Intestinal bitter taste receptors play important and complex roles in nutrient digestion, absorption, and metabolism, and regulate glucose and lipid homeostasis through the release of gastrointestinal hormones. Numerous bitter taste receptors in mammalian species have been identified over the past decades, and growing evidence support that dietary supplementation of bitter herbs may provide health benefits in glucose and lipid metabolic disorders. Bitter medicinal herbs were widely used in traditional herbal medicine for their properties to aid digestion and/or anti-inflammation, and recent studies have investigated the value of some medicinal plants and their bitter constituents for treating metabolic disorders. Despite the complexity of bitter taste receptors in the digestive system, emerging evidence highlights bitter agonists isolated from medicinal herbs activate bitter signal transduction and facilitate the enteroendocrine secretion of GLP-1 and other gut hormones. Given that the impaired incretin effects are associated with the occurrence of type 2 diabetes, the nutritional and pharmacological studies of bitter melon, hops strobiles, and berberine-containing herbs were carried to evaluate the therapeutic potential in the prevention or treatment of metabolic syndrome and obesity-associated diabetes. Based on current clinical and preclinical evidence, bitter melon can be applied as a dietary supplementation for patients with mild diabetes. Moreover, bitter compounds, such as hops derived KDT501 and berberine, can be used to improve both glycemic control and lipid profile through targeting bitter taste receptors (i.e. human TAS2R1 and TAS2R3 with specific agonists) with the modulation of the enteroendocrine hormone secretion and bile acid turnover. Therefore, such an approach may offer an alternative treatment for metabolic syndrome individuals or diabetic patients with dyslipidemia-related comorbidities beyond incretin-based therapy.
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