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

Yu, Yunli; Hao, Gang; Quan-ying, Zhang; Hua, Wenyan; Wang, Meng; Zhou, Wenjia; Zong, Shunlin; Huang, Ming; Wen, Xiaozhou

doi:10.1016/j.bcp.2015.07.012

Cited by 84 publications

(59 citation statements)

References 27 publications

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“…, Yu et al . ). Intra‐gastric administration of bitter agonists (DB, PTC, salicin, propylthiouracil) in mice resulted in increased plasma ghrelin levels, which were partially mediated via activation of α ‐gustducin and resulted in a short‐term increase in food intake.…”

Section: Expression and Function Of Extra‐oral Bitter Taste Receptorsmentioning

confidence: 97%

“…The human enteroendocrine cell line HuTu-80 released CCK in response to an extract of the plant Hoodia Gordonii, presumably via activation of hTAS2R14 (Le Neve et al 2010). In another human enteroendocrine cell line, NCI-H716, bitter tastants (oflatoxin, quinine, DB) or extracts of the bitter herb Gentiana Scabra also induced a dose-dependent rise in GLP-1 release through activation of hTAS2Rs and the canonical taste signalling pathway (Dotson et al 2008, Kim et al 2013, 2014, Suh et al 2015, Yu et al 2015. Intra-gastric administration of bitter agonists (DB, PTC, salicin, propylthiouracil) in mice resulted in increased plasma ghrelin levels, which were partially mediated via activation of a-gustducin and resulted in a short-term increase in food intake.…”

Section: Expression and Function Of Extra-oral Bitter Taste Receptorsmentioning

confidence: 99%

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The bitter truth about bitter taste receptors: beyond sensing bitter in the oral cavity

Avau

Depoortere

2015

Acta Physiologica

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The bitter taste receptor (TAS2R)-family of G-protein-coupled receptors has been identified on the tongue as detectors of bitter taste over a decade ago. In the last few years, they have been discovered in an ever growing number of extra-oral tissues, including the airways, the gut, the brain and even the testis. In tissues that contact the exterior, protective functions for TAS2Rs have been proposed, in analogy to their function on the tongue as toxicity detector. However, TAS2Rs have also been found in internal organs, suggesting other roles for these receptors, perhaps involving as yet unidentified endogenous ligands. The current review gives an overview of the different proposed functions for TAS2Rs in tissues other than the oral cavity; from appetite regulation to the treatment of asthma, regulation of gastrointestinal motility and control of airway innate immunity.

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Section: Expression and Function Of Extra‐oral Bitter Taste Receptorsmentioning

confidence: 97%

Section: Expression and Function Of Extra-oral Bitter Taste Receptorsmentioning

confidence: 99%

The bitter truth about bitter taste receptors: beyond sensing bitter in the oral cavity

Avau

Depoortere

2015

Acta Physiologica

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“…Berberine, the major bitter constituent of the Chinese herb Coptis root (Rhizoma coptidis), has been shown to influence secretion of GLP-1 via binding to the bitter taste receptor TAS2R38 (in this case expressed on human enteroendocrine NCI-H716 cells) (Yu et al, 2015) (Yu et al, 2015). The GLP-1 secretion was associated with good effects on hyperglycemia (Lu et al, 2009;Yu et al, 2010).…”

Section: Dietary Factors Affecting Metabolism Via Bitter Taste Receptorsmentioning

confidence: 99%

Taste receptors in the gut – A new target for health promoting properties in diet

Ekstrand

Young

Rasmussen

2017

Food Research International

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These receptors are involved in an intricate signalling network for monitoring of taste and nutrient intake, homeostasis and energy metabolism, and they are also an early warning system for toxic substances in our diet. Especially the receptors for bitter taste provide a new possibility to activate a number of health related signalling pathways, already at low concentrations of the active substance, without requiring uptake into the body and transport via the circulation. When ligands bind to these receptors, signalling is induced either via peptide hormones into the circulation to other organs in the body, or via nerve fibers directly to the brain.

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“…However, it is a daily injectable treatment that is also relatively high cost [6,9].Due to these limitations on GLP-1 and its analogues, cost-effective herbal supplements, including natural products, medicinal plant extracts and Chinese herbal medicine, are popular alternatives for weight reduction. Natural products such as epigallocatechin gallate (EGCG) [5], geniposide [10], berberine [11] and ginsenoside metabolite compound K [12] have been shown to stimulate GLP-1 secretion in in vitro experiments.In this paper, we have investigated the commercially available RCM-107 formula (Slimming Plus), a modification of our previously studied RCM-104 formula, which demonstrated significant effects on weight loss in clinical trials [13]. RCM-107 contains eight Chinese herbs, including Camellia sinensis/Lu cha ye; Poria/Poria cocos (schw.)…”

mentioning

confidence: 99%

“…Due to these limitations on GLP-1 and its analogues, cost-effective herbal supplements, including natural products, medicinal plant extracts and Chinese herbal medicine, are popular alternatives for weight reduction. Natural products such as epigallocatechin gallate (EGCG) [5], geniposide [10], berberine [11] and ginsenoside metabolite compound K [12] have been shown to stimulate GLP-1 secretion in in vitro experiments.…”

mentioning

confidence: 99%

The Effects of a Weight-Loss Herbal Formula RCM-107 and Its Eight Individual Ingredients on Glucagon-Like Peptide-1 Secretion—An In Vitro and In Silico Study

Luo

Gill

Feltis

et al. 2020

IJMS

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Obesity is a multifactorial disease that can lead to other health issues. Glucagon-like peptide-1(GLP-1), as one of the satiety signal, has been linked with appetite suppression and weight loss. Due to the limitations of GLP-1 and its analogues, alternative treatments such as herbal therapies have become popular. The herbal formula RCM-107 has demonstrated its inhibitory effects on lipid and carbohydrate absorption in our previous work. However, no published data described its effects on GLP-1 secretion. Therefore, this study aimed to determine the effects of RCM-107 and its individual ingredients on GLP-1 secretion via enzyme-linked immunosorbent assay (ELISA). Furthermore, molecular docking was performed to predict the key chemical compounds that are likely to be GLP-1 receptor agonists. Gardeniae fructus, one of the ingredients in RCM-107, demonstrated significantly greater effects on inducing GLP-1 secretion than the positive control epigallocatechin gallate (EGCG). Two Gardeniae fructus ligands, 3-epioleanolic acid and crocin were predicted to bind to the active form of GLP-1 receptor at the binding pocket with residues known for the receptor activation, suggesting that they could potentially serve as receptor agonists. Overall, this study reported the effects of researched herbs on GLP-1 secretion and proposed two compounds that may be responsible for antiobesity via GLP-1 receptor activation.Int. J. Mol. Sci. 2020, 21, 2854 2 of 13 hunger. It is known as an incretin hormone, secreted by enteroendocrine L cells in the gastrointestinal tract (GI) [5]. The amount of GLP-1 secretion is in response to calory intake. It can be stimulated by both fats and carbohydrates, while protein has only a minor impact [6]. The existing two major molecular forms of GLP-1 include GLP-1 (7-36) and GLP-1 (7-37), while the circulating active GLP-1 is mainly found in the form of GLP-1(7-36) [7].Reports showed that native GLP-1 has a very short half-life (less than 2 min) in vivo as a result of degradation by dipeptidyl peptidase-4 (DPP-4) in plasma [7,8]. Liraglutide, a stable GLP-1 analogue, was approved by FDA for treating obesity in 2014. It can suppress appetite and increase satiety by activating the GLP-1 receptor, which is located in the hypothalamus, gastrointestinal tract and pancreas. However, it is a daily injectable treatment that is also relatively high cost [6,9].Due to these limitations on GLP-1 and its analogues, cost-effective herbal supplements, including natural products, medicinal plant extracts and Chinese herbal medicine, are popular alternatives for weight reduction. Natural products such as epigallocatechin gallate (EGCG) [5], geniposide [10], berberine [11] and ginsenoside metabolite compound K [12] have been shown to stimulate GLP-1 secretion in in vitro experiments.In this paper, we have investigated the commercially available RCM-107 formula (Slimming Plus), a modification of our previously studied RCM-104 formula, which demonstrated significant effects on weight loss in clinical trials [13]. RCM-107 co...

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

Cited by 84 publications

References 27 publications

The bitter truth about bitter taste receptors: beyond sensing bitter in the oral cavity

The bitter truth about bitter taste receptors: beyond sensing bitter in the oral cavity

Taste receptors in the gut – A new target for health promoting properties in diet

The Effects of a Weight-Loss Herbal Formula RCM-107 and Its Eight Individual Ingredients on Glucagon-Like Peptide-1 Secretion—An In Vitro and In Silico Study

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