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https://www.readbyqxmd.com/read/29580624/antidiabetic-gliptins-affect-biofilm-formation-by-streptococcus-mutans
#1
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
https://www.readbyqxmd.com/read/29579965/atlantic-salmon-salmo-salar-co-product-derived-protein-hydrolysates-a-source-of-antidiabetic-peptides
#2
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
https://www.readbyqxmd.com/read/29562778/evidence-of-amniotic-epithelial-cell-differentiation-toward-hepatic-sinusoidal-endothelial-cells
#3
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
https://www.readbyqxmd.com/read/29553151/evaluating-the-effects-of-iadhfl-on-inhibiting-dpp-iv-activity-and-expression-in-caco-2-cells-and-contributing-to-the-amount-of-insulin-released-from-ins-1-cells-in-vitro
#4
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...
March 19, 2018: Food & Function
https://www.readbyqxmd.com/read/29536226/structural-insights-of-dipeptidyl-peptidase-iv-inhibitors-through-molecular-dynamics-guided-receptor-dependent-4d-qsar-studies
#5
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
https://www.readbyqxmd.com/read/29523944/bioaccessible-peptides-released-by-in-vitro-gastrointestinal-digestion-of-fermented-goat-milks
#6
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...
March 10, 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29522713/replacement-of-the-c-terminal-trp-cage-of-exendin-4-with-a-fatty-acid-improves-therapeutic-utility
#7
Jung Gi Lee, Jae Ha Ryu, Seon-Myung Kim, Moon-Young Park, San-Ho Kim, Young G Shin, Jong-Woo Sohn, Ha Hyung Kim, Zee-Yong Park, Jae Young Seong, Jae Il Kim
Exendin-4, a 39 amino acid peptide isolated from the saliva of the Gila monster, plays an important role in regulating glucose homeostasis, and is used clinically for the treatment of type 2 diabetes. Exendin-4 shares 53% sequence identity with the incretin hormone glucagon-like peptide 1 (GLP-1) but, unlike GLP-1, is highly resistant to proteolytic enzymes such as dipeptidyl peptidase IV (DPP-IV) and neutral endopeptidase 24.11 (NEP 24.11). Herein, we focused on the structure and function of the C-terminal Trp-cage of exendin-4, and suggest that it may be structurally required for resistance to proteolysis by NEP 24...
March 6, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29521244/synthesis-structural-characterization-and-docking-studies-of-sulfamoyl-phenyl-acid-esters-as-dpp-iv-inhibitors
#8
Reema Abdelkareem Abu Khalaf, Dima Sabbah, Eveen Al-Shalabi, Iyad Al-Sheikh, Ghadeer Albadawi, Ghassan Abu Sheikha
BACKGROUND: Diabetes mellitus is a major worldwide health concern that has several serious complications including retinopathy, neuropathy, nephropathy and macrovascular diseases. OBJECTIVE: Dipeptidyl peptidase-IV (DPP-IV) inhibitors, gliptins, are a new class of antidiabetic agents that potentiates the action of incretins in decreasing the blood glucose levels. METHODS: In the present study, synthesis and characterization of a series of ten N4-sulfonamido-acrylic and phthalamic acid methyl esters (3a-e and 5a-e) were achieved...
March 8, 2018: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/29520469/reduced-salivary-amylase-activity-in-metabolic-syndrome-patients-with-obesity-could-be-improved-by-treatment-with-a-dipeptidyl-peptidase-iv-inhibitor
#9
Jitjiroj Ittichaicharoen, Arintaya Phrommintikul, Nipon Chattipakorn, Siriporn Chattipakorn
OBJECTIVES: The present study is to investigate the salivary gland function of metabolic syndrome (MetS) patients, as indicated by salivary flow rate, amylase activity, and salivary oxidative stress, by measuring MDA level. MATERIALS AND METHODS: One hundred and eighty-one MetS patients from Maharaj Nakorn Chiang Mai Hospital were enrolled onto this study. The metabolic parameters of each patient were collected and evaluated. Unstimulated saliva was also collected for 5 min...
March 8, 2018: Clinical Oral Investigations
https://www.readbyqxmd.com/read/29511780/evaluation-of-pharmacokinetic-and-pharmacodynamic-parameters-following-single-dose-of-sitagliptin-in-healthy-indian-males
#10
Ganesh V Sangle, Mohan Patil, Nitin J Deshmukh, Sushant A Shengule, Shantibhushan Kamble, Kiran Kumar Vuppalavanchu, Sushil Kale, Mirza Layeeq Ahmed Baig, Geetchandra Singh, Javed Shaikh, Jitendra Tripathi, P Aravindababu
PURPOSE: Sitagliptin, a dipeptidyl peptidase (DPP)-IV inhibitor approved for the treatment of type 2 diabetes, is reported to be more efficacious in Indian patients than non-Indian patient population. The objective of the study was to evaluate pharmacokinetic and pharmacodynamic (PK/PD) parameters of single-dose sitagliptin 100 mg (Januvia) in healthy Indian male participants. METHOD: In a randomised, single-dose, open-label, three-treatment, three-period, three-sequence, crossover bioavailability study, 18 healthy male participants received single-dose of sitagliptin under fasted and fed conditions...
March 6, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29509281/rapid-detection-of-superficial-head-and-neck-squamous-cell-carcinoma-by-topically-spraying-fluorescent-probe-targeting-dipeptidyl-peptidase-iv
#11
Takeshi Mizushima, Shunsuke Ohnishi, Yuichi Shimizu, Yutaka Hatanaka, Kanako C Hatanaka, Yugo Kuriki, Mako Kamiya, Akihiro Homma, Keiko Yamamoto, Shouko Ono, Yasuteru Urano, Naoya Sakamoto
BACKGROUND: A fluorescent probe glutamylprolyl hydroxymethyl rhodamine green (EP-HMRG), which becomes fluorescent after cleavage by dipeptidyl peptidase-IV (DPP-IV), has been reported to be useful for the detection of esophageal cancer. Thus, we investigated whether head and neck squamous cell carcinoma (HNSCC) can be detected by spraying EP-HMRG. METHODS: Fluorescence imaging of 17 cases of HNSCCs resected using endoscopic or surgical resection was performed ex vivo after spraying EP-HMRG, and then the fluorescence intensity of the tumors and normal mucosa were measured...
March 6, 2018: Head & Neck
https://www.readbyqxmd.com/read/29493459/anti-diabetic-phenolic-compounds-of-black-carrot-daucus-carota-subspecies-sativus-var-atrorubens-alef-inhibit-enzymes-of-glucose-metabolism-an-in-silico-and-in-vitro-validation
#12
Suhas Gorakh Karkute, Tanmay Kumar Koley, Bijen Kumar Yengkhom, Ajay Tripathi, Shivani Srivastava, Arti Maurya, Bijendra Singh
BACKGROUND: Black carrot is known to be effective against Type 2 diabetes. The phenolic compounds present in black carrot are responsible for this property, but limited information was available about the mechanism of action and target enzymes. OBJECTIVE: The present study aims at understanding molecular interactions of phenolic compounds of black carrot with enzymes involved in glucose metabolism in human to identify the potential inhibitor that can be used as candidate drug molecule to control diabetes...
February 28, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29493228/an-activatable-near-infrared-fluorescent-probe-for-dipeptidyl-peptidase-iv-and-its-bioimaging-applications-in-living-cells-and-animals
#13
Tao Liu, Jing Ning, Bo Wang, Bin Dong, Song Li, Xiangge Tian, Zhenlong Yu, Yulin Peng, Chao Wang, Xinyu Zhao, Xiaokui Huo, Cheng-Peng Sun, Jing-Nan Cui, Lei Feng, Xiaochi Ma
Visualization of endogenous disease-associated enzymes is of great clinical significance, as it could allow earlier clinical diagnosis and timely intervention. Herein, we first synthesized and characterized an enzyme-activatable near-infrared fluorescent probe, GP-DM, for determining the activity of dipeptidyl peptidase IV (DPP IV), which is associated with various pathological processes, especially in diabetes and malignant tumors. GP-DM emitted significant turn-on NIR fluorescent signals simultaneously in response to DPP IV, making it favorable for accurately and dynamically monitoring DPP IV activity in vitro and in vivo...
March 1, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29473848/bovine-%C3%AE-lactalbumin-hydrolysates-%C3%AE-lah-ameliorate-adipose-insulin-resistance-and-inflammation-in-high-fat-diet-fed-c57bl-6j-mice
#14
Jing Gao, Jiajia Song, Min Du, Xueying Mao
Obesity-induced adipose inflammation has been demonstrated to be a key cause of insulin resistance. Peptides derived from bovine α-lactalbumin have been shown to inhibit the activities of dipeptidyl peptidase IV (DPP-IV) and angiotensin converting enzyme (ACE), scavenge 2,2'-azinobis [3-ethylbenzothiazoline-6-sulfonate] (ABTS⁺) radical and stimulate glucagon-like peptide-2 secretion. In the present study, the effects of bovine α-lactalbumin hydrolysates (α-LAH) on adipose insulin resistance and inflammation induced by high-fat diet (HFD) were investigated...
February 23, 2018: Nutrients
https://www.readbyqxmd.com/read/29462810/consumption-of-amaranth-induces-the-accumulation-of-the-antioxidant-protein-paraoxonase-arylesterase-1-and-modulates-dipeptidyl-peptidase-iv-activity-in-plasma-of-streptozotocin-induced-hyperglycemic-rats
#15
Aída J Velarde-Salcedo, Evelyn Regalado-Rentería, Rodrigo Velarde-Salcedo, Bertha I Juárez-Flores, Alberto Barrera-Pacheco, Elvira González de Mejía, Ana P Barba de la Rosa
BACKGROUND/AIM: Amaranth is a source of several bioactive compounds, among which peptides with inhibitory activity upon dipeptidyl peptidase IV (DPP-IV) have been reported. However, there is no information about the action of amaranth DPP-IV-inhibitory peptides using in vivo models. The aim of this work was to evaluate the effect of amaranth consumption on plasma and kidney DPP-IV activity as well the changes in plasma proteome profile of streptozotocin (STZ)-induced hyperglycemic rats...
February 20, 2018: Journal of Nutrigenetics and Nutrigenomics
https://www.readbyqxmd.com/read/29451201/tackling-dipeptidyl-peptidase-iv-in-neurological-disorders
#16
REVIEW
Ghaith Al-Badri, Gian Marco Leggio, Giuseppe Musumeci, Rubina Marzagalli, Filippo Drago, Alessandro Castorina
Dipeptidyl peptidase IV (DPP-IV) is a serine protease best known for its role in inactivating glucagon-like peptide-1 (GLP-1), pituitary adenylate cyclase-activating polypeptide (PACAP) and glucose-dependent insulinotropic peptide (GIP), three stimulators of pancreatic insulin secretion with beneficial effects on glucose disposal. Owing to the relationship between DPP-IV and these peptides, inhibition of DPP-IV enzyme activity is considered as an attractive treatment option for diabetic patients. Nonetheless, increasing studies support the idea that DPP-IV might also be involved in the development of neurological disorders with a neuroinflammatory component, potentially through its non-incretin activities on immune cells...
January 2018: Neural Regeneration Research
https://www.readbyqxmd.com/read/29442423/impact-of-type-1-diabetes-mellitus-and-sitagliptin-treatment-on-the-neuropeptide-y-system-of-rat-retina
#17
Elisa J Campos, João Martins, Dan Brudzewsky, Sandra Correia, Ana R Santiago, David Pd Woldbye, António F Ambrósio
BACKGROUND: Neuropeptide Y (NPY) is a neuromodulator that is expressed in the retina. Increasing evidence suggests that NPY has pronounced anti-inflammatory effects, which might depend on the inhibition of dipeptidyl-peptidase-IV (DPP-IV). The aim of this study was to investigate the impact of type 1 diabetes mellitus (DM) and sitagliptin, a DPP-IV inhibitor, on the NPY system in the retina using an animal model. METHODS: Type 1 DM was induced in male Wistar rats by an intraperitoneal injection of streptozotocin (STZ)...
February 14, 2018: Clinical & Experimental Ophthalmology
https://www.readbyqxmd.com/read/29433298/chemical-composition-and-inhibitory-activities-on-dipeptidyl-peptidase-iv-and-pancreatic-lipase-of-two-underutilized-species-from-the-brazilian-savannah-oxalis-cordata-a-st-hil-and-xylopia-aromatica-lam-mart
#18
Verena B Oliveira, Raquel L B Araújo, Thomas Eidenberger, Maria G L Brandão
Brazil has the greatest vegetal biodiversity in the world, but products derived from native species are not optimally utilized. Oxalis cordata and Xylopia aromatica are two underutilized species whose leaves and fruits, respectively, have been used as food in the 19th century. In this study, we used chemical and in vitro assays to evaluate the potential of these species as functional foods. The inhibitory activity on pancreatic lipase and DPP-IV were evaluated using the crude extracts and fractions ethyl acetate, butanol and water of these two species...
March 2018: Food Research International
https://www.readbyqxmd.com/read/29430979/an-effective-treatment-approach-of-dpp-iv-inhibitor-encapsulated-polymeric-nano-particles-conjugated-with-anti-cd-4-mab-for-type-1-diabetes
#19
Mahesh Thondawada, Ashish Devidas Wadhwani, Dhanabal S Palanisamy, Hanumant Singh Rathore, Ramesh C Gupta, Pavan Kumar Chintamaneni, Malay K Samanta, Anil Dubala, Sameer Varma, Praveen T Krishnamurthy, Kuppusamy Gowthamarajan
Nanotechnology based bio-medical approaches and surface modification techniques made it easier for targeting specific site and improving the treatment efficacy. The present study reports on targeted polymeric nanoparticles conjugated with antibody as a site-specific carrier system for effective treatment of Type 1 diabetes. Sitagliptin (SP) loaded Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NP) were prepared by nanoprecipitation cum solvent evaporation method and were characterized in terms of morphology, size, surface charge and entrapment efficiency...
February 12, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29426867/crystal-structures-of-a-bacterial-dipeptidyl-peptidase-iv-reveal-a-novel-substrate-recognition-mechanism-distinct-from-that-of-mammalian-orthologues
#20
Saori Roppongi, Yoshiyuki Suzuki, Chika Tateoka, Mayu Fujimoto, Saori Morisawa, Ippei Iizuka, Akihiro Nakamura, Nobuyuki Honma, Yosuke Shida, Wataru Ogasawara, Nobutada Tanaka, Yasumitsu Sakamoto, Takamasa Nonaka
Dipeptidyl peptidase IV (DPP IV, DPP4, or DAP IV) preferentially cleaves substrate peptides with Pro or Ala at the P1 position. The substrate recognition mechanism has been fully elucidated for mammalian DPP IV by crystal structure analyses but not for bacterial orthologues. Here, we report the crystal structures of a bacterial DPP IV (PmDAP IV) in its free form and in complexes with two kinds of dipeptides as well as with a non-peptidyl inhibitor at 1.90 to 2.47 Å resolution. Acyl-enzyme intermediates were observed for the dipeptide complexes of PmDAP IV, whereas tetrahedral intermediates were reported for the oligopeptide complexes of mammalian DPP IVs...
February 9, 2018: Scientific Reports
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