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https://www.readbyqxmd.com/read/27557342/effects-of-polymorphisms-in-nr1h4-nr1i2-slco1b1-and-abcg2-on-the-pharmacokinetics-of-rosuvastatin-in-healthy-chinese-volunteers
#1
Mei Liu, Xiu-Jun Wu, Gui-Lian Zhao, Ti Zhang, Shan-Sen Xu, Ya-Xin Sun, Feng Qiu, Li-Mei Zhao
The nuclear receptors (NR)-farnesoid X receptor (FXR, NR1H4) and pregnane X receptor (PXR, NR1I2) have important effects on the expression of genes related to the pharmacokinetics (PKs) of rosuvastatin. This study was designed to investigate whether the genetic variants in drug disposition genes (SLCO1B1 and ABCG2) combined with their upstream regulators (NR1H4 and NR1I2) would affect the PKs of rosuvastatin in a Chinese population. Sixty-one healthy male volunteers were enrolled and the plasma concentrations of rosuvastatin were measured using the LC-MS/MS method...
August 22, 2016: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/27383204/the-farnesoid-x-receptor-in-myeloid-cells-controls-cns-autoimmunity-in-an-il-10-dependent-fashion
#2
Stephanie Hucke, Martin Herold, Marie Liebmann, Nicole Freise, Maren Lindner, Ann-Katrin Fleck, Stefanie Zenker, Stephanie Thiebes, Juncal Fernandez-Orth, Dorothea Buck, Felix Luessi, Sven G Meuth, Frauke Zipp, Bernhard Hemmer, Daniel Robert Engel, Johannes Roth, Tanja Kuhlmann, Heinz Wiendl, Luisa Klotz
Innate immune responses by myeloid cells decisively contribute to perpetuation of central nervous system (CNS) autoimmunity and their pharmacologic modulation represents a promising strategy to prevent disease progression in Multiple Sclerosis (MS). Based on our observation that peripheral immune cells from relapsing-remitting and primary progressive MS patients exhibited strongly decreased levels of the bile acid receptor FXR (farnesoid-X-receptor, NR1H4), we evaluated its potential relevance as therapeutic target for control of established CNS autoimmunity...
September 2016: Acta Neuropathologica
https://www.readbyqxmd.com/read/27079614/microrna-192-suppresses-the-expression-of-the-farnesoid-x-receptor
#3
Regina Krattinger, Adrian Boström, Helgi B Schiöth, Wolfgang E Thasler, Jessica Mwinyi, Gerd A Kullak-Ublick
Farnesoid X receptor (FXR, NR1H4) plays an important role in the regulation of bile acid homeostasis in liver and intestine and may exert protective effects against certain forms of cancer such as colon carcinoma. However, the role of FXR in cell growth regulation, apoptosis, and carcinogenesis is still controversial. Similar to FXR, microRNA-192 (miR-192) is mainly expressed in the liver and colon and plays an important role in the pathogenesis of colon carcinoma. In this study, we investigated the extent to which FXR is regulated by miR-192...
June 1, 2016: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/26946349/phenotypic-and-biomarker-evaluation-of-zebrafish-larvae-as-an-alternative-model-to-predict-mammalian-hepatotoxicity
#4
Sandra Verstraelen, Bernard Peers, Walid Maho, Karen Hollanders, Sylvie Remy, Pascale Berckmans, Adrian Covaci, Hilda Witters
Zebrafish phenotypic assays have shown promise to assess human hepatotoxicity, though scoring of liver morphology remains subjective and difficult to standardize. Liver toxicity in zebrafish larvae at 5 days was assessed using gene expression as the biomarker approach, complementary to phenotypic analysis and analytical data on compound uptake. This approach aimed to contribute to improved hepatotoxicity prediction, with the goal of identifying biomarker(s) as a step towards the development of transgenic models for prioritization...
September 2016: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/26888176/mutations-in-the-nuclear-bile-acid-receptor-fxr-cause-progressive-familial-intrahepatic-cholestasis
#5
Natalia Gomez-Ospina, Carol J Potter, Rui Xiao, Kandamurugu Manickam, Mi-Sun Kim, Kang Ho Kim, Benjamin L Shneider, Jennifer L Picarsic, Theodora A Jacobson, Jing Zhang, Weimin He, Pengfei Liu, A S Knisely, Milton J Finegold, Donna M Muzny, Eric Boerwinkle, James R Lupski, Sharon E Plon, Richard A Gibbs, Christine M Eng, Yaping Yang, Gabriel C Washington, Matthew H Porteus, William E Berquist, Neeraja Kambham, Ravinder J Singh, Fan Xia, Gregory M Enns, David D Moore
Neonatal cholestasis is a potentially life-threatening condition requiring prompt diagnosis. Mutations in several different genes can cause progressive familial intrahepatic cholestasis, but known genes cannot account for all familial cases. Here we report four individuals from two unrelated families with neonatal cholestasis and mutations in NR1H4, which encodes the farnesoid X receptor (FXR), a bile acid-activated nuclear hormone receptor that regulates bile acid metabolism. Clinical features of severe, persistent NR1H4-related cholestasis include neonatal onset with rapid progression to end-stage liver disease, vitamin K-independent coagulopathy, low-to-normal serum gamma-glutamyl transferase activity, elevated serum alpha-fetoprotein and undetectable liver bile salt export pump (ABCB11) expression...
2016: Nature Communications
https://www.readbyqxmd.com/read/26878262/recent-progress-on-bile-acid-receptor-modulators-for-treatment-of-metabolic-diseases
#6
Yanping Xu
Bile acids are steroid-derived molecules synthesized in the liver, secreted from hepatocytes into the bile canaliculi, and subsequently stored in the gall bladder. During the feeding, bile flows into the duodenum, where it contributes to the solubilization and digestion of lipid-soluble nutrients. After a meal, bile-acid levels increase in the intestine, liver, and also in the systemic circulation. Therefore, serum bile-acid levels serve as an important sensing mechanism for nutrient and energy. Recent studies have described bile acids as versatile signaling molecules endowed with systemic endocrine functions...
July 28, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26738723/transcriptional-analysis-of-porcine-intestinal-mucosa-infected-with-salmonella-typhimurium-revealed-a-massive-inflammatory-response-and-disruption-of-bile-acid-absorption-in-ileum
#7
Juber Herrera Uribe, Melania Collado-Romero, Sara Zaldívar-López, Cristina Arce, Rocío Bautista, Ana Carvajal, Susanna Cirera, M Gonzalo Claros, Juan J Garrido
Infected pork meat is an important source of non-typhoidal human salmonellosis. Understanding of molecular mechanisms involved in disease pathogenesis is important for the development of therapeutic and preventive strategies. Thus, hereby we study the transcriptional profiles along the porcine intestine during infection with Salmonella Typhimurium, as well as post-transcriptional gene modulation by microRNAs (miRNA). Sixteen piglets were orally challenged with S. Typhimurium. Samples from jejunum, ileum and colon, collected 1, 2 and 6 days post infection (dpi) were hybridized to mRNA and miRNA expression microarrays and analyzed...
January 7, 2016: Veterinary Research
https://www.readbyqxmd.com/read/26526836/bile-acids-in-physiology-pathology-and-pharmacology
#8
REVIEW
Jose J G Marin, Rocio I R Macias, Oscar Briz, Jesus M Banales, Maria J Monte
Bile acids, synthesized by hepatocytes from cholesterol, are specific and quantitatively important organic components of bile, where they are the main driving force of the osmotic process that generates bile flow toward the canaliculus. The bile acid pool comprises a variety of species of amphipathic acidic steroids. They are not mere detergent molecules that play a key role in fat digestion and the intestinal absorption of hydrophobic compounds present in the intestinal lumen after meals, including liposoluble vitamins...
2015: Current Drug Metabolism
https://www.readbyqxmd.com/read/26430762/identification-of-target-genes-involved-in-wound-healing-angiogenesis-of-endothelial-cells-with-the-treatment-of-a-chinese-2-herb-formula
#9
Jacqueline Chor Wing Tam, Chun Hay Ko, Chi Man Koon, Zhang Cheng, Wong Hing Lok, Ching Po Lau, Ping Chung Leung, Kwok Pui Fung, Wai Yee Chan, Clara Bik San Lau
Angiogenesis is vitally important in diabetic wound healing. We had previously demonstrated that a Chinese 2-herb formula (NF3) significantly stimulated angiogenesis of HUVEC in wound healing. However, the molecular mechanism has not yet been elucidated. In line with this, global expression profiling of NF3-treated HUVEC was performed so as to assess the regulatory role of NF3 involved in the underlying signaling pathways in wound healing angiogenesis. The microarray results illustrated that different panels of differentially expressed genes were strictly governed in NF3-treated HUVEC in a time-regulated manner...
2015: PloS One
https://www.readbyqxmd.com/read/26186884/effect-of-roux-en-y-gastric-bypass-on-the-distribution-and-hormone-expression-of-small-intestinal-enteroendocrine-cells-in-obese-patients-with-type-2-diabetes
#10
Nicolai A Rhee, Camilla D Wahlgren, Jens Pedersen, Brynjulf Mortensen, Ebbe Langholz, Erik P Wandall, Steffen U Friis, Peter Vilmann, Sarah J Paulsen, Viggo B Kristiansen, Jacob Jelsing, Louise S Dalbøge, Steen S Poulsen, Jens J Holst, Tina Vilsbøll, Filip K Knop
AIMS/HYPOTHESIS: We studied the impact of Roux-en-Y gastric bypass (RYGB) on the density and hormonal gene expression of small-intestinal enteroendocrine cells in obese patients with type 2 diabetes. METHODS: Twelve patients with diabetes and 11 age- and BMI-matched controls underwent RYGB followed by enteroscopy ~10 months later. Mucosal biopsies taken during surgery and enteroscopy were immunohistochemically stained for glucagon-like peptide-1 (GLP-1), peptide YY (PYY), cholecystokinin (CCK), glucose-dependent insulinotropic polypeptide (GIP) and prohormone convertase 2 (PC2) and the expression of GCG (encoding preproglucagon), PYY, CCK, GIP, GHRL (encoding ghrelin), SCT (encoding secretin), NTS (encoding neurotensin) and NR1H4 (encoding farnesoid X receptor) was evaluated...
October 2015: Diabetologia
https://www.readbyqxmd.com/read/26055905/cross-talk-between-bile-acids-and-intestinal-microbiota-in-host-metabolism-and-health
#11
REVIEW
Yang-fan Nie, Jun Hu, Xiang-hua Yan
Bile acid (BA) is de novo synthesized exclusively in the liver and has direct or indirect antimicrobial effects. On the other hand, the composition and size of the BA pool can be altered by intestinal microbiota via the biotransformation of primary BAs to secondary BAs, and subsequently regulate the nuclear farnesoid X receptor (FXR; NR1H4). The BA-activated FXR plays important roles in BA synthesis and metabolism, glucose and lipid metabolism, and even hepatic autophagy. BAs can also play a role in the interplays among intestinal microbes...
June 2015: Journal of Zhejiang University. Science. B
https://www.readbyqxmd.com/read/26045277/nuclear-receptor-variants-in-liver-disease
#12
REVIEW
Vincent Zimmer, Roman Liebe, Frank Lammert
This snapshot reviews the current state of knowledge on genetic variants of nuclear receptors (NRs) involved in regulating various aspects of liver metabolism. Interindividual differences in responses to diet and other 'in-' and environmental stressors can be caused by variants in components of the NR regulatory gene network. We recapitulate recent evidence for the application of NRs in genetic diagnosis of monogenic liver disease. Genetic analysis of multifactorial liver diseases, such as nonalcoholic fatty liver disease and diabetes mellitus, pinpoints key players in disease predisposition and progression...
2015: Digestive Diseases
https://www.readbyqxmd.com/read/25948514/modulation-of-cholesterol-related-gene-expression-by-ergosterol-and-ergosterol-enriched-extracts-obtained-from-agaricus-bisporus
#13
Alicia Gil-Ramírez, Víctor Caz, Roberto Martin-Hernandez, Francisco R Marín, Carlota Largo, Arantxa Rodríguez-Casado, María Tabernero, Alejandro Ruiz-Rodríguez, Guillermo Reglero, Cristina Soler-Rivas
PURPOSE: To investigate the effect of two extracts obtained from Agaricus bisporus on the mRNA expression of cholesterol-related genes. One of the extracts contained ergosterol and other fungal sterols (SFE) and the other contained β-glucans and fungal sterols (EβG). METHODS: Firstly, the dietary mixed micelles (DMMs) generated after in vitro digestion of standards and SFE were applied to Caco2 cells. Then, the lower compartment after a Caco2-transport experiment was applied to HepG2 cells...
April 2016: European Journal of Nutrition
https://www.readbyqxmd.com/read/25869321/a-novel-formulation-of-veggies-with-potent-liver-detoxifying-activity
#14
Mohit M Jain, Nirmala Kumari, Geeta Rai
LXR (encoded by NR1H2 and 3) and FXR (known as bile acid receptor) encoded by NR1H4 (nuclear receptor subfamily 1, group H and member 4) are nuclear receptors in humans and are important regulators of bile acid production, cholesterol, fatty acid and glucose homeostasis hence responsible for liver detoxification. Several strategies for drug design with numerous ligands for this target have failed owing to the inability of the ligand to access the target/receptor or their early metabolisation. In this work, we have evaluated FXR and LXR structure bound with agonist and compared the binding energy affinity of active ligands present in live green-real veggies with reference drugs (ligands) present in the market...
2015: International Journal of Computational Biology and Drug Design
https://www.readbyqxmd.com/read/25733650/high-folic-acid-consumption-leads-to-pseudo-mthfr-deficiency-altered-lipid-metabolism-and-liver-injury-in-mice
#15
Karen E Christensen, Leonie G Mikael, Kit-Yi Leung, Nancy Lévesque, Liyuan Deng, Qing Wu, Olga V Malysheva, Ana Best, Marie A Caudill, Nicholas D E Greene, Rima Rozen
BACKGROUND: Increased consumption of folic acid is prevalent, leading to concerns about negative consequences. The effects of folic acid on the liver, the primary organ for folate metabolism, are largely unknown. Methylenetetrahydrofolate reductase (MTHFR) provides methyl donors for S-adenosylmethionine (SAM) synthesis and methylation reactions. OBJECTIVE: Our goal was to investigate the impact of high folic acid intake on liver disease and methyl metabolism. DESIGN: Folic acid-supplemented diet (FASD, 10-fold higher than recommended) and control diet were fed to male Mthfr(+/+) and Mthfr(+/-) mice for 6 mo to assess gene-nutrient interactions...
March 2015: American Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/25719402/chronic-activation-of-fxr-in-transgenic-mice-caused-perinatal-toxicity-and-sensitized-mice-to-cholesterol-toxicity
#16
Qiuqiong Cheng, Yuka Inaba, Peipei Lu, Meishu Xu, Jinhan He, Yueshui Zhao, Grace L Guo, Ramalinga Kuruba, Rona de la Vega, Rhobert W Evans, Song Li, Wen Xie
The nuclear receptor farnesoid X receptor (FXR) (nuclear receptor subfamily 1, group H, member 4, or NR1H4) is highly expressed in the liver and intestine. Previous reports have suggested beneficial functions of FXR in the homeostasis of bile acids, lipids, and glucose, as well as in promoting liver regeneration and inhibiting carcinogenesis. To investigate the effect of chronic FXR activation in vivo, we generated transgenic mice that conditionally and tissue specifically express the activated form of FXR in the liver and intestine...
April 2015: Molecular Endocrinology
https://www.readbyqxmd.com/read/25623328/investigation-of-the-dominant-positive-effect-of-porcine-farnesoid-x-receptor-fxr-splice-variant-1
#17
Matthew A Gray, E James Squires
Pigs are well recognized as a model for humans in research studies due to similarities in metabolism and physiology between the two species. The potential for pigs to model humans in studying metabolic diseases is highly dependent on similarities in hepatic metabolism between the two species, including similarities in the farnesoid X receptor (FXR; NR1H4) which regulate bile acid homeostasis. During initial cloning of porcine FXR (pFXR), an alternative splice variant (pFXR-SV1) was isolated which contained a four amino acid (MYTG) insert that exerted a dominant positive effect on the wild type receptor (pFXR-WT)...
April 10, 2015: Gene
https://www.readbyqxmd.com/read/25466967/expression-of-drug-transporters-and-drug-metabolizing-enzymes-in-the-bladder-urothelium-in-man-and-affinity-of-the-bladder-spasmolytic-trospium-chloride-to-transporters-likely-involved-in-its-pharmacokinetics
#18
Maria Bexten, Stefan Oswald, Markus Grube, Jia Jia, Tanja Graf, Uwe Zimmermann, Kathrin Rodewald, Oliver Zolk, Ulrich Schwantes, Werner Siegmund, Markus Keiser
The cationic, water-soluble quaternary trospium chloride (TC) is incompletely absorbed from the gut and undergoes wide distribution but does not pass the blood-brain barrier. It is secreted by the kidneys, liver, and intestine. To evaluate potential transport mechanisms for TC, we measured affinity of the drug to the human uptake and efflux transporters known to be of pharmacokinetic relevance. Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured...
January 5, 2015: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/25388534/recent-advances-in-non-steroidal-fxr-antagonists-development-for-therapeutic-applications
#19
REVIEW
Huang Huang, Yong Xu, Jin Zhu, Jian Li
Farnesoid X receptor (FXR, NR1H4), a nuclear receptor (NR) highly expressed in the liver, intestine, kidney, adrenal glands and other cholesterol-rich tissues, functions as the master regulator for bile acid homeostasis. FXR, which regulates the expression of genes encoding proteins involved in cholesterol homeostasis, plays an essential role in regulating cholesterol, lipid, and glucose metabolism. Recently, some FXR agonists are reported to have low selectivity on NRs, which forces the researchers to move their eyes onto the development of FXR antagonists with high selectivity...
2014: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/25383539/nutrient-sensing-nuclear-receptors-coordinate-autophagy
#20
Jae Man Lee, Martin Wagner, Rui Xiao, Kang Ho Kim, Dan Feng, Mitchell A Lazar, David D Moore
Autophagy is an evolutionarily conserved catabolic process that recycles nutrients upon starvation and maintains cellular energy homeostasis. Its acute regulation by nutrient-sensing signalling pathways is well described, but its longer-term transcriptional regulation is not. The nuclear receptors peroxisome proliferator-activated receptor-α (PPARα) and farnesoid X receptor (FXR) are activated in the fasted and fed liver, respectively. Here we show that both PPARα and FXR regulate hepatic autophagy in mice...
December 4, 2014: Nature
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