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https://www.readbyqxmd.com/read/28326327/ameliorating-effect-of-gemigliptin-on-renal-injury-in-murine-adriamycin-induced-nephropathy
#1
Da Rae Kim, Shin Yeong Lee, Jin Sug Kim, Yang Gyun Kim, Ju-Young Moon, Sang Ho Lee, Tae Won Lee, Chun Gyoo Ihm, Kyung Hwan Jeong
Background. Previous studies have shown the antiapoptotic and anti-inflammatory potential of DPP-IV inhibitor in experimental models of renal injury. We tested whether DPP-IV inhibitor (gemigliptin) ameliorates renal injury by suppressing apoptosis, inflammation, and oxidative stress in mice with adriamycin nephropathy. Methods. Mice were treated with normal saline (control), gemigliptin (GM), adriamycin (ADR), or adriamycin combined with gemigliptin (ADR+GM). Apoptosis, inflammation, and oxidative stress were analyzed via western blotting, real-time PCR, light microscopy, and immunofluorescence...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28318663/dipeptidyl-peptidase-iv-in-chronic-heart-failure-with-reduced-ejection-fraction
#2
Patrícia Lourenço, Sérgio Silva, Filipe Cunha, Joana Pereira, Ana Ribeiro, Nuno Silva, João Tiago Guimarães, José Paulo Araújo, Paulo Bettencourt
BACKGROUND: An association between dipeptidyl peptidase-IV (DPP-IV) inhibitors with worse prognosis in HF has been suggested. We aimed to assess the serum DPP-IV levels in chronic stable HF patients and determine their association with prognosis. METHODS AND RESULTS: Chronic stable HF patients with optimized prognostic-modifying therapy were prospectively recruited. EXCLUSION CRITERIA: 1) ejection fraction>50%, 2) hospitalizations or therapeutic adjustments in the previous 2months; 3) patients on renal replacement therapy, and 4) use of DPP-IV inhibitors...
March 11, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28292762/gpr40-reduces-food-intake-and-body-weight-through-glp-1
#3
Judith N Gorski, Michele J Pachanski, Joel Mane, Christopher W Plummer, Sarah Souza, Brande S Thomas-Fowlkes, Aimie M Ogawa, Adam B Weinglass, Jerry Di Salvo, Boonlert Cheewatrakoolpong, Andrew D Howard, Steven L Colletti, Maria E Trujillo
GPR40 partial agonists lower glucose through the potentiation of glucose-stimulated insulin secretion, which is believed to provide significant glucose lowering without the weight gain or hypoglycemic risk associated with exogenous insulin or glucose independent insulin secretagogues. The class of small molecule GPR40 modulators, known as AgoPAMs (agonist also capable of acting as positive allosteric modulators), differentiate from partial agonists, binding to a distinct site and functioning as full agonists to stimulate the secretion of both insulin and GLP-1 (17)...
March 14, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28290371/release-of-dipeptidyl-peptidase-iv-dpp-iv-inhibitory-peptides-from-milk-protein-isolate-mpi-during-enzymatic-hydrolysis
#4
Alice B Nongonierma, Caterina Mazzocchi, Sara Paolella, Richard J FitzGerald
The release of dipeptidyl peptidase IV (DPP-IV) inhibitory peptides from bovine milk protein isolate (MPI) during trypsin hydrolysis was studied using a design of experiments (DOE) approach. A 3 factor×3 level DOE including temperature (40, 50 and 60°C), enzyme to substrate ratio (E:S; 0.50, 1.25 and 2.00% (w/w)) and hydrolysis time (60, 150 and 240min) was used during the generation of 15 hydrolysates (H1-H15). The degree of hydrolysis (DH) varied between 6.98±0.31 (H8) to 12.75±0.62% (H10). The DPP-IV half maximal inhibitory concentration (IC50) ranged from 0...
April 2017: Food Research International
https://www.readbyqxmd.com/read/28290288/using-caco-2-cells-as-novel-identification-tool-for-food-derived-dpp-iv-inhibitors
#5
Juliette Caron, Dorothée Domenger, Pascal Dhulster, Rozenn Ravallec, Benoit Cudennec
Dietary proteins have recently been investigated as a new source of DPP-IV inhibitory peptides with limited side effects and promising applications. Numerous studies have highlighted and identified peptide sequences able to inhibit DPP-IV activity in vitro, mostly from milk proteins. However, the correlation to in vivo studies remains scarce because standard in vitro assays with purified enzyme do not accurately simulate key factors impacting peptide bioactivity such as intestinal and brush border enzymes or cellular permeability...
February 2017: Food Research International
https://www.readbyqxmd.com/read/28276830/bariatric-surgery-time-to-replace-with-glp-1
#6
Dominic-Luc Webb, Niclas Abrahamsson, Magnus Sundbom, Per M Hellström
Obesity with a body mass index (BMI) over 30 kg/m(2) represents a significant risk for increased morbidity and mortality, with reduced life expectancy of about 10 years. Until now, surgical treatment has been the only effective longterm intervention. The currently standardized method of bariatric surgery, gastric bypass, means that many gastrointestinal peptide hormones are activated, yielding net reductions in appetite and food intake. Among the most important gut peptide hormones in this perspective is glucagon-like peptide-1 (GLP-1), which rises sharply after gastric bypass...
February 24, 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28155144/enzyme-histochemistry-technique-for-visualizing-the-dipeptidyl-peptidase-iv-dpp-iv-activity-in-the-liver-biliary-tree
#7
Vittorio Bertone, Eleonora Tarantola, Isabel Freitas
Dipeptidyl-peptidase IV is an enzyme involved in a lot of biochemical processes, where it modifies a number of regulatory proteins by removing the terminal peptides by hydrolysis. Here we describe a histochemical method to demonstrate with accuracy and precision its in situ activity on cryostatic section of Wistar rat liver by means of a simultaneous azo-coupling method.
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28155089/predicting-dpp-iv-inhibitors-with-machine-learning-approaches
#8
Jie Cai, Chanjuan Li, Zhihong Liu, Jiewen Du, Jiming Ye, Qiong Gu, Jun Xu
Dipeptidyl peptidase IV (DPP-IV) is a promising Type 2 diabetes mellitus (T2DM) drug target. DPP-IV inhibitors prolong the action of glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP), improve glucose homeostasis without weight gain, edema, and hypoglycemia. However, the marketed DPP-IV inhibitors have adverse effects such as nasopharyngitis, headache, nausea, hypersensitivity, skin reactions and pancreatitis. Therefore, it is still expected for novel DPP-IV inhibitors with minimal adverse effects...
February 2, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28119159/hindbrain-dpp-iv-inhibition-improves-glycemic-control-and-promotes-negative-energy-balance
#9
Elizabeth G Mietlicki-Baase, Lauren E McGrath, Kieran Koch-Laskowski, Joanna Krawczyk, Tram Pham, Rinzin Lhamo, David J Reiner, Matthew R Hayes
The beneficial glycemic and food intake-suppressive effects of glucagon-like peptide-1 (GLP-1) have made this neuroendocrine system a leading target for pharmacological approaches to the treatment of diabetes and obesity. One strategy to increase the activity of endogenous GLP-1 is to prevent the rapid degradation of the hormone by the enzyme dipeptidyl peptidase-IV (DPP-IV). However, despite the expression of both DPP-IV and GLP-1 in the brain, and the clear importance of central GLP-1 receptor (GLP-1R) signaling for glycemic and energy balance control, the metabolic effects of central inhibition of DPP-IV activity are unclear...
January 22, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28098291/investigation-into-the-bioavailability-of-milk-protein-derived-peptides-with-dipeptidyl-peptidase-iv-inhibitory-activity-using-caco-2-cell-monolayers
#10
Isabelle M E Lacroix, Xiu-Min Chen, David D Kitts, Eunice C Y Li-Chan
In recent years, peptides derived from a variety of dietary proteins have been reported to exhibit inhibitory activity against the dipeptidyl-peptidase IV (DPP-IV) enzyme, a target in the management of type 2 diabetes. While much attention has been given to the production and identification of peptides with DPP-IV inhibitory activity from food proteins, particularly dairy proteins, little is known on the bioavailability of these molecules. In this study, the stability and transport of five previously identified milk-derived peptides (LKPTPEGDL, LPYPY, IPIQY, IPI and WR) and a whey protein isolate (WPI) digest with DPP-IV-inhibitory activity were investigated using Caco-2 cell monolayers as a model system for human intestinal absorption...
January 18, 2017: Food & Function
https://www.readbyqxmd.com/read/28062644/ligand-induced-conformational-changes-in-prolyl-oligopeptidase-a-kinetic-approach
#11
R Van Elzen, E Schoenmakers, I Brandt, P Van Der Veken, A M Lambeir
Most kinetic studies of prolyl oligopeptidase (PREP) were performed with the porcine enzyme using modified peptide substrates. Yet recent biophysical studies used the human homolog. Therefore, the aim of this study was to compare the kinetic behavior of human and porcine PREP, as well as to find a suitable method to study enzyme kinetics with an unmodified biological substrate. It was found that human PREP behaves identically to the porcine homolog, displaying a double bell-shaped pH profile and a pH-dependent solvent kinetic isotope effect of the kcat/Km, features that set it apart from the related exopeptidase dipeptidyl peptidase IV (DPP IV)...
January 5, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/27990119/oral-administration-of-sitagliptin-activates-creb-and-is-neuroprotective-in-murine-model-of-brain-trauma
#12
Brian DellaValle, Gitte S Brix, Birgitte Brock, Michael Gejl, Jørgen Rungby, Agnete Larsen
Introduction: Traumatic brain injury is a major cause of mortality and morbidity. We have previously shown that the injectable glucagon-like peptide-1 (GLP-1) analog, liraglutide, significantly improved the outcome in mice after severe traumatic brain injury (TBI). In this study we are interested in the effects of oral treatment of a different class of GLP-1 based therapy, dipeptidyl peptidase IV (DPP-IV) inhibition on mice after TBI. DPP-IV inhibitors reduce the degradation of endogenous GLP-1 and extend circulation of this protective peptide in the bloodstream...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27983830/peptides-derived-from-soy-and-lupin-protein-as-dipeptidyl-peptidase-iv-inhibitors-in-vitro-biochemical-screening-and-in-silico-molecular-modeling-study
#13
Carmen Lammi, Chiara Zanoni, Anna Arnoldi, Giulio Vistoli
Dipeptidyl peptidase IV (DPP-IV) is a new molecular target correlated with the development of type 2 diabetes. Literature describes the identification of some inhibitory peptides from the hydrolysis of different food proteins. This article reports a study on six peptides from soybean and lupin proteins, i.e., Soy 1 (IAVPTGVA), Soy 2 (YVVNPDNDEN), Soy 3 (YVVNPDNNEN), Lup 1 (LTFPGSAED), Lup 2 (LILPKHSDAD), and Lup 3 (GQEQSHQDEGVIVR), which were screened for their capacity to inhibit the activity of DPP-IV, using an in vitro bioassay against human recombinant DPP-IV...
December 28, 2016: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/27970351/tct-180-impact-of-the-novel-dpp-iv-inhibitor-dutogliptin-in-combination-with%C3%A2-g-csf-on-survival-rates-and-cardiac-remodelling-after-acute-myocardial%C3%A2-infarction
#14
Roman Schenk, Darrell Nix
No abstract text is available yet for this article.
November 1, 2016: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/27923191/a-highly-specific-ratiometric-two-photon-fluorescent-probe-to-detect-dipeptidyl-peptidase-iv-in-plasma-and-living-systems
#15
Li-Wei Zou, Ping Wang, Xing-Kai Qian, Lei Feng, Yang Yu, Dan-Dan Wang, Qiang Jin, Jie Hou, Zhi-Hong Liu, Guang-Bo Ge, Ling Yang
In this study, a highly specific ratiometric two-photon fluorescent probe GP-BAN was developed and well-characterized to monitor dipeptidyl peptidase IV in plasma and living systems. GP-BAN was designed on the basis of the catalytic properties and substrate preference of DPP-IV, and it could be readily hydrolyzed upon addition of DPP-IV under physiological conditions. Both reaction phenotyping and inhibition assays demonstrated that GP-BAN displayed good reactivity and high selectivity towards DPP-IV over other human serine hydrolases including FAP, DPP-VIII, and DPP-IX...
April 15, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/27868279/involvement-of-dpp-iv-cd26-in-cutaneous-wound-healing-process-in-mice
#16
Lara Baticic Pucar, Ester Pernjak Pugel, Dijana Detel, Jadranka Varljen
Dipeptidyl peptidase IV (DPP IV/CD26) is a widely distributed multifunctional protein that plays a significant role in different physiological as well as pathological processes having a broad spectrum of bioactive substrates and immunomodulative properties. It has potential influence on different processes crucial for wound healing, including cell adhesion, migration, apoptosis, and extracellular matrix degradation. However, despite its known enzymatic and immunomodulative functions, limited data characterize the role of DPP IV/CD26 in cutaneous wound healing mechanisms...
November 21, 2016: Wound Repair and Regeneration
https://www.readbyqxmd.com/read/27806063/biomarker-profiles-in-women-with-pcos-and-pcos-offspring-a-pilot-study
#17
Nadine M P Daan, Maria P H Koster, Marlieke A de Wilde, Gerdien W Dalmeijer, Annemieke M V Evelein, Bart C J M Fauser, Wilco de Jager
OBJECTIVE: To study metabolic/inflammatory biomarker risk profiles in women with PCOS and PCOS offspring. DESIGN: Cross-sectional comparison of serum biomarkers. SETTING: University Medical Center Utrecht. PATIENTS: Hyperandrogenic PCOS women (HA-PCOS, n = 34), normoandrogenic PCOS women (NA-PCOS, n = 34), non-PCOS reference population (n = 32), PCOS offspring (n = 14, age 6-8 years), and a paedriatic reference population (n = 30)...
2016: PloS One
https://www.readbyqxmd.com/read/27761990/effects-of-renal-impairment-on-the-pharmacokinetics-and-pharmacodynamics-of-a-novel-dipeptidyl-peptidase-4-inhibitor-evogliptin-da-1229
#18
Jaeseong Oh, Andrew HyoungJin Kim, SeungHwan Lee, Hyunjeong Cho, Yon Su Kim, Mi Young Bahng, Seo Hyun Yoon, Joo-Youn Cho, In-Jin Jang, Kyung-Sang Yu
Evogliptin is a novel potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor. The aim of the present study was to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of evogliptin in participants with renal impairment (RI). An open-label, parallel-group clinical study was conducted in participants with mild, moderate and severe RI and in matched participants with normal renal function (NRF). A single oral 5-mg dose of evogliptin was administered and serial blood and urine samples were obtained to assess the PK and PD characteristics of evogliptin...
October 20, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27723572/zinc-oxide-nanoparticles-and-a-standard-antidiabetic-drug-restore-the-function-and-structure-of-beta-cells-in-type-2-diabetes
#19
Rehab Mohmed El-Gharbawy, Ashraf Mahmoud Emara, Sally El-Sayed Abu-Risha
The aim of this study was to use Zinc oxide nanoparticles and a standard antidiabetic drug to restore the function and structure of beta cells in a rat model of Type-2 diabetes and compare the effects of a DPP-IV inhibitor with or without zinc oxide nanoparticles (ZnONPs) using a model of type 2 diabetes (rats fed a high fat diet that was treated with a low dose of streptozotocin). Ninety male Wistar rats were randomly divided into three groups 10days after the induction of diabetes: group I: non-diabetic animals that received only the chow diet plus 2ml of 0...
December 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27719926/bioactive-peptides-from-atlantic-salmon-salmo-salar-with-angiotensin-converting-enzyme-and-dipeptidyl-peptidase-iv-inhibitory-and-antioxidant-activities
#20
Adriana C Neves, Pádraigín A Harnedy, Martina B O'Keeffe, Richard J FitzGerald
The pH shift method was utilised for the recovery of proteins from salmon trimmings (ST), yielding 93% (w/w) protein. ST protein (STP) hydrolysates were generated with different enzyme preparations. STP incubated with Corolase PP for 1h (STP-C1) had the most potent angiotensin converting enzyme (ACE) and dipeptidyl peptidase IV (DPP-IV) inhibitory and oxygen radical absorbance capacity (ORAC) activities. Analysis of fractions of STP-C1 using UPLC-MS/MS identified sixteen peptides/amino acids. Tyr-Pro had the highest ACE inhibitory activity (ACE IC50=5...
March 1, 2017: Food Chemistry
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