Steviol, an aglycone of steviol glycoside sweeteners, interacts with the pregnane X (PXR) and aryl hydrocarbon (AHR) receptors in detoxification regulation

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F17%3A10365291" target="_blank" >RIV/00216208:11150/17:10365291 - isvavai.cz</a>

Alternative codes found

RIV/00216208:11160/17:10365291

Result on the web

<a href="http://www.sciencedirect.com/science/article/pii/S0278691517305124" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0278691517305124</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.fct.2017.09.007" target="_blank" >10.1016/j.fct.2017.09.007</a>

Result language

angličtina

Original language name

Steviol, an aglycone of steviol glycoside sweeteners, interacts with the pregnane X (PXR) and aryl hydrocarbon (AHR) receptors in detoxification regulation

Original language description

Stevia rebaudiana Bertoni is a herb known for the high content of natural sweeteners in its leaves. Its main secondary metabolite stevioside is used as non-caloric sweetener. No information, however, is available on whether stevioside or steviol interact with drug-metabolizing enzymes and pose the potential risk of food-drug interactions. Similarly, data are lacking on the interactions of steviol and stevioside with key nuclear receptors controlling the expression of the main drug metabolizing enzymes. We studied the interactions of steviol and stevioside with the pregnane X (PXR), vitamin D (VDR), constitutive androstane (CAR), farnesoid X (FXR), glucocorticoid (GR) and aryl hydrocarbon (AHR) receptors, which control expression of genes of xenobiotic metabolism. In addition, the inhibitory activities of steviol and stevioside towards the major cytochrome P450 enzymes CYP3A4, CYP2C9, CYP2D6, CYP1A2 and CYP2B6 were evaluated in vitro. We found that steviol moderately activated the PXR and AHR, resulting in the induction of their target genes including CYP3A4 and CYP1A2 in primary human hepatocytes. A weak inhibition of CYP3A4 and CYP2C9 with steviol was also found. Our results provide mechanistic data indicating that stevioside and stevia sweeteners may have the potential to induce food-drug interactions, a finding that warrants future prospective clinical investigation.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

30104 - Pharmacology and pharmacy

Project

<a href="/en/project/GA17-06841S" target="_blank" >GA17-06841S: Dynamics of nuclear receptor-mediated gene regulation:implement for the understanding of detoxification functions and optimization of therapy</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2017

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Food and Chemical Toxicology

ISSN

0278-6915

e-ISSN

—

Volume of the periodical

109

Issue of the periodical within the volume

November

Country of publishing house

GB - UNITED KINGDOM

Number of pages

13

Pages from-to

130-142

UT code for WoS article

000415911400013

EID of the result in the Scopus database

2-s2.0-85028890164