Arsenite and its metabolites, MMAIII and DMAIII, modify CYP3A4, PXR and RXR alpha expression in the small intestine of CYP3A4 transgenic mice


Por: Medina-Díaz I.M., Estrada-Muñiz E., Reyes-Hernández O.D., Ramírez P., Vega L., Elizondo G.

Publicada: 1 sep 2009
Resumen:
Arsenic is an environmental pollutant that has been associated with an increased risk for the development of cancer and several other diseases through alterations of cellular homeostasis and hepatic function. Cytochrome P450 (P450) modification may be one of the factors contributing to these disorders. Several reports have established that exposure to arsenite modifies P450 expression by decreasing or increasing mRNA and protein levels. Cytochrome P450 3A4 (CYP3A4), the predominant P450 expressed in the human liver and intestines, which is regulated mainly by the Pregnane X Receptor-Retinoid X Receptor alpha (PXR-RXR alpha) heterodimer, contributes to the metabolism of approximately half the drugs in clinical use today. The present study investigates the effect of sodium arsenite and its metabolites monomethylarsonous acid (MMAIII) and dimethylarsinous acid (DMAIII) on CYP3A4, PXR, and RXR alpha expression in the small intestine of CYP3A4 transgenic mice. Sodium arsenite treatment increases mRNA, protein and CYP3A4 activity in a dose-dependent manner. However, the increase in protein expression was not as marked as compared to the increase in mRNA levels. Arsenite treatment induces the accumulation of Ub-protein conjugates, indicating that the activation of this mechanism may explain the differences observed between the mRNA and protein expression of CYP3A4 induction. Treatment with 0.05 mg/kg of DMAIII induces CYP3A4 in a similar way, while treatment with 0.05 mg/kg of MMAIII increases mostly mRNA, and to a lesser degree, CYP3A4 activity. Sodium arsenite and both its metabolites increase PXR mRNA, while only DMAIII induces RXR alpha expression. Overall, these results suggest that sodium arsenite and its metabolites induce CYP3A4 expression by increasing PXR expression in the small intestine of CYP3A4 transgenic mice. © 2008 Elsevier Inc. All rights reserved.

Filiaciones:
Medina-Díaz I.M.:
 Universidad Autónoma de Nayarit, Nayarit, Mexico

Estrada-Muñiz E.:
 Sección Externa de Toxicología, Centro de Investigación y de Estudios Avanzados, I.P.N., México City, Mexico

Reyes-Hernández O.D.:
 Sección Externa de Toxicología, Centro de Investigación y de Estudios Avanzados, I.P.N., México City, Mexico

Ramírez P.:
 Univ Nacl Autonoma Mexico, Unidad Multidisciplinaria Invest, Lab Toxicol & Genet, Fac Estudios Super Cuautitlan, Cuautitlan, Mexico

Vega L.:
 Sección Externa de Toxicología, Centro de Investigación y de Estudios Avanzados, I.P.N., México City, Mexico

Elizondo G.:
 Dept. de Biología Celular, Centro de Investigación y de Estudios Avanzados, I.P.N., México City, Mexico
ISSN: 0041008X
Editorial
ACADEMIC PRESS INC ELSEVIER SCIENCE, 525 B ST, STE 1900, SAN DIEGO, CA 92101-4495 USA, Estados Unidos America
Tipo de documento: Article
Volumen: 239 Número: 2
Páginas: 162-168
WOS Id: 000269585800006
ID de PubMed: 19084030