November 28, 2013

The expression and relaxant effect of bitter taste receptors in human bronchi

Open Access
Research

The expression and relaxant effect of bitter taste receptors in human bronchi

Stanislas Grassin-DelyleCharlotte AbrialSarah Fayad-KobeissiMarion BrolloChristophe FaisyJean-Claude AlvarezEmmanuel Naline and Philippe Devillier
For all author emails, please log on.



Respiratory Research 2013, 14:134  doi:10.1186/1465-9921-14-134
Published: 22 November 2013

Abstract (provisional)

Background

Bitter-taste receptors (TAS2Rs) have recently been involved in the relaxation of mouse and guinea pig airways, and increased expression of TAS2Rs was shown in blood leucocytes from asthmatic children. We sought to identify and characterize the TAS2Rs expressed in isolated human bronchi and the subtypes involved in relaxation.

Methods

Human bronchi were isolated from resected lungs and TAS2R transcripts were assessed with RT-qPCR. Relaxation to TAS2R agonists was tested in organ bath in the presence or absence of pharmacological modulators of the signalling pathways involved in bronchial relaxation.

Results

We detected the expression of TAS2R transcripts in human bronchi. The non-selective agonists chloroquine, quinine, caffeine, strychnine and diphenidol produced a bronchial relaxation as effective and potent as theophylline but much less potent than formoterol and isoproterenol. Denatonium, saccharin and colchicine did not produce relaxation. Receptor expression analysis together with the use of selective agonists suggest a predominant role for TAS2R5, 10 and 14 in bitter taste agonist-induced relaxation. The mechanism of relaxation was independent of the signalling pathways modulated by conventional bronchodilators and may be partly explained by the inhibition of phosphatidylinositol-3-kinases.

Conclusions

The TAS2Rs may constitute a new therapeutic target in chronic obstructive lung diseases such as asthma.

The complete article is available as a provisional PDF. The fully formatted PDF and HTML versions are in production.

No comments:

Post a Comment