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https://www.readbyqxmd.com/read/29018272/bile-acid-microbiota-crosstalk-in-gastrointestinal-inflammation-and-carcinogenesis
#1
REVIEW
Wei Jia, Guoxiang Xie, Weiping Jia
Emerging evidence points to a strong association between the gut microbiota and the risk, development and progression of gastrointestinal cancers such as colorectal cancer (CRC) and hepatocellular carcinoma (HCC). Bile acids, produced in the liver, are metabolized by enzymes derived from intestinal bacteria and are critically important for maintaining a healthy gut microbiota, balanced lipid and carbohydrate metabolism, insulin sensitivity and innate immunity. Given the complexity of bile acid signalling and the direct biochemical interactions between the gut microbiota and the host, a systems biology perspective is required to understand the liver-bile acid-microbiota axis and its role in gastrointestinal carcinogenesis to reverse the microbiota-mediated alterations in bile acid metabolism that occur in disease states...
October 11, 2017: Nature Reviews. Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28993998/lithocholic-bile-acid-inhibits-lipogenesis-and-induces-apoptosis-in-breast-cancer-cells
#2
Trang H Luu, Jean-Marie Bard, Delphine Carbonnelle, Chloé Chaillou, Jean-Michel Huvelin, Christine Bobin-Dubigeon, Hassan Nazih
BACKGROUND: It has amply been documented that mammary tumor cells may exhibit an increased lipogenesis. Biliary acids are currently recognized as signaling molecules in the intestine, in addition to their classical roles in the digestion and absorption of lipids. The aim of our study was to evaluate the impact of lithocholic acid (LCA) on the lipogenesis of breast cancer cells. The putative cytotoxic effects of LCA on these cells were also examined. METHODS: The effects of LCA on breast cancer-derived MCF-7 and MDA-MB-231 cells were studied using MTT viability assays, Annexin-FITC and Akt phosphorylation assays to evaluate anti-proliferative and pro-apoptotic properties, qRT-PCR and Western blotting assays to assess the expression of the bile acid receptor TGR5 and the estrogen receptor ERα, and genes and proteins involved in apoptosis (Bax, Bcl-2, p53) and lipogenesis (SREBP-1c, FASN, ACACA)...
October 9, 2017: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/28949776/beneficial-effects-of-bile-acid-receptor-agonists-in-pulmonary-disease-models
#3
Paolo Comeglio, Annamaria Morelli, Luciano Adorini, Mario Maggi, Linda Vignozzi
Bile acids act as steroid hormones, controlling lipid, glucose and energy metabolism, as well as inflammation and fibrosis. Their actions are implemented through activation of nuclear (FXR, VDR, PXR) and membrane G protein-coupled (TGR5, S1PR2) receptors. Areas covered: This review discusses the potential of FXR and TGR5 as therapeutic targets in the treatment of pulmonary disorders linked to metabolism and/or inflammation. Obeticholic acid (OCA) is the most clinically advanced bile acid-derived agonist for FXR-mediated anti-inflammatory and anti-fibrotic effects...
November 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28946907/the-relationship-between-bile-acid-concentration-glucagon-like-peptide-1-fibroblast-growth-factor-15-and-bile-acid-receptors-in-rats-during-progression-of-glucose-intolerance
#4
Xinfeng Yan, Peicheng Li, Zhaosheng Tang, Bo Feng
BACKGROUND: Recent studies show that bile acids are involved in glucose and energy homeostasis through activation of G protein coupled membrane receptor (TGR5) and farnesoid X receptor (FXR). A few researches have explored changes of TGR5 and FXR in animals with impaired glucose regulation. This study aimed to observe changes of plasma total bile acids (TBA), glucagon-like-peptide 1 (GLP-1), fibroblast growth factor 15 (FGF15), intestinal expressions of TGR5 and FXR, and correlations between them in rats with glucose intolerance...
September 25, 2017: BMC Endocrine Disorders
https://www.readbyqxmd.com/read/28916388/differential-effects-of-fxr-or-tgr5-activation-in-cholangiocarcinoma-progression
#5
O Erice, I Labiano, A Arbelaiz, A Santos-Laso, P Munoz-Garrido, R Jimenez-Agüero, P Olaizola, A Caro-Maldonado, N Martín-Martín, A Carracedo, E Lozano, J J Marin, C J O'Rourke, J B Andersen, J Llop, V Gómez-Vallejo, D Padro, A Martin, M Marzioni, L Adorini, M Trauner, L Bujanda, M J Perugorria, J M Banales
BACKGROUND AND AIMS: Cholangiocarcinoma (CCA) is an aggressive tumor type affecting cholangiocytes. CCAs frequently arise under certain cholestatic liver conditions. Intrahepatic accumulation of bile acids may facilitate cocarcinogenic effects by triggering an inflammatory response and cholangiocyte proliferation. Here, the role of bile acid receptors FXR and TGR5 in CCA progression was evaluated. METHODS: FXR and TGR5 expression was determined in human CCA tissues and cell lines...
September 13, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28903349/the-g-protein-coupled-bile-acid-receptor-gpbar1-tgr5-protects-against-renal-inflammation-and-renal-cancer-cell-proliferation-and-migration-through-antagonizing-nf-%C3%AE%C2%BAb-and-stat3-signaling-pathways
#6
Jia Su, Qiqi Zhang, Hui Qi, Linlin Wu, Yuanqiang Li, Donna Yu, Wendong Huang, Wei-Dong Chen, Yan-Dong Wang
Gpbar1 (TGR5), a G-protein-coupled bile acid membrane receptor, is well known for its roles in regulation of glucose metabolism and energy homeostasis. In the current work, we found that TGR5 activation by its ligand suppressed lipopolysaccharide (LPS)-induced proinflammatory gene expression in wild-type (WT) but not TGR5(-/-) mouse kidney. Furthermore, we found that TGR5 is a suppressor of kidney cancer cell proliferation and migration. We show that TGR5 activation antagonized NF-κB and STAT3 signaling pathways through suppressing the phosphorylation of IκBα, the translocation of p65 and the phosphorylation of STAT3...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28894223/long-term-administration-of-nuclear-bile-acid-receptor-fxr-agonist-prevents-spontaneous-hepatocarcinogenesis-in-abcb4-mice
#7
Marica Cariello, Claudia Peres, Roberta Zerlotin, Emanuele Porru, Carlo Sabbà, Aldo Roda, Antonio Moschetta
Altered bile acid (BA) signaling is associated with hepatotoxicity. The farnesoid X receptor (FXR) is a nuclear receptor that transcriptionally regulates BA homeostasis. Mice with FXR ablation present hepatocarcinoma (HCC) due to high toxic BA levels. Mice with Abcb4 ablation accumulate toxic BA within the bile ducts and present HCC. We have previously shown that intestinal specific activation of FXR by transgenic VP16-FXR chimera is able to reduce BA pool size and prevent HCC. Here we tested chemical FXR activation by administering for 15 months the dual FXR/ membrane G protein-coupled receptor (TGR5) agonist INT-767 (6α-ethyl-3α,7α,23-trihydroxy-24-nor-5β-cholan-23-sulphate) to Fxr(-/-) and Abcb4(-/-) mice...
September 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28881290/glycyrrhizic-acid-increases-glucagon-like-peptide-1-secretion-via-tgr5-activation-in-type-1-like-diabetic-rats
#8
Lin-Yu Wang, Kai Chun Cheng, Yingxiao Li, Chiang-Shan Niu, Juei-Tang Cheng, Ho-Shan Niu
Glycyrrhizic acid (GA) is belonged to triterpenoid saponin that is contained in the root of licorice and is known to affect metabolic regulation. Recently, glucagon like peptide-1 (GLP-1) has widely been applied in diabetes therapeutics. However, the role of GLP-1 in GA-induced anti-diabetic effects is still unknown. Therefore, we are interested in understanding the association of GLP-1 with GA-induced effects. In type 1-like diabetic rats induced by streptozotocin (STZ-treated rats), GA increased the level of plasma GLP-1, which was blocked by triamterene at a dose sufficient to inhibit Takeda G-protein-coupled receptor 5 (TGR5)...
September 4, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28856736/interactions-between-bile-salts-gut-microbiota-and-hepatic-innate-immunity
#9
REVIEW
Kristin Schubert, Steven W M Olde Damink, Martin von Bergen, Frank G Schaap
Bile salts are the water-soluble end products of hepatic cholesterol catabolism that are released into the duodenum and solubilize lipids due to their amphipathic structure. Bile salts also act as endogenous ligands for dedicated nuclear receptors that exert a plethora of biological processes, mostly related to metabolism. Bile salts are actively reclaimed in the distal part of the small intestine, released into the portal system, and subsequently extracted by the liver. This enterohepatic cycle is critically dependent on dedicated bile salt transporters...
September 2017: Immunological Reviews
https://www.readbyqxmd.com/read/28844960/bile-acid-receptors-in-the-biliary-tree-tgr5-in-physiology-and-disease
#10
REVIEW
Kathleen Deutschmann, Maria Reich, Caroline Klindt, Carola Dröge, Lina Spomer, Dieter Häussinger, Verena Keitel
Bile salts represent signalling molecules with a variety of endocrine functions. Bile salt effects are mediated by different receptor molecules, comprising ligand-activated nuclear transcription factors as well as G protein-coupled membrane-bound receptors. The farnesoid X receptor (FXR) and the plasma membrane-bound G protein-coupled receptor TGR5 (Gpbar-1) are prototypic bile salt receptors of both classes and are highly expressed in the liver including the biliary tree as well as in the intestine. In liver, TGR5 is localized in different non-parenchymal cells such as sinusoidal endothelial cells, Kupffer cells, hepatic stellate cells and small and large cholangiocytes...
August 25, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28769799/allspice-and-clove-as-source-of-triterpene-acids-activating-the-g-protein-coupled-bile-acid-receptor-tgr5
#11
Angela Ladurner, Martin Zehl, Ulrike Grienke, Christoph Hofstadler, Nadina Faur, Fátima C Pereira, David Berry, Verena M Dirsch, Judith M Rollinger
Worldwide, metabolic diseases such as obesity and type 2 diabetes have reached epidemic proportions. A major regulator of metabolic processes that gained interest in recent years is the bile acid receptor TGR5 (Takeda G protein-coupled receptor 5). This G protein-coupled membrane receptor can be found predominantly in the intestine, where it is mainly responsible for the secretion of the incretins glucagon-like peptide 1 (GLP-1) and peptide YY (PYY). The aim of this study was (i) to identify plant extracts with TGR5-activating potential, (ii) to narrow down their activity to the responsible constituents, and (iii) to assess whether the intestinal microbiota produces transformed metabolites with a different activity profile...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28756460/ursolic-acid-activates-the-tgr5-receptor-to-enhance-glp-1-secretion-in-type-1-like-diabetic-rats
#12
Shih-Hsiang Lo, Yingxiao Li, Kai Chun Cheng, Chiang-Shan Niu, Juei-Tang Cheng, Ho-Shan Niu
Endogenous Takeda G-protein-coupled receptor 5 (TGR5), G-protein-coupled bile acid receptor 1 (GPBAR1), regulates glucose metabolism. In animals, TGR5 activation by a chemical agonist may increase incretin secretion and reduce the blood sugar level. Recently, betulinic acid has been suggested to activate TGR5. Ursolic acid is a well-known pentacyclic triterpenoid that is similar to betulinic acid. It is of special interest to determine the potential effect of ursolic acid on TGR5. Therefore, we transfected cultured Chinese hamster ovary (CHO-K1) cells with the TGR5 gene...
July 30, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28669667/transhepatic-bile-acid-kinetics-in-pigs-and-humans
#13
Hannah M Eggink, F Samuel van Nierop, Marieke G Schooneman, Anita Boelen, Andries Kalsbeek, Martijn Koehorst, Gabriella A M Ten Have, L Maurits de Brauw, Albert K Groen, Johannes A Romijn, Nicolaas E P Deutz, Maarten R Soeters
BACKGROUND & AIMS: Bile acids (BAs) play a key role in lipid uptake and metabolic signalling in different organs including gut, liver, muscle and brown adipose tissue. Portal and peripheral plasma BA concentrations increase after a meal. However, the exact kinetics of postprandial BA metabolism have never been described in great detail. We used a conscious porcine model to investigate postprandial plasma concentrations and transorgan fluxes of BAs, glucose and insulin using the para-aminohippuric acid dilution method...
June 19, 2017: Clinical Nutrition: Official Journal of the European Society of Parenteral and Enteral Nutrition
https://www.readbyqxmd.com/read/28646179/herbal-medicine-yinchenhaotang-protects-against-%C3%AE-naphthylisothiocyanate-induced-cholestasis-in-rats
#14
Jingyu Yan, Guoxiang Xie, Chungeng Liang, Yiyang Hu, Aihua Zhao, Fengjie Huang, Ping Hu, Ping Liu, Wei Jia, Xiaoning Wang
Cholestasis is a clinical disorder defined as an impairment of bile flow, and that leads to toxic bile acid (BA) accumulation in hepatocytes. Here, we investigated the hepatoprotective effect of Yinchenhaotang (YCHT), a well-known formulae for the treatment of jaundice and liver disorders, against the cholestasis using the α-naphthylisothiocyanate (ANIT)-induced cholestasis in male Wistar rats. ANIT feeding induced significant cholestasis with substantially increased intrahepatic retention of hydrophobic BAs...
June 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28607110/the-bile-acid-receptor-gpbar1-regulates-the-m1-m2-phenotype-of-intestinal-macrophages-and-activation-of-gpbar1-rescues-mice-from-murine-colitis
#15
Michele Biagioli, Adriana Carino, Sabrina Cipriani, Daniela Francisci, Silvia Marchianò, Paolo Scarpelli, Daniele Sorcini, Angela Zampella, Stefano Fiorucci
GPBAR1 (TGR5 or M-BAR) is a G protein-coupled receptor for secondary bile acids that is highly expressed in monocytes/macrophages. In this study, we aimed to determine the role of GPBAR1 in mediating leukocyte trafficking in chemically induced models of colitis and investigate the therapeutic potential of BAR501, a small molecule agonist for GPBAR1. These studies demonstrated that GPBAR1 gene ablation enhanced the recruitment of classically activated macrophages in the colonic lamina propria and worsened the severity of inflammation...
July 15, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28602676/interactions-between-gut-bacteria-and-bile-in-health-and-disease
#16
REVIEW
Sarah L Long, Cormac G M Gahan, Susan A Joyce
Bile acids are synthesized from cholesterol in the liver and released into the intestine to aid the digestion of dietary lipids. The host enzymes that contribute to bile acid synthesis in the liver and the regulatory pathways that influence the composition of the total bile acid pool in the host have been well established. In addition, the gut microbiota provides unique contributions to the diversity of bile acids in the bile acid pool. Gut microbial enzymes contribute significantly to bile acid metabolism through deconjugation and dehydroxylation reactions to generate unconjugated bile acids and secondary bile acids...
August 2017: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/28596381/a-dual-agonist-of-farnesoid-x-receptor-fxr-and-the-g-protein-coupled-receptor-tgr5-int-767-reverses-age-related-kidney-disease-in-mice
#17
Xiaoxin X Wang, Yuhuan Luo, Dong Wang, Luciano Adorini, Mark Pruzanski, Evgenia Dobrinskikh, Moshe Levi
Even in healthy individuals, renal function gradually declines during aging. However, an observed variation in the rate of this decline has raised the possibility of slowing or delaying age-related kidney disease. One of the most successful interventional measures that slows down and delays age-related kidney disease is caloric restriction. We undertook the present studies to search for potential factors that are regulated by caloric restriction and act as caloric restriction mimetics. Based on our prior studies with the bile acid-activated nuclear hormone receptor farnesoid X receptor (FXR) and G protein-coupled membrane receptor TGR5 that demonstrated beneficial effects of FXR and TGR5 activation in the kidney, we reasoned that FXR and TGR5 could be excellent candidates...
July 21, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28594916/identification-of-key-amino-acid-residues-in-the-htgr5-nomilin-interaction-and-construction-of-its-binding-model
#18
Takashi Sasaki, Moeko Mita, Naho Ikari, Ayane Kuboyama, Shuzo Hashimoto, Tatsuya Kaneko, Masaji Ishiguro, Makoto Shimizu, Jun Inoue, Ryuichiro Sato
TGR5, a member of the G protein-coupled receptor (GPCR) family, is activated by bile acids. Because TGR5 promotes energy expenditure and improves glucose homeostasis, it is recognized as a key target in treating metabolic diseases. We previously showed that nomilin, a citrus limonoid, activates TGR5 and confers anti-obesity and anti-hyperglycemic effects in mice. Information on the TGR5-nomilin interaction regarding molecular structure, however, has not been reported. In the present study, we found that human TGR5 (hTGR5) shows higher nomilin responsiveness than does mouse TGR5 (mTGR5)...
2017: PloS One
https://www.readbyqxmd.com/read/28580281/glucagon-like-peptide-2-promotes-gallbladder-refilling-via-a-tgr5-independent-glp-2r-dependent-pathway
#19
Bernardo Yusta, Dianne Matthews, Grace B Flock, John R Ussher, Brigitte Lavoie, Gary M Mawe, Daniel J Drucker
OBJECTIVE: Glucagon-like peptides (GLPs) are secreted from enteroendocrine cells in response to nutrients and bile acids and control metabolism via actions on structurally-related yet distinct G protein coupled receptors. GLP-1 regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2 enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabetes and obesity, and a GLP-2R agonist is approved to treat short bowel syndrome. Unexpectedly, reports of gallbladder disease have been associated with the use of both GLP-1R and GLP-2R agonists and after bariatric surgery, although the mechanisms remain unknown...
June 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28573213/chemoproteomic-profiling-of-bile-acid-interacting-proteins
#20
Shentian Zhuang, Qiang Li, Lirong Cai, Chu Wang, Xiaoguang Lei
Bile acids (BAs) are a family of endogenous metabolites synthesized from cholesterol in liver and modified by microbiota in gut. Being amphipathic molecules, the major function of BAs is to help with dietary lipid digestion. In addition, they also act as signaling molecules to regulate lipid and glucose metabolism as well as gut microbiota composition in the host. Remarkably, recent discoveries of the dedicated receptors for BAs such as FXR and TGR5 have uncovered a number of novel actions of BAs as signaling hormones which play significant roles in both physiological and pathological conditions...
May 24, 2017: ACS Central Science
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