Insight into the Interaction of Humulus lupulus L. Specialized Metabolites and Gastrointestinal Bitter Taste Receptors: In Vitro Study in STC-1 Cells and Molecular Docking

Aug 10, 2024Journal of natural products

How Hop Plant Compounds Interact with Bitter Taste Receptors in Gut Cells: Lab Study and Molecular Modeling

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Abstract

The tested bitter compounds induced the secretion of anorexigenic hormones glucagon-like peptide 1 and cholecystokinin.

Bitter taste receptors (T2R) are found throughout the body and regulate various physiological processes.
T2R expression in the intestines may influence food intake and obesity prevalence.
Xanthohumol and α-acids selectively increased the expression of specific T2R proteins in intestinal cells.
β-acids increased the expression of all bitter receptors studied.
Increased levels of intracellular calcium confirmed the activity of the bitter compounds on T2R.
Molecular docking experiments suggested that the bitter compounds could bind to both T2R138 and its human counterpart T2R38.

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Bitter taste receptors, also known as taste 2 receptors (T2R), are expressed throughout the body and are involved in regulating different physiological processes. T2R expression in the intestinal tract regulates orexigenic and anorexigenic peptide secretion, thus becoming potential a potential target for controlling food intake and the prevalence of obesity and overweight. The present study aims to investigate the implication of hop bitter compounds such as α-acids, β-acids, and xanthohumol in the secretion of anorexigenic hormones and T2R expression in intestinal STC-1 cells. The tested bitter compounds induced the secretion of the anorexigenic hormones glucagon-like peptide 1 and cholecystokinin concurrently with a selective increase of murineexpression. Xanthohumol and α-acids selectively increase138 and130-138 expression, respectively, in STC-1 cells, while β-acids increased the expression of all bitter receptors studied, including119,105,138,120, and130. Increased intracellular calcium levels confirmed this activity. As all investigated bitter molecules increased138 expression, computational studies were performed on138 and its human orthologue T2R38 for the first time. Molecular docking experiments showed that all molecules might be able to bind both bitter receptors, providing an excellent basis for applying hop bitter molecules as lead compounds to further design gastrointestinal-permeable T2R agonists. Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r Tas2r

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Insight into the Interaction of Humulus lupulus L. Specialized Metabolites and Gastrointestinal Bitter Taste Receptors: In Vitro Study in STC-1 Cells and Molecular Docking

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