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https://www.readbyqxmd.com/read/29656109/bile-acids-are-important-direct-and-indirect-regulators-of-the-secretion-of-appetite-and-metabolism-regulating-hormones-from-the-gut-and-pancreas
#1
Rune E Kuhre, Nicolai J Wewer Albrechtsen, Olav Larsen, Sara L Jepsen, Emilie Balk-Møller, Daniel B Andersen, Carolyn F Deacon, Kristina Schoonjans, Frank Reimann, Fiona M Gribble, Reidar Albrechtsen, Bolette Hartmann, Mette M Rosenkilde, Jens J Holst
OBJECTIVE: Bile acids (BAs) facilitate fat absorption and may play a role in glucose and metabolism regulation, stimulating the secretion of gut hormones. The relative importance and mechanisms involved in BA-stimulated secretion of appetite and metabolism regulating hormones from the gut and pancreas is not well described and was the purpose of this study. METHODS: The effects of bile acids on the secretion of gut and pancreatic hormones was studied in rats and compared to the most well described nutritional secretagogue: glucose...
March 17, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29655980/evaluation-of-novel-tgr5-agonist-in-combination-with-sitagliptin-for-possible-treatment-of-type-2-diabetes
#2
Sameer Agarwal, Santosh Sasane, Jeevan Kumar, Prashant Deshmukh, Hitesh Bhayani, Poonam Giri, Suresh Giri, Shubhangi Soman, Neelima Kulkarni, Mukul Jain
TGR5 is a member of G protein-coupled receptor (GPCR) superfamily, a promising molecular target for metabolic diseases. Activation of TGR5 promotes secretion of glucagon-like peptide-1 (GLP-1), which activates insulin secretion. A series of 2-thio-imidazole derivatives have been identified as novel, potent and orally efficacious TGR5 agonists. Compound 4d, a novel TGR5 agonist, in combination with Sitagliptin, a DPP-4 inhibitor, has demonstrated an adequate GLP-1 secretion and glucose lowering effect in animal models, suggesting a potential clinical option in treatment of type-2 diabetes...
April 5, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29655782/lithocholic-acid-a-bacterial-metabolite-reduces-breast-cancer-cell-proliferation-and-aggressiveness
#3
Edit Mikó, András Vida, Tünde Kovács, Gyula Ujlaki, György Trencsényi, Judit Márton, Zsanett Sári, Patrik Kovács, Anita Boratkó, Zoltán Hujber, Tamás Csonka, Péter Antal-Szalmás, Mitsuhiro Watanabe, Imre Gombos, Balazs Csoka, Borbála Kiss, László Vígh, Judit Szabó, Gábor Méhes, Anna Sebestyén, James J Goedert, Péter Bai
Our study aimed at finding a mechanistic relationship between the gut microbiome and breast cancer. Breast cancer cells are not in direct contact with these microbes, but disease could be influenced by bacterial metabolites including secondary bile acids that are exclusively synthesized by the microbiome and known to enter the human circulation. In murine and bench experiments, a secondary bile acid, lithocholic acid (LCA), reduced cancer cell proliferation (by 10-20%) and VEGF production (by 37%), aggressiveness and metastatic potential of primary tumors through inducing mesenchymal-to-epithelial transition, increased antitumor immune response, OXPHOS and the TCA cycle...
April 12, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29606134/tgr5-expression-in-normal-kidney-and-renal-neoplasms
#4
Chaohui Lisa Zhao, Ali Amin, Yiang Hui, Dongfang Yang, Weibiao Cao
BACKGROUND: The G protein-coupled bile acid receptor (TGR5) is a cell surface receptor which induces the production of intracellular cAMP and promotes epithelial-mesenchymal transition in gastric cancer cell lines. TGR5 is found in a wide variety of tissues including the kidney. However, the patterns of TGR5 expression have not been well characterized in physiologic kidney or renal neoplasms. We explore the expression of TGR5 in benign renal tissue and renal neoplasms and assess its utility as a diagnostic marker...
April 2, 2018: Diagnostic Pathology
https://www.readbyqxmd.com/read/29576437/enterochromaffin-5-ht-cells-a-major-target-for-glp-1-and-gut-microbial-metabolites
#5
Mari L Lund, Kristoffer L Egerod, Maja S Engelstoft, Oksana Dmytriyeva, Elvar Theodorsson, Bhavik A Patel, Thue W Schwartz
OBJECTIVES: 5-HT storing enterochromaffin (EC) cells are believed to respond to nutrient and gut microbial components, and 5-HT receptor-expressing afferent vagal neurons have been described to be the major sensors of nutrients in the GI-tract. However, the molecular mechanism through which EC cells sense nutrients and gut microbiota is still unclear. METHODS AND RESULTS: TPH1, the 5-HT generating enzyme, and chromogranin A, an acidic protein responsible for secretory granule storage of 5-HT, were highly enriched in FACS-purified EC cells from both small intestine and colon using a 5-HT antibody-based method...
March 10, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29569377/immune-regulation-by-microbiome-metabolites
#6
REVIEW
Chang H Kim
Commensal microbes and the host immune system have been co-evolved for mutual regulation. Microbes regulate the host immune system, in part, by producing metabolites. A mounting body of evidence indicates that diverse microbial metabolites profoundly regulate the immune system via host receptors and other target molecules. Immune cells express metabolite-specific receptors such as P2X7 , GPR41, GPR43, GPR109A, aryl hydrocarbon receptor precursor (AhR), pregnane X receptor (PXR), farnesoid X receptor (FXR), TGR5 and other molecular targets...
March 22, 2018: Immunology
https://www.readbyqxmd.com/read/29553998/new-insights-in-the-multiple-roles-of-bile-acids-and-their-signaling-pathways-in-metabolic-control
#7
Jan F de Boer, Vincent W Bloks, Esther Verkade, M Rebecca Heiner-Fokkema, Folkert Kuipers
PURPOSE OF REVIEW: There is a growing awareness that individual bile acid species exert different physiological functions, beyond their classical roles in bile formation and fat absorption, due to differential stimulatory effects on the bile-acid-activated receptors farnesoid X receptor (FXR) and takeda G receptor 5 (TGR5). This review integrates recent findings on the role of individual bile acids and their receptors in metabolic control, with special emphasis on cholesterol homeostasis...
March 16, 2018: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/29486523/intestine-farnesoid-x-receptor-agonist-and-the-gut-microbiota-activate-g-protein-bile-acid-receptor-1-signaling-to-improve-metabolism
#8
Preeti Pathak, Xie Cen, Robert G Nichols, Jessica M Ferrell, Shannon Boehme, Kristopher W Krausz, Andrew D Patterson, Frank J Gonzalez, John Y L Chiang
Bile acids activate farnesoid X receptor (FXR) and G protein-coupled bile acid receptor-1 (Gpbar-1, aka TGR5) to regulate bile acid metabolism and glucose and insulin sensitivity. FXR and TGR5 are co-expressed in the enteroendocrine L cells but their roles in integrated regulation of metabolism are not completely understood. We reported recently that activation of FXR induces TGR5 to stimulate glucagon-like peptide-1 (GLP-1) secretion to improve insulin sensitivity and hepatic metabolism. In this study, we used the intestine-restricted FXR agonist fexaramine (FEX) to study the effect of activation of intestinal FXR on the gut microbiome, bile acid metabolism, and FXR and TGR5 signaling...
February 27, 2018: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/29471473/bidirectional-gpr119-agonism-requires-peptide-yy-and-glucose-for-activity-in-mouse-and-human-colon-mucosa
#9
Iain R Tough, Sarah Forbes, Herbert Herzog, Robert M Jones, Thue W Schwartz, Helen M Cox
The lipid sensor GPR119 is highly expressed by enteroendocrine L-cells and pancreatic β-cells that release the hormones, PYY and GLP-1, and insulin, respectively. Endogenous oleoylethanolamide (OEA) and the dietary metabolite, 2-monoacylglycerol (2-OG) can each activate GPR119. Here we compared mucosal responses to selective, synthetic GPR119 agonists (AR440006, AR231453) and the lipids, OEA, 2-OG and N-oleoyldopamine (OLDA) monitoring epithelial ion transport as a read-out for L-cell activity in native mouse and human gastrointestinal (GI) mucosae...
February 19, 2018: Endocrinology
https://www.readbyqxmd.com/read/29458053/circulating-bile-acids-in-healthy-adults-respond-differently-to-a-dietary-pattern-characterized-by-whole-grains-legumes-and-fruits-and-vegetables-compared-to-a-diet-high-in-refined-grains-and-added-sugars-a-randomized-controlled-crossover-feeding-study
#10
Bigina N R Ginos, Sandi L Navarro, Yvonne Schwarz, Haiwei Gu, Dongfang Wang, Timothy W Randolph, Ali Shojaie, Meredith A J Hullar, Paul D Lampe, Mario Kratz, Marian L Neuhouser, Daniel Raftery, Johanna W Lampe
OBJECTIVE: The effects of diets high in refined grains on biliary and colonic bile acids have been investigated extensively. However, the effects of diets high in whole versus refined grains on circulating bile acids, which can influence glucose homeostasis and inflammation through activation of farnesoid X receptor (FXR) and G protein-coupled bile acid receptor 1 (TGR5), have not been studied. MATERIALS AND METHODS: We conducted a secondary analysis from a randomized controlled crossover feeding trial (NCT00622661) in 80 healthy adults (40 women/40 men, age 18-45 years) from the greater Seattle Area, half of which were normal weight (BMI 18...
February 16, 2018: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/29450114/flavonoid-rich-extract-of-chromolaena-odorata-modulate-circulating-glp-1-in-wistar-rats-computational-evaluation-of-tgr5-involvement
#11
Olaposi Idowu Omotuyi, Oyekanmi Nash, Olumide Kayode Inyang, Joyce Ogidigo, Ojochenemi Enejoh, Okiemute Okpalefe, Tsuyoshi Hamada
Chromolaena odorata is a major bio-resource in folkloric treatment of diabetes. In the present study, its anti-diabetic component and underlying mechanism were investigated. A library containing 140 phytocompounds previously characterized from C. odorata was generated and docked (Autodock Vina) into homology models of dipeptidyl peptidase (DPP)-4, Takeda-G-protein-receptor-5 (TGR5), glucagon-like peptide 1 (GLP1) receptor, renal sodium dependent glucose transporter (SGLUT)-1/2 and nucleotide-binding oligomerization domain (NOD) proteins 1&2...
February 2018: 3 Biotech
https://www.readbyqxmd.com/read/29393918/nanotherapeutics-containing-lithocholic-acid-based-amphiphilic-scorpion-like-macromolecules-reduce-in-vitro-inflammation-in-macrophages-implications-for-atherosclerosis
#12
Alysha Moretti, Qi Li, Rebecca Chmielowski, Laurie B Joseph, Prabhas V Moghe, Kathryn E Uhrich
Previously-designed amphiphilic scorpion-like macromolecule (AScM) nanoparticles (NPs) showed elevated potency to counteract oxidized low-density lipoprotein (oxLDL) uptake in atherosclerotic macrophages, but failed to ameliorate oxLDL-induced inflammation. We designed a new class of composite AScMs incorporating lithocholic acid (LCA), a natural agonist for the TGR5 receptor that is known to counteract atherosclerotic inflammation, with two complementary goals: to simultaneously decrease lipid uptake and inhibit pro-inflammatory cytokine secretion by macrophages...
February 2, 2018: Nanomaterials
https://www.readbyqxmd.com/read/29393300/adipose-tissue-bile-acid-tgr5-axis-promotes-beiging
#13
Conor A Bradley
No abstract text is available yet for this article.
February 2, 2018: Nature Reviews. Endocrinology
https://www.readbyqxmd.com/read/29375205/int-767-improves-histopathological-features-in-a-diet-induced-ob-ob-mouse-model-of-biopsy-confirmed-non-alcoholic-steatohepatitis
#14
Jonathan D Roth, Michael Feigh, Sanne S Veidal, Louise Kd Fensholdt, Kristoffer T Rigbolt, Henrik H Hansen, Li C Chen, Mathieu Petitjean, Weslyn Friley, Niels Vrang, Jacob Jelsing, Mark Young
AIM: To characterize the efficacy of the dual FXR/TGR5 receptor agonist INT-767 upon histological endpoints in a rodent model of diet-induced and biopsy-confirmed non-alcoholic steatohepatitis (NASH). METHODS: The effects of INT-767 on histological features of NASH were assessed in two studies using Lepob/ob (ob/ob) NASH mice fed the AMLN diet (high fat with trans-fat, cholesterol and fructose). In a proof-of-concept study, Lepob/ob (ob/ob) NASH mice were first dosed with INT-767 (3 or 10 mg/kg for 8 wk)...
January 14, 2018: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29365494/effect-of-bile-acid-receptor-fxr-tgr5-agonist-int-767-on-peripheral-immune-cells
#15
Zuzana Papackova, Marie Heczkova, Helena Dankova, Monika Cahova
No abstract text is available yet for this article.
August 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29361497/reversal-of-metabolic-disorders-by-pharmacological-activation-of-bile-acid-receptors-tgr5-and-fxr
#16
Kavita Jadhav, Yang Xu, Yanyong Xu, Yuanyuan Li, Jiesi Xu, Yingdong Zhu, Luciano Adorini, Yoon Kwang Lee, Takhar Kasumov, Liya Yin, Yanqiao Zhang
OBJECTIVES: Activation of the bile acid (BA) receptors farnesoid X receptor (FXR) or G protein-coupled bile acid receptor (GPBAR1; TGR5) improves metabolic homeostasis. In this study, we aim to determine the impact of pharmacological activation of bile acid receptors by INT-767 on reversal of diet-induced metabolic disorders, and the relative contribution of FXR vs. TGR5 to INT-767's effects on metabolic parameters. METHODS: Wild-type (WT), Tgr5-/- , Fxr-/- , Apoe-/- and Shp-/- mice were used to investigate whether and how BA receptor activation by INT-767, a semisynthetic agonist for both FXR and TGR5, could reverse diet-induced metabolic disorders...
March 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29339725/tgr5-signalling-promotes-mitochondrial-fission-and-beige-remodelling-of-white-adipose-tissue
#17
Laura A Velazquez-Villegas, Alessia Perino, Vera Lemos, Marika Zietak, Mitsunori Nomura, Thijs Willem Hendrik Pols, Kristina Schoonjans
Remodelling of energy storing white fat into energy expending beige fat could be a promising strategy to reduce adiposity. Here, we show that the bile acid-responsive membrane receptor TGR5 mediates beiging of the subcutaneous white adipose tissue (scWAT) under multiple environmental cues including cold exposure and prolonged high-fat diet feeding. Moreover, administration of TGR5-selective bile acid mimetics to thermoneutral housed mice leads to the appearance of beige adipocyte markers and increases mitochondrial content in the scWAT of Tgr5 +/+ mice but not in their Tgr5 -/- littermates...
January 16, 2018: Nature Communications
https://www.readbyqxmd.com/read/29339445/bile-acids-in-glucose-metabolism-in-health-and-disease
#18
REVIEW
Hagit Shapiro, Aleksandra A Kolodziejczyk, Daniel Halstuch, Eran Elinav
Bile acids (BAs) are cholesterol-derived metabolites that facilitate the intestinal absorption and transport of dietary lipids. Recently, BAs also emerged as pivotal signaling molecules controlling glucose, lipid, and energy metabolism by binding to the nuclear hormone farnesoid X receptor (FXR) and Takeda G protein receptor 5 (TGR5) in multiple organs, leading to regulation of intestinal incretin secretion, hepatic gluconeogenesis, glycogen synthesis, energy expenditure, inflammation, and gut microbiome configuration...
February 5, 2018: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/29317077/the-pruritus-of-cholestasis-from-bile-acids-to-opiate-agonists-relevant-after-all-these-years
#19
Nora V Bergasa
The pruritus of cholestasis is a maddening complication of liver disease. Increased opioidergic tone contributes to the pruritus of cholestasis, as evidenced by the amelioration of the symptom by opiate antagonists. Obeticholic acid, an agonist of the farnesoid receptor, has been approved for the treatment of primary biliary cholangitis, a disease characterized by cholestasis; this drug is associated with pruritus, the cause of which is unknown. In animal models, bile acids, which accumulate in the body as a result of cholestasis, have been reported to cause scratching behavior mediated by the TGR5 receptor, in an opioid-dependent manner, in laboratory animals...
January 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29285057/chenodeoxycholic-acid-attenuates-high-fat-diet-induced-obesity-and-hyperglycemia-via-the-g-protein-coupled-bile-acid-receptor-1-and-proliferator-activated-receptor-%C3%AE-pathway
#20
Xiaosong Chen, Liu Yan, Zhihui Guo, Ying Chen, Ming Li, Chushan Huang, Zhaohong Chen, Xiyong Meng
G protein-coupled bile acid receptor 1 (TGR5) serves a key function in regulating glycometabolism. TGR5 is highly expressed in the mitochondria of brown adipose tissue (BAT) and downregulates adenosine triphosphate synthesis via the bile acid-TGR5-cyclic adenosine monophosphate-2-iodothyronine deiodinase (D2)-triiodothyronine-uncoupling protein pathway, thus regulating energy homeostasis and reducing body weight. Chenodeoxycholic acid (CDCA), the primary bile acid, is a natural ligand of TGR5. The present study aimed to characterize the ability of CDCA to reduce high-fat diet-induced obesity and improve glucose tolerance...
December 2017: Experimental and Therapeutic Medicine
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