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Glucagon-like peptide

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https://www.readbyqxmd.com/read/28109096/-vildagliptin-suppresses-temporal-lobe-epilepsy-by-up-regulating-glucagon-like-peptide-1
#1
Yue-Tao Wen, Kun-Lun Wu, Quan-Hong Shi
OBJECTIVE: To investigate the effect of vildagliptin on pentamethazol (PTZ)-induced epilepsy in rats and explore the molecular mechanism. METHODS: Samples of temporal cortex from 23 patients with temporal lobe epilepsy were collected as epilepsy group and samples of temporal cortex from 14 patients with brain trauma were used as control group. Ninety male SD rats were randomly divided into control group (group A), PTZ-induced epilepsy group (group B), saline 2 mL/kg group (group C), vildagliptin 2...
January 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28108848/glucagon-like-peptide-1-is-co-localized-with-neurotensin-in-the-chicken-ileum
#2
Kei Nishimura, Kohzy Hiramatsu, Takafumi Watanabe, Kazumi Kita
Glucagon-like peptide (GLP)-1 and neurotensin (NT) are distributed throughout the chicken ileum. Here, we attempt to determine if GLP-1 and NT co-localize in the chicken ileum by using immunofluorescence, immunocytochemistry and in situ hybridization techniques. Three types of enteroendocrine cells, GLP-1(+)/NT(+), GLP-1(+)/NT(-) and GLP-1(-)/NT(+) cells, were detected in the mucosal epithelium by the double immunofluorescence method. The ratio of GLP-1(+)/NT(+) cells at the crypts in the distal ileum was significantly higher than that in the proximal ileum...
January 20, 2017: Cell and Tissue Research
https://www.readbyqxmd.com/read/28106217/flavanol-concentrations-do-not-predict-dipeptidyl-peptidase-iv-inhibitory-activities-of-four-cocoas-with-different-processing-histories
#3
Caroline M Ryan, Weslie Khoo, Amanda C Stewart, Sean F O'Keefe, Joshua D Lambert, Andrew P Neilson
Cocoa and its constituent bioactives (particularly flavanols) have reported anti-diabetic and anti-obesity activities. One potential mechanism of action is inhibition of dipeptidyl peptidase-IV (DPP4), the enzyme that inactivates incretin hormones such as glucagon-like peptide-1 and gastric inhibitory peptide. The objective of this study was to determine the DPP4 inhibitory activities of cocoas with different processing histories, and identify processing factors and bioactive compounds that predict DPP4 inhibition...
January 20, 2017: Food & Function
https://www.readbyqxmd.com/read/28106207/natural-sweetener-agave-inhibits-gastric-emptying-in-rats-by-a-cholecystokinin-2-and-glucagon-like-peptide-1-receptor-dependent-mechanism
#4
E Bihter Gürler, Dilek Özbeyli, Hülya Buzcu, Sezin Bayraktar, İrem Carus, Beyza Dağ, Yasemin Geriş, Seda Jeral, Berrak Ç Yeğen
Low-calorie sweeteners are considered to be beneficial in calorie control, but the impact of these sweeteners on gastric emptying is not well described. The purpose of this study was to compare the gastric emptying rate of agave nectar with those of glucose and fructose, and to evaluate the interaction of cholecystokinin (CCK)-1, CCK-2 and glucagon-like peptide-1 (GLP-1) receptors in agave-induced alterations in gastric emptying. Female Sprague-Dawley rats were fitted with gastric cannulas. Following the recovery, the gastric emptying rates of glucose, fructose and agave at 12...
January 20, 2017: Food & Function
https://www.readbyqxmd.com/read/28105738/glucagon-like-peptide-1-agonists-and-risk-of-acute-pancreatitis-in-patients-with-type-2-diabetes
#5
Heidi Storgaard, Frederik Cold, Lise L Gluud, Tina Vilsbøll, Filip K Knop
Glucagon-like peptide-1 receptor agonist (GLP-1RAs) labels warn about acute pancreatitis (AP) and impose doctors to inform patients about symptoms of AP. Here we systematically reviewed the risk of AP in randomized placebo-controlled trials (RCTs) investigating the effect of GLP-1RAs in type 2 diabetes. We performed a systematic review with meta-analysis of long-term (minimum 24 months), placebo-controlled GLP-1RA RCTs in which AP was a predefined adverse event and adjudicated by blinded and independent adjudicating committees...
January 20, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28105345/attenuation-by-incretins-of-thyroid-hormone-stimulated-osteocalcin-synthesis-in-osteoblasts
#6
Shingo Kainuma, Haruhiko Tokuda, Kazuhiko Fujita, Tetsu Kawabata, Go Sakai, Rie Matsushima-Nishiwaki, Atsushi Harada, Osamu Kozawa, Takanobu Otsuka
Incretins, the polypeptide hormone glucose- dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) secreted from the small intestine after nutrient ingestion, are generally known to stimulate insulin secretion from pancreatic β-cells. We previously demonstrated that triiodothyronine (T3) stimulates osteocalcin synthesis at least in part through p38 mitogen-activated protein kinase in osteoblast-like MC3T3-E1 cells. In the present study, we investigated the effects of GIP and GLP-1 on T3-stimulated osteocalcin synthesis and the mechanism of action involved in MC3T3-E1 cells...
December 2016: Biomedical Reports
https://www.readbyqxmd.com/read/28104916/trpv1-activation-counters-diet-induced-obesity-through-sirtuin-1-activation-and-prdm-16-deacetylation-in-brown-adipose-tissue
#7
P Baskaran, V Krishnan, K Fettel, P Gao, Z Zhu, J Ren, B Thyagarajan
BACKGROUND/OBJECTIVE: An imbalance between energy intake and expenditure leads to obesity. Increasing metabolism and thermogenesis in brown adipose tissue (BAT) can help in overcoming obesity. Here, we investigated the effect of activation of transient receptor potential vanilloid subfamily 1 (TRPV1) in the upregulation of thermogenic proteins in BAT to counter diet-induced obesity. SUBJECTS/METHODS: We investigated the effect of dietary supplementation of capsaicin (TRPV1 agonist) on the expression of metabolically important thermogenic proteins in BAT of wild type and TRPV1(-/-) mice that received either a normal chow or high fat (±capsaicin; TRPV1 activator) diet by immunoblotting...
January 20, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28104586/synergy-of-glucagon-like-peptide-2-and-epidermal-growth-factor-co-administration-on-intestinal-adaptation-in-neonatal-piglets-with-short-bowel-syndrome
#8
David W Lim, Crystal L Levesque, Donna F Vine, Mitsuru Muto, Jacob R Koepke, Patrick N Nation, Pamela R Wizzard, Julang Li, David L Bigam, Patricia L Brubaker, Justine M Turner, Paul W Wales
BACKGROUND: Glucagon-like peptide-2 (GLP-2) and epidermal growth factor (EGF) treatment enhance intestinal adaptation. To determine whether these growth factors exert synergistic effects on intestinal growth and function, GLP-2 and EGF-containing media (EGF-cm) were administered, alone and in combination, in neonatal piglet with short bowel syndrome (SBS). METHODS: Neonatal Landrace/Large White piglets were block-randomized to 75% mid-intestinal (JI group) or distal-intestinal (JC group) resection or sham control, with 7-d infusion of saline (control), intravenous human GLP-2 (11 nmol/kg/day) alone, enteral EGF-cm (80 μg/kg/day) alone, or GLP-2 and EGF-cm in combination...
January 19, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28103783/understanding-corticotropin-releasing-factor-receptor-crfr-activation-using-structural-models
#9
Arnau Cordomi, George Liapakis, Minos Timotheos Matsoukas
The corticotropin-releasing factor type 1 and 2 receptors (CRF1R and CRF2R) belong to the secretin-like family, also known as class B1, of G protein-coupled receptors (GPCRs). Several endogenous hormones mediate their responses through the CRF receptors, such as CRF and the urocortins. The structures for the N-terminus extracellular domain of both CRF1R and CRF2R in complex with peptidic ligands were released a few years ago and permitted the study of hormone binding to the orthosteric binding site. It was not until more recently, when the crystal structure of the transmembrane domain of human CRF1R in its inactive state bound to an allosteric antagonist became available...
January 10, 2017: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28103285/radioiodinated-exendin-4-is-superior-to-the-radiometal-labelled-glucagon-like-peptide-1-receptor-probes-overcoming-their-high-kidney-uptake
#10
Tilman Läppchen, Roswitha Tönnesmann, Jos Eersels, Philipp T Meyer, Helmut R Maecke, Svetlana N Rylova
GLP-1 receptors are ideal targets for preoperative imaging of benign insulinoma and for quantifying the beta cell mass. The existing clinical tracers targeting GLP-1R are all agonists with low specific activity and very high kidney uptake. In order to solve those issues we evaluated GLP-1R agonist Ex-4 and antagonist Ex(9-39) radioiodinated at Tyr40 side by side with [Nle14,Lys40(Ahx-DOTA-68Ga)NH2]Ex-4 (68Ga-Ex-4) used in the clinic. The Kd, Bmax, internalization and binding kinetics of [Nle14,125I-Tyr40-NH2]Ex-4 and [Nle14,125I-Tyr40-NH2]Ex(9-39) were studied in vitro using Ins-1E cells...
2017: PloS One
https://www.readbyqxmd.com/read/28103022/discovery-of-a-novel-series-of-orally-bioavailable-and-cns-penetrant-glucagon-like-peptide-1-receptor-glp-1r-non-competitive-antagonists-based-on-a-1-3-disubstituted-7-aryl-5-5-bis-trifluoromethyl-5-8-dihydropyrimido-4-5-d-pyrimidine-2-4-1h-3h-dione-core
#11
Kellie D Nance, Emily L Days, C David Weaver, Anastasia Coldren, Tiffany D Farmer, Hyekyung P Cho, Colleen M Niswender, Anna L Blobaum, Kevin D Niswender, Craig W Lindsley
A duplexed, functional multi-addition high throughput screen and subsequent optimization effort identified the first orally bioavailable and CNS penetrant glucagon-like peptide-1 receptor (GLP-1R) non-competitive antagonist. Antagonist 5d not only blocked Exendin-4-stimulated insulin release in islets, but also lowered insulin levels while increasing blood glucose in vivo.
January 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28102093/cardiovascular-safety-and-benefits-of-glp-1-receptor-agonists
#12
Niels B Dalsgaard, Andreas Brønden, Tina Vilsbøll, Filip K Knop
Glucagon-like peptide-1 (GLP-1) receptor agonists (GLP-1RAs) constitute a class of drugs for the treatment of type 2 diabetes, and currently, six different GLP-1RAs are approved. Besides improving glycemic control, the GLP-1RAs have other beneficial effects such as weight loss and a low risk of hypoglycemia. Treatment with the GLP-1RA lixisenatide has been shown to be safe in patients with type 2 diabetes and recent acute coronary syndrome. Furthermore, liraglutide and semaglutide have been shown to reduce cardiovascular (CV) disease (CVD) risk in type 2 diabetes patients with established and/or high risk of CVD...
January 19, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28101843/postprandial-glp-2-levels-are-increased-after-biliopancreatic-diversion-in-diabetic-individuals-with-class-i-obesity-a-prospective-study
#13
Everton Cazzo, José Carlos Pareja, Bruno Geloneze, Elinton Adami Chaim, Maria Rita Lazzarini Barreto, Daniéla Oliveira Magro
BACKGROUND: Biliopancreatic diversion (BPD) is a predominantly malabsorptive procedure. Glucagon-like peptide 2 (GLP-2) plays predominantly trophic effects on the gut. A significant increase in GLP-2 after BPD in rats was previously observed, but there are no studies investigating the effect of BPD in GLP-2 levels in humans. OBJECTIVE: The aim of this study is to evaluate the influence of BPD on the release of GLP-2. METHODS: This is a prospective cohort study that evaluated diabetic individuals with class I obesity which underwent BPD (Scopinaro operation) and were followed up for 12 months...
January 18, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28101792/medical-management-of-diabesity-do-we-have-realistic-targets
#14
REVIEW
Joseph M Pappachan, Ananth K Viswanath
PURPOSE OF REVIEW: The global prevalence of "diabesity"-diabetes related to obesity-is increasing steadily over the past few decades because of the obesity epidemic. Although bariatric surgery is an effective treatment option for patients with diabesity, its limited availability, invasiveness, relatively high costs and the potential for surgical and postsurgical complications restrict its widespread use. Therefore, medical management is the only option for a majority of patients with diabesity...
January 2017: Current Diabetes Reports
https://www.readbyqxmd.com/read/28098405/shielding-engineered-islets-with-mesenchymal-stem-cells-enhance-survival-under-hypoxia
#15
Bhawna Chandravanshi, Ramesh Ramchandra Bhonde
In the present study we focused on the improvisation of islet survival in hypoxia.The Islet like cell aggregates (ICAs) derived from wharton's jelly mesenchymal stem cells (WJ MSC) were cultured with and without WJ MSC for 48h in hypoxia and normoxia and tested for their direct trophic effect on β cell survival. The WJ MSCs themselves secreted insulin upon glucose challenge and expressed the pancreatic markers at both transcription and translational level (C-peptide, Insulin,Glucagon and Glut 2). Direct contact of MSCs with ICAs facilitated highest viability under hypoxia as evidenced by fluorescein diacetate/propidium iodide and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay...
January 18, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28098360/morroniside-a-secoiridoid-glycoside-from-cornus-officinalis-attenuates-neuropathic-pain-by-activation-of-spinal-glucagon-like-peptide-1-receptors
#16
Meng Xu, Hai-Yun Wu, Hao Liu, Nian Gong, Yi-Rui Wang, Yong-Xiang Wang
BACKGROUND AND PURPOSE: Iridoid glycosides with intact double bond scaffold of cyclopentapyran were reversible and orthosteric agonists of glucagon-like peptide-1 (GLP-1) receptors and possess antinociception and neuroprotection. Morroniside, derived from the medicinal herb Cornus officinalis, is an atypical secoiridoid replaced by a six-membered cyclic inner ether fragment. This study investigated whether morroniside was an orthosteric GLP-1 receptor agonist and had antihypersensitivity activities in neuropathy...
January 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28098139/appetite-responses-to-high-fat-meals-or-diets-of-varying-fatty-acid-composition-a-comprehensive-review
#17
REVIEW
S Kaviani, J A Cooper
Dietary fatty acids (FA) act as signaling molecules with diverse effects on physiologic function. The aim of this article is to review and summarize the clinical human studies in the literature on how dietary FA composition in meals and diets affects hunger and satiety signaling in the body. Studies examining FA saturation (monounsaturated (MUFA), saturated or polyunsaturated (PUFA) FAs) or FA chain length from high-fat meals/diets were included. Measures of appetite included visual analog scale (VAS) questionnaires, appetite hormones (Cholecystokinin (CCK), glucagon-like peptide-1 (GLP-1), peptide YY (PYY), gastric insulinotropic polypeptide gastric inhibitory peptide (GIP), ghrelin, leptin, insulin) and/or energy intake (EI) data...
January 18, 2017: European Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/28097390/a-role-of-plc-pkc-dependent-pathway-in-glp-1-stimulated-insulin-secretion
#18
REVIEW
Makoto Shigeto, Chae Young Cha, Patrik Rorsman, Kohei Kaku
Glucagon-like peptide-1 (GLP-1) is an endogenous glucose-lowering hormone and GLP-1 receptor agonists are currently being used as antidiabetic drugs clinically. The canonical signalling pathway (including cAMP, Epac2, protein kinase A (PKA) and KATP channels) is almost universally accepted as the main mechanism of GLP-1-stimulated insulin secretion. This belief is based on in vitro studies that used nanomolar (1-100 nM) concentrations of GLP-1. Recently, it was found that the physiological concentrations (1-10 pM) of GLP-1 also stimulate insulin secretion from isolated islets, induce membrane depolarization and increase of intracellular [Ca(2+)] in isolated β cells/pancreatic islets...
January 17, 2017: Journal of Molecular Medicine: Official Organ of the "Gesellschaft Deutscher Naturforscher und Ärzte"
https://www.readbyqxmd.com/read/28096522/control-of-food-intake-by-gastrointestinal-peptides-mechanisms-of-action-and-possible-modulation-in-the-treatment-of-obesity
#19
REVIEW
Philip Prinz, Andreas Stengel
This review focuses on the control of appetite by food intake-regulatory peptides secreted from the gastrointestinal tract, namely cholecystokinin, glucagon-like peptide 1, peptide YY, ghrelin, and the recently discovered nesfatin-1 via the gut-brain axis. Additionally, we describe the impact of external factors such as intake of different nutrients or stress on the secretion of gastrointestinal peptides. Finally, we highlight possible conservative-physical activity and pharmacotherapy-treatment strategies for obesity as well as surgical techniques such as deep brain stimulation and bariatric surgery also altering these peptidergic pathways...
January 17, 2017: Journal of Neurogastroenterology and Motility
https://www.readbyqxmd.com/read/28095318/interoceptive-modulation-of-neuroendocrine-emotional-and-hypophagic-responses-to-stress
#20
REVIEW
James W Maniscalco, Linda Rinaman
Periods of caloric deficit substantially attenuate many centrally mediated responses to acute stress, including neural drive to the hypothalamic-pituitary-adrenal (HPA) axis, anxiety-like behavior, and stress-induced suppression of food intake (i.e., stress hypophagia). It is posited that this stress response plasticity supports food foraging and promotes intake during periods of negative energy balance, even in the face of other internal or external threats, thereby increasing the likelihood that energy stores are repleted...
January 14, 2017: Physiology & Behavior
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