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https://www.readbyqxmd.com/read/29450114/flavonoid-rich-extract-of-chromolaena-odorata-modulate-circulating-glp-1-in-wistar-rats-computational-evaluation-of-tgr5-involvement
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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...
January 11, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29339725/tgr5-signalling-promotes-mitochondrial-fission-and-beige-remodelling-of-white-adipose-tissue
#7
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
#8
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...
January 16, 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
#9
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
#10
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
https://www.readbyqxmd.com/read/29259742/synthesis-and-biological-evaluation-of-a-series-of-bile-acid-derivatives-as-fxr-agonists-for-treatment-of-nash
#11
Hualing Xiao, Peng Li, Xiaolin Li, Haiying He, Jianhua Wang, Fengxun Guo, Jiliang Zhang, Luxia Wei, Hongmei Zhang, Yueyuan Shi, Lijuan Hou, Liang Shen, Zhengxia Chen, Chunyan Du, Shouliang Fu, Pengtao Zhang, Fei Hao, Ping Wang, Deming Xu, Wei Liang, Xin Tian, Aiming Zhang, Xingdong Cheng, Ling Yang, Xiangjian Wang, Xiquan Zhang, Jian Li, Shuhui Chen
Farnesoid X receptor (FXR) has become a particularly attractive target for the discovery of drugs for the treatment of liver and metabolic diseases. Obeticholic acid (INT-747), a FXR agonist, has advanced into clinical phase III trials in patients with nonalcoholic steatohepatitis (NASH), but adverse effects (e.g., pruritus, LDL increase) were observed. Pruritus might be induced by Takeda G-protein-coupled receptor 5 (TGR5, GPBAR1), and there are chances to develop FXR agonists with higher selectivity over TGR5...
December 14, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29233934/chronic-infusion-of-taurolithocholate-into-the-brain-increases-fat-oxidation-in-mice
#12
Hannah M Eggink, Lauren L Tambyrajah, Rosa van den Berg, Isabel Mol, Jose K van den Heuvel, Martijn Koehorst, Albert K Groen, Anita Boelen, Andries Kalsbeek, Johannes A Romijn, Patrick C N Rensen, Sander Kooijman, Maarten R Soeters
Bile acids can function in the postprandial state as circulating signaling molecules in the regulation of glucose and lipid metabolism via the transmembrane receptor TGR5 and nuclear receptor FXR. Both receptors are present in the central nervous system, but their function in the brain is unclear. Therefore, we investigated the effects of intracerebroventricular (icv) administration of taurolithocholate (tLCA), a strong TGR5 agonist, and GW4064, a synthetic FXR agonist, on energy metabolism. We determined the effects of chronic icv infusion of tLCA, GW4064, or vehicle on energy expenditure, body weight and composition as well as tissue specific fatty acid uptake in mice equipped with osmotic minipumps...
December 12, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/29203510/mechanisms-to-elevate-endogenous-glucagon-like-peptide-1-glp-1-beyond-injectable-glp-1-analogues-and-metabolic-surgery
#13
Daniel A Briere, Ana B Bueno, Ellen J Gunn, M Dodson Michael, Kyle W Sloop
Therapeutic engineering of glucagon-like peptide-1 (GLP-1) has enabled development of new medicines to treat type 2 diabetes mellitus. These injectable analogues achieve robust glycemic control by increasing concentrations of 'GLP-1 equivalents' (∼50 pM). Similar levels of endogenous GLP-1 occur following gastric bypass surgery, and mechanistic studies indicate glucose lowering by these procedures is driven by GLP-1. Therefore, due to the remarkable signaling and secretory capacity of the GLP-1 system, we sought to discover mechanisms that raise GLP-1 pharmacologically...
December 4, 2017: Diabetes
https://www.readbyqxmd.com/read/29200718/%C3%AE-glucosidase-inhibitory-activity-from-ethyl-acetate-extract-of-antidesma-bunius-l-spreng-stem-bark-containing-triterpenoids
#14
Marista Gilang Mauldina, Rani Sauriasari, Berna Elya
Background: Buni (Antidesma bunius [L.] Spreng) has been used as a traditional antidiabetic agent in Asia. Objective: The mechanism of antidiabetic properties was studied in this study by determine its α-glucosidase inhibitory activity. Method: Inhibition of α-glucosidase was performed in all fraction of Buni stem bark with acarbose and miglitol as standards. The half maximal inhibitory concentration (IC50) value of acarbose and miglitol was 5...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29188025/recent-advances-in-understanding-bile-acid-homeostasis
#15
REVIEW
John Yl Chiang
Bile acids are derived from cholesterol to facilitate intestinal nutrient absorption and biliary secretion of cholesterol. Recent studies have identified bile acids as signaling molecules that activate nuclear farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (Gpbar-1, also known as TGR5) to maintain metabolic homeostasis and protect liver and other tissues and cells from bile acid toxicity. Bile acid homeostasis is regulated by a complex mechanism of feedback and feedforward regulation that is not completely understood...
2017: F1000Research
https://www.readbyqxmd.com/read/29173647/diet-induced-obesity-and-weight-loss-alter-bile-acid-concentrations-and-bile-acid-sensitive-gene-expression-in-insulin-target-tissues-of-c57bl-6j-mice
#16
Michael R La Frano, Angelina Hernandez-Carretero, Natalie Weber, Kamil Borkowski, Theresa L Pedersen, Olivia Osborn, John W Newman
Bile acids (BAs) influence the metabolism of glucose, lipids, and energy expenditure. We hypothesized that BA concentrations and related gene expression would be altered in lean (low-fat diet fed; LFD) vs diet-induced obese (high-fat diet fed; HFD) groups of mice and that some detected changes would remain after weight loss in an HFD group switched to the LFD (SW). Taurine conjugates dominated the bile acid composition of the liver, epididymal white adipose tissue (eWAT), and hypothalamus, with the latter having lower levels (~95%, ~95%, and ~80%, respectively; P<...
October 2017: Nutrition Research
https://www.readbyqxmd.com/read/29163019/bile-acid-signaling-pathways-from-the-enterohepatic-circulation-to-the-central-nervous-system
#17
REVIEW
Kim L Mertens, Andries Kalsbeek, Maarten R Soeters, Hannah M Eggink
Bile acids are best known as detergents involved in the digestion of lipids. In addition, new data in the last decade have shown that bile acids also function as gut hormones capable of influencing metabolic processes via receptors such as FXR (farnesoid X receptor) and TGR5 (Takeda G protein-coupled receptor 5). These effects of bile acids are not restricted to the gastrointestinal tract, but can affect different tissues throughout the organism. It is still unclear whether these effects also involve signaling of bile acids to the central nervous system (CNS)...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29150974/reciprocal-interactions-between-bile-acids-and-gut-microbiota-in-human-liver-diseases
#18
REVIEW
Tadashi Ikegami, Akira Honda
The gut microbiota (GM) play a central role in their hosts' metabolism of bile acids (BAs) by regulating deconjugation, dehydroxylation, dehydrogenation, and epimerization reactions to generate unconjugated free BAs and secondary BAs. These BAs generated by the GM are potent signaling molecules that interact with BA receptors, such as the farnesoid X receptor (FXR) and Takeda G-protein-coupled receptor 5 (TGR5). Each BA has a differential affinity to these receptors; therefore, alterations in BA composition by GM could modify the intensity of receptor signaling...
November 18, 2017: Hepatology Research: the Official Journal of the Japan Society of Hepatology
https://www.readbyqxmd.com/read/29123941/bile-acids-as-global-regulators-of-hepatic-nutrient-metabolism
#19
Phillip B Hylemon, Kazuaki Takabe, Mikhail Dozmorov, Masayuki Nagahashi, Huiping Zhou
Bile acids (BA) are synthesized from cholesterol in the liver. They are essential for promotion of the absorption of lipids, cholesterol, and lipid-soluble vitamins from the intestines. BAs are hormones that regulate nutrient metabolism by activating nuclear receptors (farnesoid X receptor (FXR), pregnane X receptor, vitamin D) and G protein-coupled receptors (e.g., TGR5, sphingosine-1-phosphate receptor 2 (S1PR2)) in the liver and intestines. In the liver, S1PR2 activation by conjugated BAs activates the extracellular signal-regulated kinase 1/2 and AKT signaling pathways, and nuclear sphingosine kinase 2...
June 2017: Liver Research
https://www.readbyqxmd.com/read/29118282/the-role-of-bile-acids-in-glucose-metabolism-and-their-relation-with-diabetes
#20
José Alberto González-Regueiro, Lidia Moreno-Castañeda, Misael Uribe, Norberto C Chávez-Tapia
Bile acids (BAs), the end products of cholesterol catabolism, are essential for the absorption of lipids and fat-soluble vitamins; but they have also emerged as novel signaling molecules that act as metabolic regulators. It has been well described that the enterohepatic circulation, a nuclear (FXR) and a cytoplasmic (TGR5/M-BAR) receptor aid in controlling hepatic bile acid synthesis. Modulating bile acid synthesis greatly impacts in metabolism, because these receptors also are implicated in glucose, lipid, and energy expenditure...
November 2017: Annals of Hepatology
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