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https://www.readbyqxmd.com/read/28741970/efficacy-and-safety-of-once-weekly-semaglutide-for-the-treatment-of-type-2-diabetes
#1
Xueying Tan, Xiaojing Cao, Minzhi Zhou, Ping Zou, Jingbo Hu
Type 2 diabetes is a chronic metabolic disease characterized by persistent hyperglycemia resulting from progressive deficient of insulin in patients with a background of insulin resistance. Current treatment algorithms recommended by American Diabetes Association/The European Association for the Study of Diabetes promote a patient-centered approach that takes into account a comprehensive consideration of pharmacological properties of drugs, including glucose-lowering action, effects on body weight, correction on multiple pathophysiologic defects, tolerability, and long-term safety...
July 25, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28741456/effects-of-oral-and-non-insulin-injectable-antidiabetic-treatment-in-hypertension-a-systematic-review
#2
Vasiliki Katsi, Georgios Georgiopoulos, Georgia Vogiatzi, Dimitrios Oikonomou, Maria Megapanou, John Skoumas, Charalampos Vlachopoulos, Petros Nihoyannopoulos, Dimitris Tousoulis
BACKGROUND: Diabetes mellitus type 2 (T2DM) often co-exists with hypertension, and this aggregation of co-morbidities amplifies the risk for future cardiovascular events. Therefore, it appears crucial to understand the essence of choosing oral and non-insulin injectable anti-diabetic drugs (ADs) with a favorable hemodynamic impact that could partially attenuate the increased baseline cardiovascular risk. OBJECTIVE: We sought to evaluate the effect of ADs on blood pressure (BP) indices and to assess the potential role of certain ADs towards hypertension treatment...
May 19, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28741313/exploiting-the-medbz-linker-to-generate-protected-or-unprotected-c-terminally-modified-peptides
#3
Christine A Arbour, Hasina Y Saraha, Timothy F McMillan, Jennifer Stockdill
C-terminally modified peptides are important targets for pharmaceutical and biochemical applications. Known methods for C-terminal diversification are limited mainly in terms of the scope of accessible modifications or by epimerization of the C-terminal amino acid. In this work, we present a broadly applicable approach that enables access to a variety of C-terminally functionalized peptides in either protected or unprotected form. This chemistry proceeds without epimerization of C-terminal Ala and tolerates nucleophiles of varying nucleophilicity...
July 24, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28738763/an-evaluation-of-the-clinical-therapeutic-effect-of-lixisenatide-in-type-2-diabetes-patients-a-systematic-literature-review
#4
Arinze Nkemdirim Okere, Janele Montesdeoca, April Glasper, Vakaramoko Diaby
BACKGROUND: With cardiovascular disease accounting for approximately 50% of deaths in patients diagnosed with type 2 diabetes, it is pertinent to initiate anti-diabetic medications with cardiovascular benefits. This systematic clinical review critically examines the clinical therapeutic effect of lixisenatide. METHODS: Data were gathered from articles indexed in PubMed, Google Scholar and Medline from 2010 - 2017, with the following search terms, "lixisenatide" and "GLP-1 receptor agonist...
July 24, 2017: Current Diabetes Reviews
https://www.readbyqxmd.com/read/28738080/effects-of-exogenous-glucagon-like-peptide-2-and-distal-bowel-resection-on-intestinal-and-systemic-adaptive-responses-in-rats
#5
Sarah W Lai, Elaine de Heuvel, Laurie E Wallace, Bolette Hartmann, Jens J Holst, Mary E Brindle, Prasanth K Chelikani, David L Sigalet
OBJECTIVE: To determine the effects of exogenous glucagon-like peptide-2 (GLP-2), with or without massive distal bowel resection, on adaptation of jejunal mucosa, enteric neurons, gut hormones and tissue reserves in rats. BACKGROUND: GLP-2 is a gut hormone known to be trophic for small bowel mucosa, and to mimic intestinal adaptation in short bowel syndrome (SBS). However, the effects of exogenous GLP-2 and SBS on enteric neurons are unclear. METHODS: Sprague Dawley rats were randomized to four treatments: Transected Bowel (TB) (n = 8), TB + GLP-2 (2...
2017: PloS One
https://www.readbyqxmd.com/read/28736546/zb-16-a-novel-gpr119-agonist-relieves-the-severity-of-streptozotocin-nicotinamide-induced-diabetes-in-rats
#6
Ivan N Tyurenkov, Denis V Kurkin, Dmitry A Bakulin, Elena V Volotova, Mikhail A Chafeev, Alexey V Smirnov, Evgeny I Morkovin
GPR119 is involved in the regulation of incretin and insulin secretion, so the GPR119 agonists have been suggested as novel antidiabetic medications. The purpose of this work was to assess the influence of novel GPR119 agonist ZB-16 on the glucose utilization, insulin, and glucagon-like peptide-1 (GLP-1) secretion and the morphology of pancreas in rats with streptozotocin-nicotinamide-induced diabetes. 45 male Wistar rats were used in the study. The criteria of streptozotocin-nicotinamide-induced diabetes were blood glucose levels of 9-14 mmol/l measured in fasting conditions on the third day since administration of streptozotocin (65 mg/kg) and nicotinamide (230 mg/kg)...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28734203/exenatide-mitigated-diet-induced-vascular-aging-and-atherosclerotic-plaque-growth-in-apoe-deficient-mice-under-chronic-stress
#7
Guang Yang, Yanna Lei, Aiko Inoue, Limei Piao, Lina Hu, Haiying Jiang, Takeshi Sasaki, Hongxian Wu, Wenhu Xu, Chenglin Yu, Guangxian Zhao, Shinyu Ogasawara, Kenji Okumura, Masafumi Kuzuya, Xian-Wu Cheng
BACKGROUND AND AIMS: Exposure to psychosocial stress is a risk factor for cardiovascular disorders. Because the glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonist prevents cardiovascular injury, we investigated the beneficial effects and mechanism of the GLP-1 analogue exenatide on stress-related vascular senescence and atherosclerosis in apolipoprotein E-deficient (ApoE(-/-)) mice fed a high-fat (HF) diet. METHODS: ApoE(-/-) mice fed the HF diet were assigned to non-stressed and immobilized-stress groups for 12 weeks...
July 13, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28733905/glp-1-glucagon-receptor-co-agonism-for-treatment-of-obesity
#8
REVIEW
Miguel A Sánchez-Garrido, Sara J Brandt, Christoffer Clemmensen, Timo D Müller, Richard D DiMarchi, Matthias H Tschöp
Over a relatively short period, obesity and type 2 diabetes have come to represent a large medical and economic burden to global societies. The epidemic rise in the prevalence of obesity has metabolic consequences and is paralleled by an increased occurrence of other diseases, such as diabetes, cancer and cardiovascular complications. Together, obesity and type 2 diabetes constitute one of the more preventable causes of premature death and the identification of novel, safe and effective anti-obesity drugs is of utmost importance...
July 21, 2017: Diabetologia
https://www.readbyqxmd.com/read/28733378/is-it-time-to-change-the-type-2-diabetes-treatment-paradigm-no-metformin-should-remain-the-foundation-therapy-for-type-2-diabetes
#9
Silvio E Inzucchi
Most treatment guidelines, including those from the American Diabetes Association/European Association for the Study of Diabetes and the International Diabetes Federation, suggest metformin be used as the first-line therapy after diet and exercise. This recommendation is based on the considerable body of evidence that has accumulated over the last 30 years, but it is also supported on clinical grounds based on metformin's affordability and tolerability. As such, metformin is the most commonly used oral antihyperglycemic agent in the U...
August 2017: Diabetes Care
https://www.readbyqxmd.com/read/28733377/is-it-time-to-change-the-type-2-diabetes-treatment-paradigm-yes-glp-1-ras-should-replace-metformin-in-the-type-2-diabetes-algorithm
#10
Muhammad Abdul-Ghani, Ralph A DeFronzo
Most treatment guidelines, including those from the American Diabetes Association/European Association for the Study of Diabetes and the International Diabetes Federation, suggest metformin be used as the first-line therapy after diet and exercise. This recommendation is based on the considerable body of evidence that has accumulated over the last 30 years, but it is also supported on clinical grounds based on metformin's affordability and tolerability. As such, metformin is the most commonly used oral antihyperglycemic agent in the U...
August 2017: Diabetes Care
https://www.readbyqxmd.com/read/28733306/species-dependent-mechanisms-regulating-glucose-dependent-glp-1-secretion
#11
Patricia L Brubaker
No abstract text is available yet for this article.
August 2017: Diabetes
https://www.readbyqxmd.com/read/28730832/liraglutide-preserves-intracellular-calcium-handling-in-isolated-murine-myocytes-exposed-to-oxidative-stress
#12
S Palee, S C Chattipakorn, N Chattipakorn
In ischemic/reperfusion (I/R) injured hearts, severe oxidative stress occurs and is associated with intracellular calcium (Ca(2+)) overload. Glucagon-Like Peptide 1 (GLP-1) analogues have been shown to exert cardioprotection in I/R heart. However, there is little information regarding the effects of GLP-1 analogue on the intracellular Ca(2+) regulation in the presence of oxidative stress. Therefore, we investigated the effects of GLP-1 analogue, (liraglutide, 10 microM) applied before or after hydrogen peroxide (H(2)O(2), 50 microM) treatment on intracellular Ca(2+) regulation in isolated cardiomyocytes...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28730824/glucagon-like-peptide-1-analogues-exenatide-and-liraglutide-exert-inhibitory-effect-on-the-early-phase-of-liver-regeneration-after-partial-hepatectomy-in-rats
#13
J Fontana, O Kučera, V Mezera, M Anděl, Z Červinková
Glucagon-like peptide-1 (GLP-1) is an incretin known for proliferative and antiapoptotic effects on various tissues. Exenatide and Liraglutide are GLP-1 analogues used in clinical practice as antidiabetic drugs. Since GLP-1 and its analogues exert significant effect on liver metabolism and since changes in intermediary metabolism play an important role in the process of liver regeneration, we decided to determine the effect of Exenatide and Liraglutide on the early phase of liver regeneration and selected metabolic parameters in a model of 2/3 partial hepatectomy (PHx) in rats...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28730750/improving-type-2-diabetes-mellitus-glycaemic-outcomes-is-possible-without-spending-more-on-medication-lessons-from-the-uk-national-diabetes-audit
#14
Adrian H Heald, Mark Livingston, Nagaraj Malipatil, Michal Becher, Joyce Craig, Mike Stedman, Anthony A Fryer
OBJECTIVES: There is continuing discussion globally about how to optimise outcomes for type 2 diabetes (T2DM) patients. In the UK, national (NICE) guidance was updated in 2016 (NG28). We aimed to determine the factors at a GP practice level that relate to glycaemic control outcome. METHODS: Data was accessed from 4,050 GP practices (GPP) (50% of total) covering 1.6 million T2DM patients in the UK National Diabetes Audit 2013-14 and 2014-15. This reported T2DM population characteristics, services and outcomes, including % total glycaemic control (TGC) (at 67...
July 20, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28730728/beneficial-long-term-antidiabetic-actions-of-n-and-c-terminally-modified-analogues-of-apelin-13-in-diet-induced-obese-diabetic-mice
#15
V Parthsarathy, C Hogg, P R Flatt, F P M O'Harte
AIMS: This study investigated the chronic effects of twice daily administration of stable apelin analogues, apelin-13 amide and (pGlu)apelin-13 amide, on metabolic parameters in glucose intolerant and insulin resistant diet-induced obese (DIO) mice fed a high-fat diet for 150 days. STUDY DESIGN & METHODS: Groups of mice received twice daily (09:00 and 17:00 h) injections of saline vehicle, apelin-13 amide, (pGlu)apelin-13 amide or exendin-4(1-39) for 28 days (all at 25 nmol/kg)...
July 20, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28727604/preclinical-development-of-ebi-005-an-il-1-receptor-1-inhibitor-for-the-topical-ocular-treatment-of-ocular-surface-inflammatory-diseases
#16
Joseph Kovalchin, Bracken King, Allyson Masci, Elizabeth Hopkins, Jeremy Fry, Jay Hou, Christian Li, Kelly Tenneson, Steve Weber, Gary Wolfe, Kathy Collins, Eric S Furfine
OBJECTIVE: Topical interleukin (IL)-1 receptor (R)1 blockade is therapeutically active in reducing signs and symptoms of dry eye disease. Herein, we describe in vitro and in vivo nonclinical Investigational New Drug (IND)-enabling studies of EBI-005, a novel protein chimera of IL-1β and IL-1 receptor antagonist (IL-1Ra or anakinra) that potently binds IL-1R1 and blocks signaling. These studies provide an assessment of receptor affinity, drug bioavailability, immunogenic response, safety, and tolerability in mice and rabbits...
July 18, 2017: Eye & Contact Lens
https://www.readbyqxmd.com/read/28727063/effect-of-dietary-fiber-and-diet-particle-size-on-nutrient-digestibility-and-gastrointestinal-secretory-function-in-growing-pigs
#17
M Saqui-Salces, Z Luo, P E Urriola, B J Kerr, G C Shurson
Reduction of diet particle size (PS) increases feed efficiency due to an increase in the apparent total tract (ATTD) of GE. However, other effects of PS on the gut secretory function are not known. Therefore, the objective of this experiment was to measure the effect of diet composition (DC) and PS on nutrient digestibility, gastrointestinal hormones, total bile acids (TBA), total cholesterol and glucose concentrations in plasma of finishing pigs ( = 8/diet). Pigs were fed finely (374 ± 29 µm) or coarsely (631 ± 35 µm) ground corn-soybean meal (CSB), CSB + 35% corn dried distillers' grains with solubles (DDGS), and CSB with 21% soybean hulls (SBH) diets for 49 d...
June 2017: Journal of Animal Science
https://www.readbyqxmd.com/read/28725624/incretin-effect-of-urena-lobata-leaves-extract-on-structure-and-function-of-rats-islet-%C3%AE-cells
#18
Y Purnomo, D W Soeatmadji, S B Sumitro, M A Widodo
This study aims to determine the incretin effects of Urena lobata leaves extract on the structure and function of rats islet β-cells. This study utilizes male Sprague-Dawley rats divided into 2 control group and 3 test group (n = 5). Diabetic rats were induced with High Fructose Diet (HFD) and single dose intraperitoneal streptozotocin 25 mg/kg bw. Aqueous leaves extract of U. lobata was prepared by decoction methods and administrated orally with doses of 250, 500, and 1000 mg/kg bw for 4 weeks then incretin effect was evaluated by measuring serum GLP-1, insulin, and blood glucose levels...
July 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28724693/new-peptide-inhibitor-of-dipeptidyl-peptidase-iv-emdb-1-extends-the-half-life-of-glp-2-and-attenuates-colitis-in-mice-after-topical-administration
#19
Maciej Salaga, Anna Mokrowiecka, Marta Zielinska, Ewa Malecka-Panas, Radzislaw Kordek, Elzbieta Kamysz, Jakub Fichna
Protease inhibition has become a new possible approach in the inflammatory bowel disease (IBD) therapy. A serine exopeptidase, dipeptidyl peptidase IV (DPP IV) is responsible for inactivation of incretine hormone, glucagon-like peptide 2 (GLP-2), a potent stimulator of intestinal epithelium regeneration and growth. Recently we showed that the novel peptide analog of endomorphin-2, EMDB-1 is a potent blocker of DPP IV and has an inhibitory effect on gastrointestinal (GI) smooth muscle contractility. The aim of this study was to characterize the anti-inflammatory effect and mechanism of action of EMDB-1 in the mouse GI tract...
July 19, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28724607/renal-hemodynamic-effects-of-glucagon-like-peptide-1-agonist-are-mediated-by-nitric-oxide-but-not-prostaglandin
#20
Scott Culver Thomson, Ali Kashkouli, Zhi Zhao Liu, Prabhleen Singh
The incretin hormone, glucagon like peptide-1 (GLP-1), is known for responding to dietary fat and carbohydrate. It elicits effects on pancreas, gut, and brain to stabilize blood glucose levels. We have previously reported that the GLP-1 agonist, exenatide, vasodilates the kidney and suppresses proximal reabsorption. The present study was undertaken to determine whether the renal effects of exenatide are mediated by nitric oxide (NO) and/or prostaglandins. Inulin clearance (GFR) and urine flow rate (UV) were measured in anesthetized rats before and during exenatide infusion (1 nmol/h iv)...
July 19, 2017: American Journal of Physiology. Renal Physiology
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