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Qi Li, Jiade Li, Yanli Liu, Mingyu Zhang, Chang Chen
Dipeptidyl peptidase IV (DPP-IV) inhibitors are novel oral anti-hyperglycemic agents. Here, the anti-apoptotic effect of Anagliptin in human umbilical vein endothelial cells (HUVECs) was evaluated. Cultured HUVECs were pre-incubated with Anagliptin, and then treated hydrongen peroxide (H2 O2 ) to induce apoptosis. The apoptosis of HUVECs were detected by viability, LIVE/DEAD staining assay and flow cytometry assays. HUVECs were transfected with plasmid harboring human NADPH oxidases (NOX) 4 or an empty vector...
July 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Eugene A Zubkov, Yana A Zorkina, Elena V Orshanskaya, Nadezhda N Khlebnikova, Natalia A Krupina, Vladimir P Chekhonin
BACKGROUND: Previous studies have shown the development of emotional and motivational disorders, such as anxiety-depression-like disorders with increased aggression in adolescent and adult Wistar rats, occurs after neonatal exposure to the dipeptidyl peptidase-IV (DPP-IV, EC inhibitors diprotin A and sitagliptin (postnatal days 5-18). METHODS: In this study, using real-time PCR, we evaluated changes in the gene expression of serine protease DPP-IV and prolyl endopeptidase (PREP, EC 3...
June 1, 2018: Neuropsychobiology
Giuseppina Catanzaro, Zein Mersini Besharat, Martina Chiacchiarini, Luana Abballe, Claudia Sabato, Alessandra Vacca, Paola Borgiani, Francesco Dotta, Manfredi Tesauro, Agnese Po, Elisabetta Ferretti
The circulating microRNAs (miRNAs) associated with type 2 diabetes (T2D) in elderly patients are still being defined. To identify novel miRNA biomarker candidates for monitoring responses to sitagliptin in such patients, we prospectively studied 40 T2D patients (age > 65) with HbA1c levels of 7.5-9.0% on metformin. After collection of baseline blood samples ( t 0 ), the dipeptidyl peptidase-IV (DPP-IV) inhibitor (DPP-IVi) sitagliptin was added to the metformin regimen, and patients were followed for 15 months...
2018: International Journal of Endocrinology
Momin Mohetaer, Guoqing Li, Yang Wang, Li Cao
Degradation of components of the extracellular matrix such as type II collagen in articular cartilage induced by matrix metalloproteinases (MMPs) has been considered as a major pathological characteristic of osteoarthritis (OA). Gemigliptin is a potent and a highly selective dipeptidyl peptidase-IV (DPP-IV) inhibitor, which has been clinically used as an oral agent for the treatment of type 2 diabetes. However, the effects of gemigliptin on articular cartilage destruction and the pathogenesis of OA remain unknown...
May 22, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Rina Soni, Shubhangi S Soman
DPP-IV "a moonlighting protein" has immerged as promising pathway to control Type 2 diabetes as well as found to play key role in earlier stages of cancer. Here we have reported design, synthesis and applications of aminocoumarin derivatives as DPP-IV inhibitors. Compounds have been synthesized and studied for their DPP-IV inhibition activity. Three compounds have shown moderate inhibition at 100 µM concentration. All compounds were also screened for their anticancer activity against A549 (Lung cancer cell line), MCF-7 (Breast cancer cell line) using MTT assay...
May 17, 2018: Bioorganic Chemistry
Abhinav Sharma, Christopher P Cannon, William B White, Yuyin Liu, George L Bakris, William C Cushman, Faiez Zannad
BACKGROUND: Antihyperglycemic therapies may increase the risk of cardiovascular events including hospitalization for heart failure. There is a paucity of data evaluating the cardiovascular safety of antihyperglycemic therapies in the high-risk period following an acute coronary syndrome (ACS). METHODS AND RESULTS: The EXAMINE (Examination of Cardiovascular Outcomes with Alogliptin versus Standard of Care) trial randomized 5380 patients who were 15 to 90 days post ACS to the dipeptidyl dipeptidase-IV (DPP-IV) inhibitor alogliptin versus placebo; mean follow-up was 18 months...
May 16, 2018: Journal of the American Heart Association
Alan C Cheng, Elizabeth M Doherty, Sheree Johnstone, Erin F DiMauro, Jennifer Dao, Abhinav Luthra, Jay Ye, Jie Tang, Thomas Nixey, Xiaoshan Min, Philip Tagari, Les P Miranda, Zhulun Wang
Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of "chemibodies" as small molecule-antibody hybrids that offer dual recognition of a single target by both a small molecule and an antibody, using DPP-IV enzyme as a proof of concept study. Biochemical characterization demonstrates that the chemibodies present superior DPP-IV inhibition compared to either small molecule or antibody component alone...
May 15, 2018: Scientific Reports
Felicia Hall, Philip E Johnson, Andrea Liceaga
Food-derived bioactive peptides have gained attention for their role in preventing chronic diseases. Edible insects are viable sources of bioactive peptides owing to their high protein content and sustainable production. In this study, whole crickets (Gryllodes sigillatus) were alcalase-hydrolyzed to a degree of hydrolysis (DH) ranging from 15 to 85%. Antioxidant activity, angiotensin converting enzyme (ACE), and dipeptidyl peptidase-4 (DPP-IV)- inhibition of the cricket protein hydrolysates (CPH) were evaluated before and after simulated gastrointestinal digestion (SGD)...
October 1, 2018: Food Chemistry
Gulmira Turdu, Hongwei Gao, Yingying Jiang, Madina Kabas
Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed to solve this increasingly serious global problem. In recent years, inhibition of dipeptidyl peptidase IV (DPP-IV) has emerged as a new treatment option for Type 2 diabetes. This article reviews various plant DPP-IV inhibitors that showed inhibition toward enzyme as a major target for the management of Type 2 diabetes...
May 11, 2018: Future Medicinal Chemistry
Fiona J Dore, Cleyton C Domingues, Neeki Ahmadi, Nabanita Kundu, Yana Kropotova, Sara Houston, Carol Rouphael, Aytan Mammadova, Linda Witkin, Anamil Khiyami, Richard L Amdur, Sabyasachi Sen
AIMS: Type 2 diabetes is associated with endothelial dysfunction leading to cardiovascular disease. CD34+ endothelial Progenitor Cells (EPCs) are responsible for endothelial repair and neo-angiogenesis and can be used as a cardiovascular disease risk biomarker. This study investigated whether the addition of saxagliptin, a DPP-IV inhibitor, to metformin, may reduce cardiovascular disease risk in addition to improving glycemic control in Type 2 diabetes patients. METHODS: In 12 week, double-blind, randomized placebo-controlled trial, 42 subjects already taking metformin 1-2 grams/day were randomized to placebo or saxagliptin 5 mg...
May 3, 2018: Cardiovascular Diabetology
Suncica Buljevic, Dijana Detel, Ester P Pugel, Jadranka Varljen
The involvement of dipeptidyl peptidase (DP) IV/CD26 (DPP IV/CD26) family members in the pathogenesis of Crohn's disease (CD), an autoimmune inflammatory condition of the gut, is effected mainly through proteolytic cleavage of immunomodulatory substrates and DPP IV/CD26's costimulatory function. DP8 and DP9 are proteases with diverse functions including cell interactions, apoptosis, and immune response but their localization remains to be clarified. We assessed the impact of DPP IV/CD26 deficiency (CD26-/- ) on the expression profiles of DP8 and DP9 by qPCR and immunodetection as well as quantified DP8/9 enzyme activity in distinctive phases of a chemically-induced CD model in mice...
April 25, 2018: Journal of Cellular Biochemistry
Priyankar Paira, S K Ashok Kumar, Sourav De, Subhasis Banerjee
Dipeptidyl Peptidase is one of the novel targets for antidiabetic and anticancer drugs. The dipeptidyl amminopeptidase IV, expressed in mammalian, releases X-Pro/Ala dipeptides from the N-terminus of peptides. It is responsible for the degradation of the incretin hormones which regulate blood glucose level. At present several DPP-IV inhibitors are approved for type-2 diabetes mellitus. These enzymes are also expressed in dimeric form on the surface of different cells (mature thymocytes, activated T cells, B cells, NK cells, macrophages, renal, prostate, liver and small intestinal epithelium, biliary canaliculae, and splenic sinus lining cells)...
April 22, 2018: Mini Reviews in Medicinal Chemistry
Priti Mudgil, Hina Kamal, Gan Chee Yuen, Sajid Maqsood
In-vitro inhibitory properties of peptides released from camel milk proteins against dipeptidyl peptidase-IV (DPP-IV), porcine pancreatic α-amylase (PPA), and porcine pancreatic lipase (PPL) were studied. Results revealed that upon hydrolysis by different enzymes, camel milk proteins displayed dramatic increase in inhibition of DPP-IV and PPL, but slight improvement in PPA inhibition was noticed. Peptide sequencing revealed a total of 20 and 3 peptides for A9 and B9 hydrolysates respectively, obtained the score of 0...
September 1, 2018: Food Chemistry
María José Ojeda-Montes, Aleix Gimeno, Sarah Tomas-Hernández, Adrià Cereto-Massagué, Raúl Beltrán-Debón, Cristina Valls, Miquel Mulero, Gerard Pujadas, Santiago Garcia-Vallvé
The inhibition of dipeptidyl peptidase-IV (DPP-IV) has emerged over the last decade as one of the most effective treatments for type 2 diabetes mellitus, and consequently (a) 11 DPP-IV inhibitors have been on the market since 2006 (three in 2015), and (b) 74 noncovalent complexes involving human DPP-IV and drug-like inhibitors are available at the Protein Data Bank (PDB). The present review aims to (a) explain the most important activity cliffs for DPP-IV noncovalent inhibition according to the binding site structure of DPP-IV, (b) explain the most important selectivity cliffs for DPP-IV noncovalent inhibition in comparison with other related enzymes (i...
April 16, 2018: Medicinal Research Reviews
Arpan De, Arianna Pompilio, Jenifer Francis, Iain C Sutcliffe, Gary W Black, Giulio Lupidi, Dezemona Petrelli, Luca A Vitali
Streptococcus mutans, a dental caries causing odontopathogen, produces X-prolyl dipeptidyl peptidase (Sm-XPDAP, encoded by pepX), a serine protease known to have a nutritional role. Considering the potential of proteases as therapeutic targets in pathogens, this study was primarily aimed at investigating the role of Sm-XPDAP in contributing to virulence-related traits. Dipeptidyl peptidase (DPP IV), an XPDAP analogous enzyme found in mammalian tissues,is a well known therapeutic target in Type II diabetes. Based on the hypothesis that gliptins, commonly used as anti-human-DPP IV drugs, may affect bacterial growth upon inhibition of Sm-XPDAP, we have determined their ex vivo antimicrobial and anti-biofilm activity towards S...
April 2018: Microbiological Research
Pádraigín A Harnedy, Vadivel Parthsarathy, Chris M McLaughlin, Martina B O'Keeffe, Philip J Allsopp, Emeir M McSorley, Finbarr P M O'Harte, Richard J FitzGerald
Large quantities of low-value protein rich co-products, such as salmon skin and trimmings, are generated annually. These co-products can be upgraded to high-value functional ingredients. The aim of this study was to assess the antidiabetic potential of salmon skin gelatin and trimmings-derived protein hydrolysates in vitro. The gelatin hydrolysate generated with Alcalase 2.4L and Flavourzyme 500L exhibited significantly higher (p < 0.001) insulin and GLP-1 secretory activity from pancreatic BRIN-BD11 and enteroendocrine GLUTag cells, respectively, when tested at 2...
April 2018: Food Research International
Monica Serra, Michela Marongiu, Antonella Contini, Toshio Miki, Erika Cadoni, Ezio Laconi, Fabio Marongiu
Amniotic epithelial cells (AECs) represent a useful and noncontroversial source for liver-based regenerative medicine, as they can differentiate into hepatocytes upon transplantation into the liver. However, the possibility that AECs can differentiate into other liver cell types, such as hepatic sinusoidal endothelial cells (HSECs), has never been assessed. In order to test this hypothesis, rat- and human-derived AECs (rAECs and hAECs, respectively) were subjected to endothelial cell tube formation assay in vitro...
January 2018: Cell Transplantation
Chi Zhang, Huaigao Liu, Shangwu Chen, Yongkang Luo
Dipeptidyl peptidase-IV (DPP-IV) is a serine exo-peptidase that can inactivate incretins by removing N-terminal dipeptides. Currently, inhibiting the DPP-IV activity is a common treatment for type 2 diabetes (T2D). The goal of this study is to investigate whether IADHFL, a novel DPP-IV inhibitory peptide identified from bighead carp (Hypophthalmichthys nobilis), has the potential to modulate T2D. IADHFL remained stable after simulated gastrointestinal digestion and significantly decreased the activity and expression of both soluble and membrane-bound DPP-IV after 24 h and 48 h of treatment...
April 25, 2018: Food & Function
Rajesh B Patil, Euzebio G Barbosa, Jaiprakash N Sangshetti, Vishal P Zambre, Sanjay D Sawant
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are promising antidiabetic agents. Currently, several DPP-IV inhibitors have been approved for therapeutic use in diabetes mellitus. Receptor-dependent 4D-QSAR is comparatively a new approach which uses molecular dynamics simulations to generate conformational ensemble profiles of compounds representing a dynamic state of compounds at a target's binding site. This work describes a receptor-dependent 4D-QSAR study on triazolopiperazine derivatives. QSARINS multiple linear regression method was adopted to generate 4D-QSAR models...
March 13, 2018: Molecular Diversity
Miriam Moreno-Montoro, Paula Jauregi, Miguel Navarro-Alarcón, Manuel Olalla-Herrera, Rafael Giménez-Martínez, Lourdes Amigo, Beatriz Miralles
In this study, ultrafiltered goat milks fermented with the classical starter bacteria Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus salivarus subsp. thermophilus or with the classical starter plus the Lactobacillus plantarum C4 probiotic strain were analyzed using ultra-high performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS/MS) and/or high performance liquid chromatography-ion trap (HPLC-IT-MS/MS). Partial overlapping of the identified sequences with regard to fermentation culture was observed...
June 2018: Analytical and Bioanalytical Chemistry
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