Berberine induces GLP-1 secretion through activation of bitter taste receptor pathways

Jul 25, 2015Biochemical pharmacology

Berberine may increase GLP-1 hormone release by activating bitter taste receptors

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Abstract

Berberine stimulated GLP-1 secretion via activation of bitter taste receptors in a PLC-dependent manner.

TAS2R38, a subtype of bitter taste receptor, was detected on human enteroendocrine NCI-H716 cells.
Inhibition of TAS2R38 reduced GLP-1 secretion induced by berberine in NCI-H716 cells.
Gene silencing of TAS2R38 led to decreased berberine-mediated GLP-1 secretion.
The PLC inhibitor U73122 hindered berberine-induced GLP-1 release, indicating a role for this pathway.
The TRPM5 blocker quinine did not affect the secretion of GLP-1 induced by berberine.

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Our previous studies revealed that berberine-mediated GLP-1 secretion was a possible mechanism for berberine exerting good effects on hyperglycemia. This study was designed to ascertain whether berberine-induced secretion of GLP-1 was related with activation of bitter taste receptors expressed in gastrointestinal tract. Western blotting results showed that TAS2R38, a subtype of bitter taste receptor, was expressed on human enteroendocrine NCI-H716 cells. GLP-1 secretion induced by berberine from NCI-H716 cells was inhibited by incubation with anti-TAS2R38 antibody. We further performed gene silencing using siRNA to knockdown TAS2R38 from NCI-H716 cells, which showed that siRNA knockdown of the TAS2R38 reduced berberine-mediated GLP-1 secretion. We adopted inhibitors of PLC and TRPM5 known to be involved in bitter taste transduction to investigate the underlying pathways mediated in berberine-induced GLP-1 secretion. It was found that PLC inhibitor U73122 inhibited berberine-induced GLP-1 release in NCI-H716 cells, while TRPM5 blocker quinine failed to attenuate berberine-induced secretion of GLP-1. The present results demonstrated that berberine stimulated GLP-1 secretion via activation of gut-expressed bitter taste receptors in a PLC-dependent manner. Because berberine was found to be a ligand of bitter taste receptor, the results of present study may provide an explanation for some bitter taste substance obtain hypoglycemic effect.

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Berberine induces GLP-1 secretion through activation of bitter taste receptor pathways

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