Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 52, 2022 - Issue 4
202
Views
0
CrossRef citations to date
0
Altmetric
General Xenobiochemistry

Metabolism of gartanin in liver microsomes and its modulating effects on cytochrome P450s

&
Pages 335-345 | Received 03 Mar 2022, Accepted 09 May 2022, Published online: 24 May 2022
 

Abstract

  1. Gartanin, a compound found in mangosteen, has various pharmacological activities, including anticancer, anti-inflammation, and antioxidation.

  2. In the present study, we reported differences of gartanin metabolism among species and the effect of gartanin on cytochrome P450 (CYP) activities and protein expression.

  3. We found significant difference in gartanin metabolism among species, where rabbits and humans had similar metabolic characteristics. Five CYP-catalysed metabolites and three glucuronosyltransferase (UGT)-catalysed metabolites were identified by LC-MS/MS. Hydroxylation was the major metabolic pathway. Gartanin exhibited mixed inhibition on CYP1A2 activity with IC50 and Ki values of 1.48 and 3.71 μM, respectively. In addition, gartanin down-regulated the protein expressions of CYP2C9 and CYP2D6 and up-regulated the protein expression of CYP2D6. The present study supports the pharmacological and toxicological research of gartanin.

Disclosure statement

The authors report no declarations of interest.

Log in via your institution

Log in to Taylor & Francis Online

PDF download + Online access

  • 48 hours access to article PDF & online version
  • Article PDF can be downloaded
  • Article PDF can be printed
USD 65.00 Add to cart

Issue Purchase

  • 30 days online access to complete issue
  • Article PDFs can be downloaded
  • Article PDFs can be printed
USD 897.00 Add to cart

* Local tax will be added as applicable

Related Research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.