Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • 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
  • 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
    • 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
  • Visit dmd on Facebook
  • Follow dmd on Twitter
  • Follow ASPET on LinkedIn
Research ArticleArticle

Metabolism of Saikosaponin a in Rats: Diverse Oxidations on the Aglycone Moiety in Liver and Intestine in Addition to Hydrolysis of Glycosidic Bonds

Guoqiang Liu, Yuan Tian, Geng Li, Lei Xu, Rui Song and Zunjian Zhang
Drug Metabolism and Disposition March 2013, 41 (3) 622-633; DOI: https://doi.org/10.1124/dmd.112.048975
Guoqiang Liu
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Yuan Tian
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Geng Li
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Lei Xu
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Rui Song
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Zunjian Zhang
Key Laboratory of Drug Quality Control and Pharmacovigilance (Gu.L., Y.T., Ge.L., L.X., R.S., Z.Z.) and State Key Laboratory of Natural Medicines (Z.Z.), China Pharmaceutical University, Nanjing, China
  • 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 + SI
  • PDF
Loading

Abstract

The main objective of the present study was to completely characterize the metabolites of the triterpenoid saikosaponin a (SSa) in rats. To this aim, we compared the metabolites in plasma, bile, urine, and feces samples following oral and i.v. routes of administration using liquid chromatography–diode array detector coupled with hybrid ion trap–time-of-flight mass spectrometry. As a result, besides 2 known metabolites, prosaikogenin f and saikogenin f, 15 new metabolites were detected in all. It was found that SSa is metabolized mainly in phase I manner, i.e., hydration and monooxidation on the aglycone moiety and hydrolysis of the β-glucosidic bond in the liver, and sequential hydrolysis of β-glucosidic and β-fucosidic bonds followed by dehydrogenation, hydroxylation, carboxylation, and combinations of these steps on the aglycone moiety in the intestinal tract. Both the renal and biliary routes were observed for the excretion of SSa and its metabolites. Further, a clear metabolic profile in rats was proposed in detail according to the results from the in vivo animal experiment after different routes of administration. Our results update the preclinical metabolism and disposition data on SSa, which is not only helpful for the future human metabolic study of this compound but also provides basic information for better understanding of the efficacy and safety of prescriptions containing saikosaponins.

Footnotes

  • This study was financially supported by the National Natural Science Foundation of China [Grant 30873439].

  • dx.doi.org/10.1124/dmd.112.048975.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Received September 11, 2012.
  • Accepted December 31, 2012.
  • Copyright © 2013 by 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: 41 (3)
Drug Metabolism and Disposition
Vol. 41, Issue 3
1 Mar 2013
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • Index by author
  • Editorial Board (PDF)
  • Front Matter (PDF)
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.
Metabolism of Saikosaponin a in Rats: Diverse Oxidations on the Aglycone Moiety in Liver and Intestine in Addition to Hydrolysis of Glycosidic Bonds
(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

Metabolism of Saikosaponin a in Rats

Guoqiang Liu, Yuan Tian, Geng Li, Lei Xu, Rui Song and Zunjian Zhang
Drug Metabolism and Disposition March 1, 2013, 41 (3) 622-633; DOI: https://doi.org/10.1124/dmd.112.048975

Citation Manager Formats

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

Metabolism of Saikosaponin a in Rats

Guoqiang Liu, Yuan Tian, Geng Li, Lei Xu, Rui Song and Zunjian Zhang
Drug Metabolism and Disposition March 1, 2013, 41 (3) 622-633; DOI: https://doi.org/10.1124/dmd.112.048975
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Introduction
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Authorship Contributions
    • Footnotes
    • Abbreviations
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF + SI
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Clearance pathways: fevipiprant with probenecid perpetrator
  • Predicting Volume of Distribution from In Vitro Parameters
  • In Vivo Functional Effects of CYP2C9 M1L
Show more Articles

Similar Articles

  • 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 © 2021 by the American Society for Pharmacology and Experimental Therapeutics