Drug Metabolism & Disposition
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Drug Metabolism & Disposition

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Visit dmd on Facebook
  • Follow dmd on Twitter
  • Follow ASPET on LinkedIn
Research ArticleArticle

Glucuronidation of Estrogens and Retinoic Acid and Expression of UDP-Glucuronosyltransferase 2B7 in Human Intestinal Mucosa

Piotr J. Czernik, Joanna M. Little, Gary W. Barone, Jean-Pierre Raufman and Anna Radominska-Pandya
Drug Metabolism and Disposition October 2000, 28 (10) 1210-1216;
Piotr J. Czernik
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Joanna M. Little
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Gary W. Barone
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Jean-Pierre Raufman
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Anna Radominska-Pandya
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

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.

Footnotes

  • Send reprint requests to: Anna Radominska-Pandya, Ph.D., University of Arkansas for Medical Sciences, Department of Biochemistry and Molecular Biology, 4301 W. Markham, Slot 516, Little Rock, AR 72205. E-mail: radominskaanna{at}exchange.uams.edu

  • This work was supported in part by National Institutes of Health Grants DK49715 and DK51971 to A.R.-P.

  • Abbreviations used are::
    UGTs
    UDP-glucuronosyltransferases
    E1
    estrone
    E2
    estradiol
    E3
    estriol
    UDP-GlcUA
    UDP-glucuronic acid
    E2-3G
    estradiol-3-O(β-d-glucuronide)
    E2-17G
    estradiol-17-O(β-d-glucuronide)
    E3-3G
    estriol-3-O(β-d-glucuronide)
    E3-16G
    estriol-16-O(β-d-glucuronide)
    E3-17G
    estriol-17-O(β-d-glucuronide)
    A
    androsterone
    T
    testosterone
    atRA
    all-trans-retinoic acid
    • Received October 18, 1999.
    • Accepted July 6, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

 

DMD articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Drug Metabolism and Disposition: 28 (10)
Drug Metabolism and Disposition
Vol. 28, Issue 10
1 Oct 2000
  • Table of Contents
  • About the Cover
  • Index by author
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Drug Metabolism & Disposition article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Glucuronidation of Estrogens and Retinoic Acid and Expression of UDP-Glucuronosyltransferase 2B7 in Human Intestinal Mucosa
(Your Name) has forwarded a page to you from Drug Metabolism & Disposition
(Your Name) thought you would be interested in this article in Drug Metabolism & Disposition.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Research ArticleArticle

Glucuronidation of Estrogens and Retinoic Acid and Expression of UDP-Glucuronosyltransferase 2B7 in Human Intestinal Mucosa

Piotr J. Czernik, Joanna M. Little, Gary W. Barone, Jean-Pierre Raufman and Anna Radominska-Pandya
Drug Metabolism and Disposition October 1, 2000, 28 (10) 1210-1216;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero

Share
Research ArticleArticle

Glucuronidation of Estrogens and Retinoic Acid and Expression of UDP-Glucuronosyltransferase 2B7 in Human Intestinal Mucosa

Piotr J. Czernik, Joanna M. Little, Gary W. Barone, Jean-Pierre Raufman and Anna Radominska-Pandya
Drug Metabolism and Disposition October 1, 2000, 28 (10) 1210-1216;
del.icio.us logo Digg logo Reddit logo Twitter logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Materials and Methods
    • Results
    • Discussion
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Determination of Acyl-, O-, and N-Glucuronide
  • TMDD Affects PK of IL-10 Fc-fusion Proteins
  • Uptake as the RDS in Pevonedistat Hepatic Clearance
Show more Article

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About DMD
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Journal of Pharmacology and Experimental Therapeutics
  • Molecular Pharmacology
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-009X (Online)

Copyright © 2022 by the American Society for Pharmacology and Experimental Therapeutics