Transl Clin Pharmacol.  2014 Jun;22(1):19-21.

Pregnane X Receptor agonist Increases the Expression Levels of the Plasma Membrane Monoamine Transporter

• Cho SK
• Oh H
• Hong SH
• Park MS
• Chung JY

Abstract

We evaluated the effect of the pregnane X receptor agonist, pregnenolone 16 alpha-carbonitrile (PCN) on the expression levels of plasma monoamine transporter (PMAT) in the intestine. Male C57/BL6 mice were divided into two 2 groups: mice in the PCN group (n=3) were administered PCN once a day for 4 days, while those in the control group (n=3) received the same volume of vehicle once a day for 4 days. After the mice were killed 24 h after administration of the last dose of PCN or vehicle, and the expression levels of PMAT in the intestine tissues were isolated and measured the expression level of PMAT using immunohistochemical and western blotting analyses. The expression level of PMAT expression levels in the small intestine increased after PCN treatment. These results suggest that the induction of PMAT may play a clinically significant role by increasing intestinal absorption of PMAT substrates such as metformin.

Keyword

PXR; PMAT; PCN; Expression

MeSH Terms

Animals
Blotting, Western
Cell Membrane*
Humans
Intestinal Absorption
Intestine, Small
Intestines
Male
Metformin
Mice
Plasma
Pregnenolone Carbonitrile
Metformin
Pregnenolone Carbonitrile

Figure

• 

  Figure 1. Effect of pregnenolone 16 alpha-carbonitrile (PCN) on PMAT expression in C57/BL6 mice. Representative immunohistochemical images for PMAT staining in the small intestine in the control (left) and PCN (right) animals.

• 

  Figure 2. The effect of PCN on PMAT expression in the liver and small intestine as assessed using western blotting analyses (samples were pooled).

Reference

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