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https://www.readbyqxmd.com/read/28078647/sitagliptin-a-review-in-type-2-diabetes
#1
Lesley J Scott
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia(®); Glactiv(®); Tesavel(®); Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD)...
January 11, 2017: Drugs
https://www.readbyqxmd.com/read/28065547/comparison-of-the-diabetes-guidelines-from-the-ada-easd-and-the-aace-ace
#2
Susan Cornell
OBJECTIVE: To compare recent diabetes guideline updates from the American Diabetes Association-European Association for the Study of Diabetes (ADA/EASD) and the American Association of Clinical Endocrinologists-American College of Endocrinology (AACE/ACE). SUMMARY: The ADA/EASD guideline continues to advocate a stepwise approach to glycemic control that initiates with metformin and intensifies treatment incrementally to dual and triple therapy at 3-month intervals until the patient is at their individualized goal...
January 5, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28062192/direct-effects-of-glucose-insulin-glp-1-and-gip-on-bulbospinal-neurons-in-the-rostral-ventrolateral-medulla-in-neonatal-wistar-rats
#3
Naoki Oshima, Hiroshi Onimaru, Hidehito Matsubara, Takahiro Uchida, Atsushi Watanabe, Toshihiko Imakiire, Yasuhiro Nishida, Hiroo Kumagai
Although patients with diabetes mellitus (DM) often exhibit hypertension, the mechanisms responsible for this correlation are not well known. We hypothesized that the bulbospinal neurons in the rostral ventrolateral medulla (RVLM) are affected by the levels of glucose, insulin, or incretins (glucagon like peptide-1 [GLP-1] or glucose-dependent insulinotropic peptide [GIP]) in patients with DM. To investigate whether RVLM neurons are activated by glucose, insulin, GLP-1, or GIP, we examined changes in the membrane potentials of bulbospinal RVLM neurons using whole-cell patch-clamp technique during superfusion with various levels of glucose or these hormones in neonatal Wistar rats...
January 3, 2017: Neuroscience
https://www.readbyqxmd.com/read/28043676/cardiovascular-safety-of-incretin-based-therapy-for-type-2-diabetes-a-meta-analysis-of-randomized-trials
#4
Ahmed N Mahmoud, Marwan Saad, Hend Mansoor, Akram Y Elgendy, Amr F Barakat, Ahmed Abuzaid, Amgad Mentias, Islam Y Elgendy
No abstract text is available yet for this article.
December 26, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/28040864/glp-1-receptor-independent-pathways-emerging-beneficial-effects-of-glp-1-breakdown-products
#5
REVIEW
Valeria Guglielmi, Paolo Sbraccia
The glucagon-like peptide-1 (GLP-1) axis has emerged as a major therapeutic target for the treatment of type 2 diabetes and, recently, of obesity. The insulinotropic activity of the native incretin hormone GLP-1(7-36)amide, which is mainly exerted through a unique G protein-coupled receptor (GLP-1R), is terminated via enzymatic cleavage by dipeptidyl peptidase-IV that generates a C-terminal GLP-1 metabolite GLP-1(9-36)amide, the major circulating form in plasma. GLP-1(28-36)amide and GLP-1(32-36)amide are further cleavage products derived from GLP-1(7-36)amide and GLP-1(9-36)amide by the action of a neutral endopeptidase known as neprilysin...
December 31, 2016: Eating and Weight Disorders: EWD
https://www.readbyqxmd.com/read/28028077/endogenous-%C3%AE-2a-adrenoceptor-operated-sympathoadrenergic-tones-attenuate-insulin-secretion-via-camp-trpm2-signaling
#6
Kiyonori Ito, Katsuya Dezaki, Masashi Yoshida, Hodaka Yamada, Rina Miura, Rauza Sukma Rita, Susumu Ookawara, Kaoru Tabei, Masanobu Kawakami, Kazuo Hara, Yoshiyuki Morishita, Toshihiko Yada, Masafumi Kakei
In pancreatic β-cells, pharmacological concentrations of catecholamines, including adrenaline, have been used to inhibit insulin release and explore the multiple mechanisms involved. However, the significance of these signaling pathways for physiological adrenergic functions in β-cells is largely unknown. In the process of glucose-induced insulin secretion, opening of background current through non-selective cation channels (NSCCs) might facilitate membrane depolarization by closure of the ATP-sensitive K(+) channels...
December 27, 2016: Diabetes
https://www.readbyqxmd.com/read/28025651/delphinidin-rich-maqui-berry-extract-delphinol%C3%A2-lowers-fasting-and-postprandial-glycemia-and-insulinemia-in-prediabetic-individuals-during-oral-glucose-tolerance-tests
#7
Jorge L Alvarado, Andrés Leschot, Álvaro Olivera-Nappa, Ana-María Salgado, Hernán Rioseco, Carolina Lyon, Pilar Vigil
Delphinidin anthocyanins have previously been associated with the inhibition of glucose absorption. Blood glucose lowering effects have been ascribed to maqui berry (Aristotelia chilensis) extracts in humans after boiled rice consumption. In this study, we aimed to explore whether a standardized delphinidin-rich extract from maqui berry (Delphinol) affects glucose metabolism in prediabetic humans based on glycemia and insulinemia curves obtained from an oral glucose tolerance test (OGTT) after a challenge with pure glucose...
2016: BioMed Research International
https://www.readbyqxmd.com/read/28008090/scaling-it-down-new-in-vitro-tools-to-get-the-balance-right
#8
Emma K Biggs, Fiona M Gribble, Frank Reimann
Treatments for diabetes and obesity based on enteroendocrine hormones are a focus of research interest, partly due to the successes of glucagon-like peptide-1 (GLP-1) mimetic peptides in the treatment of diabetes and the correlation of altered enteroendocrine profiles with the positive metabolic outcomes of gastric bypass surgery. It is thought that simultaneous stimulation of more than one receptor might mimic the superior efficacy of the latter and dual or triple-agonist peptides are under investigation. An important step in developing multiple agonists is to establish the relative pharmacological potency and efficacy of new molecules at its different target receptors, and to optimise the balance of activities to achieve the desired treatment outcome...
January 1, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28007055/physiological-and-pathophysiological-aspects-of-incretin-hormones-and-glucagon
#9
Jonatan Ising Bagger
Infusion of oxyntomodulin and the separate and combined infusion of GLP-1 and glucagon inhibited food intake similarly in healthy individuals, with no superior effect of combining GLP-1 and glucagon. We confirm the inhibitory effects of oxyntomodulin and GLP-1, respectively, on GE and appetite scores observed previously, but by adding glucagon to the infusion of GLP-1 we found no additive effects. Unexpectedly, glucagon alone had no effect on GE and appetite scores, but inhibited food intake to the same extent as oxyntomodulin, GLP-1 and GLP-1 + glucagon...
January 2017: Danish Medical Journal
https://www.readbyqxmd.com/read/28000723/plasma-dpp4-activity-is-associated-with-no-reflow-and-major-bleeding-events-in-chinese-pci-treated-stemi-patients
#10
Jing Wei Li, Yun Dai Chen, Wei Ren Chen, Jing Jing, Jie Liu, Yong Qiang Yang
Dipeptidyl peptidase-4 (DPP4) is an important regulator of incretins and inflammation, and it is involved in the pathophysiological process of myocardial infarction (MI). This study investigated the role of plasma DPP4 activity (DPP4a) in patients with ST-segment elevation myocardial infarction (STEMI) who had undergone percutaneous coronary intervention (PCI). We recruited 747 consecutive PCI-treated STEMI patients from a tertiary referral center from January 2014 to October 2015. The outcomes of interest were the rates of no-reflow, in-hospital major adverse cardiac or cerebrovascular events (iMACCE), in-hospital complications (IHC) and in-hospital major bleeding...
December 21, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27999001/glucose-metabolism-after-gastric-banding-and-gastric-bypass-in-individuals-with-type-2-diabetes-weight-loss-effect
#11
Marlena M Holter, Roxanne Dutia, Sarah M Stano, Ronald L Prigeon, Peter Homel, James J McGinty, Scott J Belsley, Christine J Ren, Daniel Rosen, Blandine Laferrère
OBJECTIVE: The superior effect of Roux-en-Y gastric bypass (RYGB) on glucose control compared with laparoscopic adjustable gastric banding (LAGB) is confounded by the greater weight loss after RYGB. We therefore examined the effect of these two surgeries on metabolic parameters matched on small and large amounts of weight loss. RESEARCH DESIGN AND METHODS: Severely obese individuals with type 2 diabetes were tested for glucose metabolism, β-cell function, and insulin sensitivity after oral and intravenous glucose stimuli, before and 1 year after RYGB and LAGB, and at 10% and 20% weight loss after each surgery...
January 2017: Diabetes Care
https://www.readbyqxmd.com/read/27997588/protective-effects-of-vildagliptin-against-pioglitazone-induced-bone-loss-in-type-2-diabetic-rats
#12
Young Sil Eom, A-Ryeong Gwon, Kyung Min Kwak, Ju-Young Kim, Seung Hee Yu, Sihoon Lee, Yeun Sun Kim, Ie Byung Park, Kwang-Won Kim, Kiyoung Lee, Byung-Joon Kim
Long-term use of thiazolidinediones (TZDs) is associated with bone loss and an increased risk of fracture in patients with type 2 diabetes (T2DM). Incretin-based drugs (glucagon-like peptide-1 (GLP-1) agonists and dipeptidylpeptidase-4 (DPP-4) inhibitors) have several benefits in many systems in addition to glycemic control. In a previous study, we reported that exendin-4 might increase bone mineral density (BMD) by decreasing the expression of SOST/sclerostin in osteocytes in a T2DM animal model. In this study, we investigated the effects of a DPP-4 inhibitor on TZD-induced bone loss in a T2DM animal model...
2016: PloS One
https://www.readbyqxmd.com/read/27991713/roles-of-the-gut-in-the-metabolic-syndrome-an-overview
#13
REVIEW
L Fändriks
The metabolic syndrome is a cluster of risk factors (central obesity, hyperglycaemia, dyslipidaemia and arterial hypertension), indicating an increased risk of diabetes, cardiovascular disease and premature mortality. The gastrointestinal tract is seldom discussed as an organ system of principal importance for metabolic diseases. The present overview connects various metabolic research lines into an integrative physiological context in which the gastrointestinal tract is included. Strong evidence for the involvement of the gut in the metabolic syndrome derives from the powerful effects of weight-reducing (bariatric) gastrointestinal surgery...
December 19, 2016: Journal of Internal Medicine
https://www.readbyqxmd.com/read/27990751/curcumin-improves-glucose-tolerance-via-stimulation-of-glucagon-like-peptide-1-secretion
#14
Masaki Kato, Sho Nishikawa, Akiho Ikehata, Kojiro Dochi, Tsubasa Tani, Tsukasa Takahashi, Atsushi Imaizumi, Takanori Tsuda
SCOPE: Glucagon-like peptide-1 (GLP-1) is a type of incretin secreted from enteroendocrine L-cells. Our previous studies demonstrated that curcumin (a yellow pigment of turmeric) significantly increases the secretion of GLP-1 in enteroendocrine L cell line (GLUTag cells). However, it is not clear whether its action in vivo directly enhances GLP-1 secretion, which then leads to a reduction in blood glucose levels via the stimulation of insulin secretion. In addition, the molecular target of curcumin-induced GLP-1 secretion has not been clarified...
November 7, 2016: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/27988872/insulin-resistance-and-neurodegeneration-progress-towards-the-development-of-new-therapeutics-for-alzheimer-s-disease
#15
REVIEW
Suzanne M de la Monte
Alzheimer's disease (AD) should be regarded as a degenerative metabolic disease caused by brain insulin resistance and deficiency, and overlapping with the molecular, biochemical, pathophysiological, and metabolic dysfunctions in diabetes mellitus, non-alcoholic fatty liver disease, and metabolic syndrome. Although most of the diagnostic and therapeutic approaches over the past several decades have focused on amyloid-beta (Aβ42) and aberrantly phosphorylated tau, which could be caused by consequences of brain insulin resistance, the broader array of pathologies including white matter atrophy with loss of myelinated fibrils and leukoaraiosis, non-Aβ42 microvascular disease, dysregulated lipid metabolism, mitochondrial dysfunction, astrocytic gliosis, neuro-inflammation, and loss of synapses vis-à-vis growth of dystrophic neurites, is not readily accounted for by Aβ42 accumulations, but could be explained by dysregulated insulin/IGF-1 signaling with attendant impairments in signal transduction and gene expression...
December 17, 2016: Drugs
https://www.readbyqxmd.com/read/27986466/mitochondrial-adaptation-in-nonalcoholic-fatty-liver-disease-novel-mechanisms-and-treatment-strategies
#16
REVIEW
Nishanth E Sunny, Fernando Bril, Kenneth Cusi
Nonalcoholic fatty liver disease (NAFLD) is prevalent in patients with obesity or type 2 diabetes. Nonalcoholic steatohepatitis (NASH), encompassing steatosis with inflammation, hepatocyte injury, and fibrosis, predisposes to cirrhosis, hepatocellular carcinoma, and even cardiovascular disease. In rodent models and humans with NAFLD/NASH, maladaptation of mitochondrial oxidative flux is a central feature of simple steatosis to NASH transition. Induction of hepatic tricarboxylic acid cycle closely mirrors the severity of oxidative stress and inflammation in NASH...
December 13, 2016: Trends in Endocrinology and Metabolism: TEM
https://www.readbyqxmd.com/read/27986341/incretin-related-drugs-and-cardiovascular-events-a-comparison-of-glp-1-analogue-and-dpp-4-inhibitor
#17
EDITORIAL
Yukihito Higashi
No abstract text is available yet for this article.
December 13, 2016: Journal of Cardiology
https://www.readbyqxmd.com/read/27982680/distinct-response-of-fat-and-gastrointestinal-tissue-to-glucose-in-gestational-diabetes-mellitus-and-polycystic-ovary-syndrome
#18
D Vejrazkova, O Lischkova, M Vankova, S Stanicka, J Vrbikova, P Lukasova, J Vcelak, G Vacinova, B Bendlova
Gestational diabetes mellitus (GDM) and polycystic ovary syndrome (PCOS) are distinct pathologies with impaired insulin sensitivity as a common feature. The aim of this study was to evaluate the response of fat tissue adipokines and gastrointestinal incretins to glucose load in patients diagnosed with one of the two disorders and to compare it with healthy controls. Oral glucose tolerance test (oGTT) was performed in 77 lean young women: 22 had positive history of GDM, 19 were PCOS patients, and 36 were healthy controls...
December 16, 2016: Physiological Research
https://www.readbyqxmd.com/read/27975209/critical-role-for-glp-1-in-symptomatic-post-bariatric-hypoglycaemia
#19
Colleen M Craig, Li-Fen Liu, Carolyn F Deacon, Jens J Holst, Tracey L McLaughlin
AIMS/HYPOTHESIS: Post-bariatric hypoglycaemia (PBH) is a rare, but severe, metabolic disorder arising months to years after bariatric surgery. It is characterised by symptomatic postprandial hypoglycaemia, with inappropriately elevated insulin concentrations. The relative contribution of exaggerated incretin hormone signalling to dysregulated insulin secretion and symptomatic hypoglycaemia is a subject of ongoing inquiry. This study was designed to test the hypothesis that PBH and associated symptoms are primarily mediated by glucagon-like peptide-1 (GLP-1)...
December 14, 2016: Diabetologia
https://www.readbyqxmd.com/read/27974210/downregulation-of-a-gpcr-by-%C3%AE-arrestin2-mediated-switch-from-an-endosomal-to-a-tgn-recycling-pathway
#20
Nazish Abdullah, Muheeb Beg, David Soares, Jeremy S Dittman, Timothy E McGraw
Glucose-dependent insulinotropic polypeptide (GIP) is an incretin hormone involved in nutrient homeostasis. GIP receptor (GIPR) is constitutively internalized and returned to the plasma membrane, atypical behavior for a G-protein-coupled receptor (GPCR). GIP promotes GIPR downregulation from the plasma membrane by inhibiting recycling without affecting internalization. This transient desensitization is achieved by altered intracellular trafficking of activated GIPR. GIP stimulation induces a switch in GIPR recycling from a rapid endosomal to a slow trans-Golgi network (TGN) pathway...
December 13, 2016: Cell Reports
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