Constitutive androstane receptor activation evokes the expression of glycolytic genes

2016 ◽  
Vol 478 (3) ◽  
pp. 1099-1105 ◽  
Author(s):  
Andrei A. Yarushkin ◽  
Yuliya A. Kazantseva ◽  
Elena A. Prokopyeva ◽  
Diana N. Markova ◽  
Yuliya A. Pustylnyak ◽  
...  
Keyword(s):  
Constitutive Androstane Receptor ◽  
Receptor Activation ◽  
Constitutive Androstane Receptor Activation

Effect of several analogs of 2,4,6-triphenyldioxane-1,3 on constitutive androstane receptor activation

2011 ◽  
Vol 192 (3) ◽  
pp. 177-183 ◽  
Author(s):  
Vladimir Pustylnyak ◽  
Andrei Yarushkin ◽  
Ekaterina Kachaylo ◽  
Nikolai Slynko ◽  
Vyacheslav Lyakhovich ◽  
...  
Keyword(s):  
Constitutive Androstane Receptor ◽  
Receptor Activation ◽  
Constitutive Androstane Receptor Activation

Effect of Aflatoxin B1 on Nuclear Receptors PXR, CAR, and AhR and Their Target Cytochromes P450 mRNA Expression in Primary Cultures of Human Hepatocytes

2011 ◽  
Vol 31 (1) ◽  
pp. 86-93 ◽  
Author(s):  
Imen Ayed-Boussema ◽  
Jean-Marc Pascussi ◽  
Patrick Maurel ◽  
Hassen Bacha ◽  
Wafa Hassen
Keyword(s):  
Mrna Expression ◽  
Aflatoxin B1 ◽  
Messenger Rna ◽  
Animal Feed ◽  
Cytochromes P450 ◽  
Primary Cultures ◽  
Constitutive Androstane Receptor ◽  
Pregnane X Receptor ◽  
Receptor Activation ◽  
Human Hepatocytes

Aflatoxin B1 (AFB1), one of the most common mycotoxins found in human foods and animal feed, is principally hepatotoxic and hepatocarcinogenic. The aim of the present study was to explore the effect of AFB1 on messenger RNA (mRNA) expression of pregnane X receptor (PXR), constitutive androstane receptor (CAR), and aryl hydrocarbon receptor (AhR) and some of their target cytochromes using primary cultures of human hepatocytes. Our results showed that AFB1, at noncytotoxic increasing concentrations, caused a significant upregulation of cytochrome P 2B6 (CYP2B6), CYP3A5, and to a lesser extent CYP3A4 and CYP2C9. Pregnane X receptor and CAR mRNA expression increased in the 3 treated livers. Aflatoxin B1 was found also to induce an overexpression of CYP1A1 and CYP1A2 genes accompanied by an increase in AhR mRNA expression. These findings suggest that AFB1 could activate PXR, CAR, and AhR; however, further investigations are needed to confirm nuclear receptor activation by AFB1.

scholarly journals The Connection of Azole Fungicides with Xeno-Sensing Nuclear Receptors, Drug Metabolism and Hepatotoxicity

Cells ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 1192 ◽  
Author(s):  
Philip Marx-Stoelting ◽  
Constanze Knebel ◽  
Albert Braeuning
Keyword(s):  
Nuclear Receptors ◽  
Nuclear Receptor ◽  
Liver Tumors ◽  
Current Knowledge ◽  
Constitutive Androstane Receptor ◽  
Pregnane X Receptor ◽  
Receptor Activation ◽  
Azole Fungicides

Azole fungicides, especially triazole compounds, are widely used in agriculture and as pharmaceuticals. For a considerable number of agricultural azole fungicides, the liver has been identified as the main target organ of toxicity. A number of previous studies points towards an important role of nuclear receptors such as the constitutive androstane receptor (CAR), the pregnane-X-receptor (PXR), or the aryl hydrocarbon receptor (AHR), within the molecular pathways leading to hepatotoxicity of these compounds. Nuclear receptor-mediated hepatic effects may comprise rather adaptive changes such as the induction of drug-metabolizing enzymes, to hepatocellular hypertrophy, histopathologically detectable fatty acid changes, proliferation of hepatocytes, and the promotion of liver tumors. Here, we present a comprehensive review of the current knowledge of the interaction of major agricultural azole-class fungicides with the three nuclear receptors CAR, PXR, and AHR in vivo and in vitro. Nuclear receptor activation profiles of the azoles are presented and related to histopathological findings from classic toxicity studies. Important issues such as species differences and multi-receptor agonism and the consequences for data interpretation and risk assessment are discussed.

scholarly journals Aryl-hydrocarbon receptor activation regulates constitutive androstane receptor levels in murine and human liver

Hepatology ◽  
2007 ◽  
Vol 46 (1) ◽  
pp. 209-218 ◽  
Author(s):  
Rushang D. Patel ◽  
Brett D. Hollingshead ◽  
Curtis J. Omiecinski ◽  
Gary H. Perdew
Keyword(s):  
Aryl Hydrocarbon Receptor ◽  
Human Liver ◽  
Constitutive Androstane Receptor ◽  
Receptor Activation ◽  
Aryl Hydrocarbon
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