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
Journal of Pharmacology and Experimental Therapeutics
  • 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
Journal of Pharmacology and Experimental Therapeutics

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 jpet on Facebook
  • Follow jpet on Twitter
  • Follow jpet on LinkedIn
OtherDRUG METABOLISM AND DISPOSITION

A New Interpretation of Salicylic Acid Transport across the Lipid Bilayer: Implications of pH-Dependent but not Carrier-Mediated Absorption from the Gastrointestinal Tract

Masanori Takagi, Yoko Taki, Toshiyasu Sakane, Tanekazu Nadai, Hitoshi Sezaki, Naoto Oku and Shinji Yamashita
Journal of Pharmacology and Experimental Therapeutics June 1998, 285 (3) 1175-1180;
Masanori Takagi
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Yoko Taki
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Toshiyasu Sakane
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Tanekazu Nadai
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hitoshi Sezaki
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Naoto Oku
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Shinji Yamashita
  • 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

Transport of several monocarboxylic acids across the lipid bilayer was examined in liposomes consisting of egg yolk phosphatidylcholine and cholesterol. In the presence of inward proton gradient, salicylic acid (SA) was taken up rapidly by liposomes showing overshoot, saturation and competitive inhibition phenomena. These carrier-mediated like profiles of SA uptake can be explained by assuming a very high permeability through the liposomal membrane of protonated SA. Protonated SA in the extraliposomal solution (pH 5.8) was taken up by liposomes rapidly, followed by a redissociation to anion according to the intraliposomal pH (pH 7.5). The concentration gradient of protonated SA across the liposomal membrane is maintained until the intraliposomal pH decreased to the extraliposomal level, which facilitates the uptake of SA into liposomes. The permeability of the lipid bilayer to several compounds was estimated from the inhibitory effects of those compounds on SA uptake by liposomes. Good linear relationships were observed between their inhibitory effects on the liposomal uptake of SA and the permeability of the intestinal membrane to them determined both in vivo and in vitro. These results clearly indicate that the carrier-independent transport mechanism of monocarboxylic acids observed in liposomes significantly contributes to their absorption from the intestinal tract under physiological conditions.

Footnotes

  • Send reprint requests to: Shinji Yamashita, Ph.D., Faculty of Pharmaceutical Sciences, Setsunan University, 45–1 Nagaotoge-cho, Hirakata, Osaka 573–01, Japan.

  • Abbreviations:
    SA
    salicylic acid
    14C-SA
    radiolabeled salicylic acid
    BBMVs
    brush-border membrane vesicles
    MCT1
    proton/monocarboxylate cotransporter
    egg-PC
    egg yolk phosphatidylcholine
    MLV
    multilamellar large liposome
    TM
    transport medium
    [pH]out
    extraliposomal pH
    [pH]in
    intraliposomal pH
    Mes
    2-morpholinoethanesulfonic acid
    Hepes
    N-(2-hydroxyethyl)piperazine-N′-ethanesulfonic acid
    FITC
    fluorescein isothiocyanate
    • Received October 6, 1997.
    • Accepted February 24, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

JPET 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

Journal of Pharmacology and Experimental Therapeutics
Vol. 285, Issue 3
1 Jun 1998
  • Table of Contents
  • Index by author
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics 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.
A New Interpretation of Salicylic Acid Transport across the Lipid Bilayer: Implications of pH-Dependent but not Carrier-Mediated Absorption from the Gastrointestinal Tract
(Your Name) has forwarded a page to you from Journal of Pharmacology and Experimental Therapeutics
(Your Name) thought you would be interested in this article in Journal of Pharmacology and Experimental Therapeutics.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
OtherDRUG METABOLISM AND DISPOSITION

A New Interpretation of Salicylic Acid Transport across the Lipid Bilayer: Implications of pH-Dependent but not Carrier-Mediated Absorption from the Gastrointestinal Tract

Masanori Takagi, Yoko Taki, Toshiyasu Sakane, Tanekazu Nadai, Hitoshi Sezaki, Naoto Oku and Shinji Yamashita
Journal of Pharmacology and Experimental Therapeutics June 1, 1998, 285 (3) 1175-1180;

Citation Manager Formats

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

Share
OtherDRUG METABOLISM AND DISPOSITION

A New Interpretation of Salicylic Acid Transport across the Lipid Bilayer: Implications of pH-Dependent but not Carrier-Mediated Absorption from the Gastrointestinal Tract

Masanori Takagi, Yoko Taki, Toshiyasu Sakane, Tanekazu Nadai, Hitoshi Sezaki, Naoto Oku and Shinji Yamashita
Journal of Pharmacology and Experimental Therapeutics June 1, 1998, 285 (3) 1175-1180;
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

  • Activation of Human Liver 3α-Hydroxysteroid Dehydrogenase by Clofibrate Derivatives
  • Purification and Characterization of Heterologously Expressed Mouse CYP2A5 and CYP2G1: Role in Metabolic Activation of Acetaminophen and 2,6-Dichlorobenzonitrile in Mouse Olfactory Mucosal Microsomes
  • Metabolism and Transport of the Macrolide Immunosuppressant Sirolimus in the Small Intestine
Show more DRUG METABOLISM AND DISPOSITION

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

ASPET's Other Journals

  • Drug Metabolism and Disposition
  • Molecular Pharmacology
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0103 (Online)

Copyright © 2023 by the American Society for Pharmacology and Experimental Therapeutics