182 results match your criteria liver fbpase


Long-term co-administration of sodium nitrite and sodium hydrosulfide inhibits hepatic gluconeogenesis in male type 2 diabetic rats: Role of PI3K-Akt-eNOS pathway.

Life Sci 2021 Jan 16;265:118770. Epub 2020 Nov 16.

Endocrine Physiology Research Center, Research Institute for Endocrine Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Electronic address:

Objective: A deficiency in hydrogen sulfide (HS) and nitric oxide (NO) contributes to the development of type 2 diabetes (T2D). An inhibitory effect on liver gluconeogenesis has been reported in rats with T2D with co-administration of sodium nitrite and sodium hydrosulfide (NaSH); the underlying mechanisms have however not yet been elucidated. The aim of this study is to determine the long-term effects of co-administering sodium nitrite and NaSH on expression of genes involved in liver gluconeogenesis in rats with T2D. Read More

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January 2021

Effects of chronic glyphosate exposure on antioxdative status, metabolism and immune response in tilapia (GIFT, Oreochromis niloticus).

Comp Biochem Physiol C Toxicol Pharmacol 2021 Jan 28;239:108878. Epub 2020 Aug 28.

Wuxi Fisheries College, Nanjing Agricultural University, Wuxi 214081, China; Key Laboratory of Freshwater Fisheries and Germplasm Resources Utilization, Ministry of Agriculture and Rural Affairs, Freshwater Fisheries Research Center, Chinese Academy of Fishery Sciences, Wuxi 214081, China; International Joint Research Laboratory for Fish Immunopharmacology, Freshwater Fisheries Research Center, Chinese Academy of Fishery Sciences, Wuxi 214081, China. Electronic address:

Glyphosate (Gly) is an active ingredient of herbicide, its underlying toxicity on fish is still unclear. The aim of this study was to evaluate chronic toxicity of Gly on tilapia via determining antioxidative status, metabolism, inflammation and immune response. The fish were exposed to different concentrations of Gly (0, 0. Read More

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January 2021

Discovery of -Arylsulfonyl-Indole-2-Carboxamide Derivatives as Potent, Selective, and Orally Bioavailable Fructose-1,6-Bisphosphatase Inhibitors-Design, Synthesis, Glucose Lowering Effects, and X-ray Crystal Complex Analysis.

J Med Chem 2020 09 12;63(18):10307-10329. Epub 2020 Sep 12.

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Liver fructose-1,6-bisphosphatase (FBPase) is a key enzyme in the gluconeogenesis pathway. Inhibiting FBPase activity represents a potential treatment for type 2 diabetes mellitus. A series of novel -arylsulfonyl-4-arylamino-indole-2-carboxamide derivatives have been disclosed as FBPase inhibitors. Read More

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September 2020

Fetal expression of genes related to metabolic function is impacted by supplementation of ground beef and sucrose during gestation in a swine model.

J Anim Sci 2020 Aug;98(8)

Department of Animal Sciences, North Dakota State University, Fargo, ND.

To determine the effects of maternal supplementation on the mRNA abundance of genes associated with metabolic function in fetal muscle and liver, pregnant sows (Landrace × Yorkshire; initial body weight (BW) 221.58 ± 33.26 kg; n = 21) fed a complete gestation diet (corn-soybean meal based diet, CSM) were randomly assigned to 1 of 4 isocaloric supplementation treatments: control (CON, 378 g/d CSM, n = 5), sucrose (SUGAR, 255 g/d crystalized sugar, n = 5), cooked ground beef (BEEF, 330 g/d n = 6), or BEEF + SUGAR (B+S, 165 g/d cooked ground beef and 129 g/d crystalized sugar, n = 5), from days 40 to 110 of gestation. Read More

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Structural Specificity of Flavonoids in the Inhibition of Human Fructose 1,6-Bisphosphatase.

J Nat Prod 2020 05 4;83(5):1541-1552. Epub 2020 May 4.

LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.

Liver fructose 1,6-bisphosphatase (FBPase) is a recognized regulatory enzyme of the gluconeogenesis pathway, which has emerged as a valid target to control gluconeogenesis-mediated overproduction of glucose. As such, the management of diabetes with FBPase inhibitors represents a potential alternative for the currently used antidiabetic agents. In this study, the FBPase inhibition of a panel of 55 structurally related flavonoids was tested, through a microanalysis screening system. Read More

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Dapagliflozin not only improves hepatic injury and pancreatic endoplasmic reticulum stress, but also induces hepatic gluconeogenic enzymes expression in obese rats.

Clin Sci (Lond) 2019 12;133(23):2415-2430

Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai, Thailand.

Background: With an increasing prevalence of obesity and metabolic syndrome, exploring the effects and delineating the mechanisms of possible therapeutic agents are of critical importance. We examined the effects of SGLT2 inhibitor-dapagliflozin on insulin resistance, hepatic gluconeogenesis, hepatic injury and pancreatic ER stress in high-fat diet-induced obese rats.

Materials And Methods: Male Wistar rats were fed with normal diet (ND) or high-fat diet for 16 weeks. Read More

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December 2019

High dietary lipid level alters the growth, hepatic metabolism enzyme, and anti-oxidative capacity in juvenile largemouth bass Micropterus salmoides.

Fish Physiol Biochem 2020 Feb 14;46(1):125-134. Epub 2019 Sep 14.

Key Laboratory of Freshwater Fish Reproduction and Development (Ministry of Education), College of Animal Science and Technology, Southwest University, Chongqing, 400715, People's Republic of China.

The present study was conducted to investigate the effects of high dietary lipid levels on growth, metabolism, antioxidant capacity, and immune responses of largemouth bass. Fish (initial body weight 13.38 ± 0. Read More

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February 2020

6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase and small chemical activators affect enzyme activity of activating glucokinase mutants by distinct mechanisms.

Biochem Pharmacol 2019 10 27;168:149-161. Epub 2019 Jun 27.

Institute of Medical Biochemistry and Molecular Biology, University Medicine, University of Rostock, 18057 Rostock, Germany; Department Life, Light & Matter, University of Rostock, Germany. Electronic address:

Glucokinase (GK), a monomeric glucose-phosphorylating enzyme characterised by high structural flexibility, acts as a glucose sensor in pancreatic beta cells and liver. Pharmaceutical efforts to control the enzyme are hampered by an incomplete understanding of GK regulation. We investigated GK characteristics of wild-type and activating S64Y and G68V mutant proteins in the presence of various combinations of the synthetic activators RO-28-1675 and compound A, the endogenous activator fructose-2,6-bisphosphatase (FBPase-2), and the inhibitor mannoheptulose. Read More

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October 2019

Linseed oil can decrease liver fat deposition and improve antioxidant ability of juvenile largemouth bass, Micropterus salmoides.

Fish Physiol Biochem 2019 Oct 3;45(5):1513-1521. Epub 2019 Apr 3.

Key Laboratory of Freshwater Fish Reproduction and Development (Ministry of Education), College of Animal Science and Technology, Southwest University, Chongqing, 400715, People's Republic of China.

A feeding trial was conducted to evaluate the effect of linseed oil (LO) on growth, plasma biochemistry, hepatic metabolism enzymes, and antioxidant capacity of juvenile largemouth bass, Micropterus salmoides. Four isonitrogenous (crude protein, 45%) and isoenergetic (gross energy, 18 MJ/kg) diets were formulated by replacing 0 (the control), 33.3%, 66. Read More

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October 2019

A novel berberine-metformin hybrid compound exerts therapeutic effects on obese type 2 diabetic rats.

Clin Exp Pharmacol Physiol 2019 06 21;46(6):533-544. Epub 2019 Apr 21.

Academy of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China.

In this study, we investigated the biological activities of a novel berberine-metformin hybrid compound (BMH473) as an anti-diabetic agent. BMH473 exhibited significant anti-hyperglycaemic and anti-hyperlipidaemic effects on T2DM rats. In white adipose tissue, BMH473 reduced the perirenal and epididymal adipose tissue mass and modulated the lesions in perirenal adipose tissue, by inhibiting the protein expressions of PPAR-Ɣ, C/EBP-α and SREBP-1c as well as the mRNA expressions of lipogenic genes. Read More

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Genetic analysis of patients with fructose-1,6-bisphosphatase deficiency.

Gene 2019 May 9;699:102-109. Epub 2019 Mar 9.

Post Graduate Program in Genetics and Molecular Biology, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil; BRAIN Laboratory, Center for Experimental Research (CPE), Hospital de Clínicas de Porto Alegre (HCPA), Porto Alegre, RS, Brazil; Departamento de Genética, Instituto de Biociências, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil; Medical Genetics Service, HCPA, Porto Alegre, RS, Brazil.

Introduction: Fructose-1,6-bisphosphatase deficiency (FBPase deficiency) is a rare inborn error of metabolism that affects gluconeogenesis. Ketotic hypoglycemia is the main symptom and can occur at any age, usually after long periods of fasting or during illness. The diagnosis may be achieved by measurement of the enzyme activity in a liver sample, but FBP1 analysis has become the most common approach. Read More

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Development of prediction model for fructose- 1,6- bisphosphatase inhibitors using the Monte Carlo method.

SAR QSAR Environ Res 2019 Mar 19;30(3):145-159. Epub 2019 Feb 19.

a Department of Pharmaceutical Sciences , Guru Jambheshwar University of Science & Technology , Hisar , India.

Fructose-1,6-bisphosphatase (FBPase) is an enzyme important for regulation of gluconeogenesis, which is a major process in the liver responsible for glucose production. Inhibition of FBPase enzyme causing blockage of the gluconeogenesis process represents a newer scheme in the progress of anti-diabetic drugs. The current research describes the development of hybrid optimal descriptors-based quantitative structure-activity relationship (QSAR) models intended for a set of 62 FBPase inhibitors with the Monte Carlo method. Read More

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Hypoglycemic and Hypolipidemic Effects of Mycelial Extract from Solid-State Culture in A Rat Model of Type 2 Diabetes.

Nutrients 2019 Jan 30;11(2). Epub 2019 Jan 30.

State Key Laboratory of Agricultural Microbiology, College of Life Science and Technology, Huazhong Agricultural University, Wuhan 430070, China.

Hypoglycemic and hypolipidemic effects of have been observed in numerous studies, but the underlying molecular mechanisms are unclear. In this study, we prepared extract (PLE) from mycelia of solid-state culture, and evaluated its hypoglycemic and hypolipidemic effects in rat models of high-fat diet (HFD)-induced and low-dose streptozotocin (STZ)-induced type 2 diabetes. PLE treatment effectively reduced blood glucose levels, and improved insulin resistance and lipid and lipoprotein profiles. Read More

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January 2019

Metformin improves the glucose homeostasis of Wuchang bream fed high-carbohydrate diets: a dynamic study.

Endocr Connect 2019 Mar;8(3):182-194

Key Laboratory of Aquatic Nutrition and Feed Science of Jiangsu Province, College of Animal Science and Technology, Nanjing Agricultural University, Nanjing, China.

After a 12-week feeding trial, the glucose tolerance test was performed in Megalobrama amblycephala to evaluate the effects of metformin on the metabolic responses of glycolipids. Plasma insulin peaked at 2 h, then decreased to the basal value at 8-12 h post-injection. Plasma triglyceride levels and liver glycogen contents of the control group was decreased significantly during the first 2 and 1 h, respectively. Read More

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Scutellariae Radix and Coptidis Rhizoma Improve Glucose and Lipid Metabolism in T2DM Rats via Regulation of the Metabolic Profiling and MAPK/PI3K/Akt Signaling Pathway.

Int J Mol Sci 2018 Nov 18;19(11). Epub 2018 Nov 18.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China.

Scutellariae Radix (SR) and Coptidis Rhizoma (CR) have often been combined to cure type 2 diabetes mellitus (T2DM) in the clinical practice for over thousands of years, but their compatibility mechanism is not clear. Mitogen-activated protein kinase (MAPK) signaling pathway has been suggested to play a critical role during the process of inflammation, insulin resistance, and T2DM. This study was designed to investigate their compatibility effects on T2DM rats and explore the underlying mechanisms by analyzing the metabolic profiling and MAPK/PI3K/Akt signaling pathway. Read More

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November 2018

In silico screening of a novel scaffold for fructose-1,6-bisphosatase (FBPase) inhibitors.

J Mol Graph Model 2019 01 20;86:142-148. Epub 2018 Oct 20.

International Cooperation Base of Pesticide and Green Synthesis (Hubei), Key Laboratory of Pesticide & Chemical Biology (CCNU), Ministry of Education, Department of Chemistry, Central China Normal University, Wuhan, 430079, China. Electronic address:

Fructose-1, 6-bisphosphatase (FBPase) has been regarded as an attractive drug target to control blood glucose against Type 2 diabetes (T2D). In this study, by using the strategy of pharmacophore-based virtual screening, a novel scaffold inhibitor targeted the AMP allosteric site of human liver FBPase were screened, their inhibitory activities were further tested. The experimental results showed that compound H27 exhibited high inhibitory activities with the IC value of 5. Read More

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January 2019

Resveratrol Improves the Energy Sensing and Glycolipid Metabolism of Blunt Snout Bream Fed High-Carbohydrate Diets by Activating the AMPK-SIRT1-PGC-1α Network.

Front Physiol 2018 11;9:1258. Epub 2018 Sep 11.

Key Laboratory of Aquatic Nutrition and Feed Science of Jiangsu Province, College of Animal Science and Technology, Nanjing Agricultural University, Nanjing, China.

This study investigated the effects of resveratrol on the growth performance, energy sensing, glycolipid metabolism and glucose and insulin load of blunt snout bream fed high-carbohydrate diets. Fish (39.44 ± 0. Read More

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September 2018

Effects of glucose administration on glucose and lipid metabolism in two strains of gibel carp (Carassius gibelio).

Gen Comp Endocrinol 2018 Oct 23;267:18-28. Epub 2018 May 23.

State Key Laboratory of Freshwater Ecology and Biotechnology, Institute of Hydrobiology, Chinese Academy of Sciences, Wuhan, Hubei, China. Electronic address:

We compared the glucose clearance ability of gibel carp CAS III (A strain) with gibel carp Dongting (DT strain). A previous study suggested that these two strains responded to insulin differently. As insulin plays an important role in glucose utilization, we hypothesized that the ability to eliminate excess glucose after a glucose load would differ between A strain and DT strain. Read More

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October 2018

Gluconeogenesis during starvation and refeeding phase is affected by previous dietary carbohydrates levels and a glucose stimuli during early life in Siberian sturgeon ().

Anim Nutr 2017 Sep 15;3(3):284-294. Epub 2017 Jun 15.

Institute of Animal Science, Chinese Academy of Agricultural Sciences, Beijing 100193, China.

Gluconeogenesis responses was assessed during a short starvation period and subsequent refeeding in Siberian sturgeon () previously fed different dietary carbohydrates levels and experienced to a glucose stimuli during early life. The sturgeon larvae were previously fed either a high glucose diet (G) or a low glucose diet (F) from the first feeding to yolk absorption (8 to 12 d post-hatching [dph]). Each group of fish was sub-divided into 2 treatments at 13 dph and was fed either a high-carbohydrate diet (H) or a low carbohydrate diet (L) until 20 wk. Read More

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September 2017

Effect of high dietary starch levels on growth, hepatic glucose metabolism, oxidative status and immune response of juvenile largemouth bass, Micropterus salmoides.

Fish Shellfish Immunol 2018 Jul 21;78:121-126. Epub 2018 Apr 21.

Key Laboratory of Freshwater Fish Reproduction and Development (Ministry of Education), College of Animal Science and Technology, Southwest University, Chongqing 400715, PR China.

An experimental trial was conducted to investigate the effects of high dietary starch levels on growth, hepatic glucose metabolism enzyme, antioxidant capacity and immune responses of largemouth bass, Micropterus salmoides. Fish (initial body weight: 16.9 ± 0. Read More

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International practices in the dietary management of fructose 1-6 biphosphatase deficiency.

Orphanet J Rare Dis 2018 01 25;13(1):21. Epub 2018 Jan 25.

Birmingham Women's and Children's Hospital, Birmingham, UK.

Background: In fructose 1,6 bisphosphatase (FBPase) deficiency, management aims to prevent hypoglycaemia and lactic acidosis by avoiding prolonged fasting, particularly during febrile illness. Although the need for an emergency regimen to avoid metabolic decompensation is well established at times of illness, there is uncertainty about the need for other dietary management strategies such as sucrose or fructose restriction. We assessed international differences in the dietary management of FBPase deficiency. Read More

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January 2018

Molecular characterization of fructose-1,6-bisphosphatase 1b in blunt snout bream Megalobrama amblycephala and the transcriptional response to glucose loading after the adaptation to high-carbohydrate diets.

Fish Physiol Biochem 2017 Oct 4;43(5):1337-1349. Epub 2017 May 4.

Key Laboratory of Aquatic Nutrition and Feed Science of Jiangsu Province, College of Animal Science and Technology, Nanjing Agricultural University, No. 1 Weigang Road, Nanjing, 210095, Jiangsu Province, People's Republic of China.

This study aimed to characterize the full-length complementary DNA (cDNA) of fructose-1,6-bisphosphatase 1b (FBP1b) from fish Megalobrama amblycephala, and investigate its transcriptional response to glucose administration after the adaptation to high-carbohydrate diets. The cDNA obtained covered 1435 bp with an open reading frame of 1014 bp. Sequence alignment and phylogenetic analysis revealed a high degree of conservation (76-96%) among most fish and other vertebrates, retaining one N-linked glycosylation site, one N-terminal acetylation site, 13 phosphorylation sites, one fructose-1,6-bisphosphatase (FBPase) active site, five metal-binding sites, four substrate-binding sites, and several AMP-binding sites. Read More

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October 2017

Metabolic and cellular stress responses of catfish, Horabagrus brachysoma (Günther) acclimated to increasing temperatures.

J Therm Biol 2017 Apr 7;65:32-40. Epub 2017 Feb 7.

Division of Fish Nutrition and Biochemistry, ICAR-Central Institute of Fisheries Education, Versova, Mumbai 400061, India.

We investigated the metabolic and cellular stress responses in an endemic catfish Horabagrus brachysoma acclimated to ambient (26°C), 31, 33 and 36°C for 30 days. After acclimation, fish were sampled to investigate changes in the levels of blood glucose, tissue glycogen and ascorbic acid, activities of enzymes involved in glycolysis (LDH), citric acid cycle (MDH), gluconeogenesis (FBPase and G6Pase), pentose phosphate pathway (G6PDH), protein metabolism (AST and ALT), phosphate metabolism (ACP and ALP) and energy metabolism (ATPase), and HSP70 levels in various tissues. Acclimation to higher temperatures (33 and 36°C) significantly increased activities of LDH, MDH, ALP, ACP, AST, ALT and ATPase and blood glucose levels, whereas decreased the G6PDH enzyme activity and, tissue glycogen and ascorbic acid. Read More

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Quadruple space-group ambiguity owing to rotational and translational noncrystallographic symmetry in human liver fructose-1,6-bisphosphatase.

Acta Crystallogr D Struct Biol 2016 11 28;72(Pt 11):1212-1224. Epub 2016 Oct 28.

pRED, Therapeutic Modalities, F. Hoffmann-La Roche, 4070 Basel, Switzerland.

Fructose-1,6-bisphosphatase (FBPase) is a key regulator of gluconeogenesis and a potential drug target for type 2 diabetes. FBPase is a homotetramer of 222 symmetry with a major and a minor dimer interface. The dimers connected via the minor interface can rotate with respect to each other, leading to the inactive T-state and active R-state conformations of FBPase. Read More

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November 2016

New insight into the binding modes of TNP-AMP to human liver fructose-1,6-bisphosphatase.

Spectrochim Acta A Mol Biomol Spectrosc 2016 08 8;165:155-160. Epub 2016 Apr 8.

Key Laboratory of Pesticide & Chemical Biology (CCNU), Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China. Electronic address:

Human liver fructose-1,6-bisphosphatase (FBPase) contains two binding sites, a substrate fructose-1,6-bisphosphate (FBP) active site and an adenosine monophosphate (AMP) allosteric site. The FBP active site works by stabilizing the FBPase, and the allosteric site impairs the activity of FBPase through its binding of a nonsubstrate molecule. The fluorescent AMP analogue, 2',3'-O-(2,4,6-trinitrophenyl)adenosine 5'-monophosphate (TNP-AMP) has been used as a fluorescent probe as it is able to competitively inhibit AMP binding to the AMP allosteric site and, therefore, could be used for exploring the binding modes of inhibitors targeted on the allosteric site. Read More

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T-to-R switch of muscle fructose-1,6-bisphosphatase involves fundamental changes of secondary and quaternary structure.

Acta Crystallogr D Struct Biol 2016 Apr 30;72(Pt 4):536-50. Epub 2016 Mar 30.

Department of Genetics, Wrocław University, Wrocław, Poland.

Fructose-1,6-bisphosphatase (FBPase) catalyzes the hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and is a key enzyme of gluconeogenesis and glyconeogenesis and, more generally, of the control of energy metabolism and glucose homeostasis. Vertebrates, and notably Homo sapiens, express two FBPase isoforms. The liver isozyme is expressed mainly in gluconeogenic organs, where it functions as a regulator of glucose synthesis. Read More

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Mechanism of bile acid-regulated glucose and lipid metabolism in duodenal-jejunal bypass.

Int J Clin Exp Pathol 2015 1;8(12):15778-85. Epub 2015 Dec 1.

Department of General Surgery, Shandong Cancer Hospital and Institute Jinan 250117, China.

Bile acid plays an important role in regulating blood glucose, lipid and energy metabolism. The present study was implemented to determine the effect of duodenal-jejunal bypass (DJB) on FXR, TGR-5expression in terminal ileum and its bile acid-related mechanism on glucose and lipid metabolism. Immunohistochemistry was used to detect relative gene or protein expression in liver and intestine. Read More

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October 2016

Oral administration of oil ameliorates the effect of cisplatin on membrane enzymes, carbohydrate metabolism and oxidative damage in rat liver.

Toxicol Rep 2016 13;3:328-335. Epub 2016 Feb 13.

Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, U.P., India.

Cisplatin (CP) is a potent anti-cancer drug widely used against solid tumors. However, it exhibits pronounced adverse effects including hepatotoxicity. Several strategies were attempted to prevent CP hepatotoxicity but were not found suitable for therapeutic application. Read More

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February 2016

A new level of regulation in gluconeogenesis: metabolic state modulates the intracellular localization of aldolase B and its interaction with liver fructose-1,6-bisphosphatase.

Biochem J 2015 Dec 28;472(2):225-37. Epub 2015 Sep 28.

Department of Biochemistry and Microbiology, Faculty of Sciences, Universidad Austral de Chile, Independencia 641,5110566, Valdivia, Chile

Understanding how glucose metabolism is finely regulated at molecular and cellular levels in the liver is critical for knowing its relationship to related pathologies, such as diabetes. In order to gain insight into the regulation of glucose metabolism, we studied the liver-expressed isoforms aldolase B and fructose-1,6-bisphosphatase-1 (FBPase-1), key enzymes in gluconeogenesis, analysing their cellular localization in hepatocytes under different metabolic conditions and their protein-protein interaction in vitro and in vivo. We observed that glucose, insulin, glucagon and adrenaline differentially modulate the intracellular distribution of aldolase B and FBPase-1. Read More

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December 2015