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Amir M Abdelhamid, Rania Ramadan Abdelaziz, Hatem A Salem
Type I diabetes (TID) is generally assumed to be caused by an immune associated, if not directly immune-mediated, destruction of pancreatic β-cells. In patients with long-term diabetes, the pancreas lacks insulin-producing cells and the residual β-cells are unable to regenerate. Patients with TID are subjected to a lifelong insulin therapy which shows risks of hypoglycemia, suboptimal control and ketosis. In this study, we investigated the potential role of Vildagliptin (Vilda) alone or in combination with Pioglitazone (Pio), as treatment regimens for TID using Streptozotocin (STZ) induced TID model in rats...
March 6, 2018: Canadian Journal of Physiology and Pharmacology
Wathik Alsalim, Margaretha Persson, Bo Ahrén
AIMS: Previous studies have shown that dipeptidyl peptidase (DPP)-4 inhibition lowers whereas sodium-glucose co-transporter 2 (SGLT-2) inhibition increases glucagon levels. This study evaluated the extent of these opposite effects in a direct comparative head-to-head study. METHODS: In a single-centre, randomized study with a cross-over design, 28 metformin-treated patients with type 2 diabetes (T2D; mean age 63 years, baseline HbA1c 6.8%) were treated with vildagliptin (50 mg twice daily) or dapagliflozin (10 mg once daily) for two weeks with a four week wash out period in between...
March 2, 2018: Diabetes, Obesity & Metabolism
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
Kanta Fujimoto, Yui Shibayama, Eriko Yamaguchi, Sachiko Honjo, Akihiro Hamasaki, Yoshiyuki Hamamoto
BACKGROUND: Glucose excursions and hypoglycemia are associated with cardiovascular complications. However, no studies have evaluated glucose excursions and the frequency of hypoglycemia in patients treated with mitiglinide/voglibose versus glimepiride as add-on to dipeptidyl peptidase-4 inhibitor therapy. METHODS: This cross-over trial included 20 patients with type 2 diabetes. After initiating vildagliptin 100 mg, patients were randomly assigned to receive mitiglinide/voglibose 10 mg/0...
March 1, 2018: Journal of Diabetes
Kornél Király, Márk Kozsurek, Erika Lukácsi, Benjamin Barta, Alán Alpár, Tamás Balázsa, Csaba Fekete, Judit Szabon, Zsuzsanna Helyes, Kata Bölcskei, Valéria Tékus, Zsuzsanna E Tóth, Károly Pap, Gábor Gerber, Zita Puskár
Altered pain sensations such as hyperalgesia and allodynia are characteristic features of various pain states, and remain difficult to treat. We have shown previously that spinal application of dipeptidyl peptidase 4 (DPP4) inhibitors induces strong antihyperalgesic effect during inflammatory pain. In this study we observed low level of DPP4 mRNA in the rat spinal dorsal horn in physiological conditions, which did not change significantly either in carrageenan-induced inflammatory or partial nerve ligation-generated neuropathic states...
February 22, 2018: Scientific Reports
André Jacques Scheen
Dipeptidyl peptidase-4 inhibitors (DPP-4is) are generally considered as glucose-lowering agents with a safe profile in type 2 diabetes. Areas covered: An updated review of recent safety data from randomised controlled trials, observational studies, meta-analyses, pharmacovigilance reports regarding alogliptin, linagliptin, saxagliptin, sitagliptin, and vildagliptin, with a special focus on risks of hypoglycemia, pancreatitis and pancreatic cancer, major cardiovascular events, hospitalisation for heart failure and other new safety issues, such as bone fractures and arthralgia...
April 2018: Expert Opinion on Drug Safety
Jun-Sing Wang, Yi-Jen Hung, Yung-Chuan Lu, Cheng-Lin Tsai, Wei-Shiung Yang, Ting-I Lee, Ya-Chun Hsiao, Wayne Huey-Herng Sheu
AIM: We aimed to investigate the association of difference between observed and predicted glycated hemoglobin (dopHbA1c) and HbA1c reduction after vildagliptin-based oral therapy in patients with type 2 diabetes (T2D). METHODS: This was a prospective observational study. Adults ≥20 years old with T2D and HbA1c ≧7% treated with oral anti-diabetic drugs (OADs) were eligible if their OADs were shifted to vildagliptin-based dual oral therapy. Fasting plasma glucose (FPG) and HbA1c were recorded at baseline, week 12, and week 24...
February 11, 2018: Diabetes Research and Clinical Practice
Outi Varpuluoma, Anna-Kaisa Försti, Jari Jokelainen, Miia Turpeinen, Markku Timonen, Laura Huilaja, Kaisa Tasanen
No abstract text is available yet for this article.
February 7, 2018: Journal of Investigative Dermatology
Chen-Jie Qin, Ling-Hao Zhao, Xu Zhou, Hui-Lu Zhang, Wen Wen, Liang Tang, Min Zeng, Ming-Da Wang, Gong-Bo Fu, Shuai Huang, Wei-Jian Huang, Yuan Yang, Zhi-Jun Bao, Wei-Ping Zhou, Hong-Yang Wang, He-Xin Yan
Obesity is a major risk factor for hepatocellular carcinoma (HCC) and is typically accompanied by higher levels of serum dipeptidyl peptidase 4 (DPP4). However, the role of DPP4 in obesity-promoted HCC is unclear. Here, we found that consumption of a high-fat diet (HFD) promoted HCC cell proliferation and metastasis and led to poor survival in a carcinogen-induced model of HCC in rats. Notably, genetic ablation of DPP4 or treatment with a DPP4 inhibitor (vildagliptin) prevented HFD-induced HCC. Moreover, HFD-induced DPP4 activity facilitated angiogenesis and cancer cell metastasis in vitro and in vivo, and vildagliptin prevented tumor progression by mediating the pro-angiogenic role of chemokine ligand 2 (CCL2)...
April 28, 2018: Cancer Letters
Sandra Hummel, Andreas Beyerlein, Markus Pfirrmann, Anna Hofelich, Daniela Much, Susanne Hivner, Melanie Bunk, Melanie Herbst, Claudia Peplow, Markus Walter, Denise Kohn, Nadine Hummel, Jürgen Kratzsch, Michael Hummel, Martin Füchtenbusch, Joerg Hasford, Anette-G Ziegler
OBJECTIVE: Women with insulin-requiring gestational diabetes mellitus (GDM) are at high risk of developing diabetes within a few years postpartum. We implemented this phase II study to test the hypothesis that vildagliptin, a dipeptidyl peptidase-4 inhibitor, is superior to placebo in terms of reducing the risk of postpartum diabetes. METHODS: Women with insulin-requiring GDM were randomized to either placebo or 50 mg vildagliptin twice daily for 24 months followed by a 12-month observation period (EudraCT: 2007-000634-39)...
January 3, 2018: Molecular Metabolism
Risa Takayanagi, Takumi Uchida, Koji Kimura, Yasuhiko Yamada
Glucagon-like peptide-1 (GLP-1) receptor agonists (liraglutide, exenatide, lixisenatide) have recently been used as anti-diabetes drugs. We examined relationships of the binding occupancy of GLP-1 receptors (Φ) and their clinical efficacy after administration of GLP-1 receptor agonists. Next, by focusing on changes of GLP-1 concentration after administration of dipeptidyl peptidase-4 (DPP-4) inhibitors (vildagliptin, alogliptin, sitagliptin, linagliptin), we analyzed the relationship between Φ and clinical efficacy...
2018: Biological & Pharmaceutical Bulletin
Alberto Palazzuoli, Elena Ceccarelli, Gaetano Ruocco, Ranuccio Nuti
Heart failure (HF) is a common complication in patients with type 2 diabetes and it is closely associated with high morbidity and mortality rate. The incidence of cardiovascular events in patients with diabetes is related to high levels of glycemia, expressed by increase of HbA1c levels. However, there is little evidence to indicate that glycemic control can reduce the incidence of HF events in this population. Recently, several new antidiabetic drugs have been proposed although the exact clinical impact on heart failure occurrence and deterioration is under debate...
January 23, 2018: Heart Failure Reviews
Koichi Kanozawa, Yuichi Noguchi, Souichi Sugahara, Satoko Nakamura, Hirohisa Yamamoto, Keiko Kaneko, Rika Kono, Saeko Sato, Tomonari Ogawa, Hajime Hasegawa, Shigehiro Katayama
BACKGROUND: We conducted the multicenter, prospective, open-label study in type 2 diabetic (T2DM) patients with renal dysfunction, to clarify the efficacy and the safety in relation to renal function and glycemic control, and the economic effect when other dipeptidyl peptidase-4 (DPP-4) inhibitors were switched to a small dose of sitagliptin depending on their renal function. METHODS: Vildagliptin, alogliptin, or linagliptin received for more than 2 months were changed to sitagliptin at 25 or 12...
December 23, 2017: Clinical and Experimental Nephrology
Michael Benzaquen, Luca Borradori, Philippe Berbis, Simone Cazzaniga, René Valero, Marie-Aleth Richard, Laurence Feldmeyer
BACKGROUND: Case reports have suggested an association between dipeptidyl peptidase-IV inhibitors (DPP4i) and development of bullous pemphigoid (BP). OBJECTIVE: To evaluate the association between DPP4i treatment and development of BP. METHODS: We conducted a retrospective 1:2 case-control study, comparing diabetic BP cases to age and sex-matched diabetic controls, issued from Swiss (Bern) and French (Marseille) dermatological departments, from January 1st 2014 to July 31st 2016...
December 20, 2017: Journal of the American Academy of Dermatology
Wen-Qin Guo, Lang Li, Qiang Su, Wei-Ran Dai, Zi-Liang Ye
BACKGROUND: Previous meta-analyses evaluating the effectiveness of individual dipeptidyl peptidase-4 (DPP-4) inhibitors on the risk of heart failure (HF) were limited because of the small number of trials with direct comparisons between two treatments. METHODS: A Bayesian network meta-analysis was performed to investigate the relationship between DPP-4 inhibitors and the risk of HF in patients with type-2 diabetes mellitus. The primary outcome was the occurrence of HF or hospital admission for HF...
December 2017: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
Thinzar Min, Gareth I Davies, Sam Rice, James Chess, Jeffrey W Stephens
AIMS: Chronic kidney disease (CKD) is common in type 2 diabetes and limits the treatment choices for glycaemic control. Our aim was to examine real-world prescribing for managing hyperglycaemia in the presence of CKD. METHODS: The SAIL (Secure Anonymised Information Linkage) databank was used to examine prescribing during the period from the 1st of January to 30th December 2014. CKD was defined as:- none or mild CKD, eGFR ≥60mL/min/1.73m2; moderate CKD eGFR <60mL/min/1...
November 23, 2017: Diabetes & Metabolic Syndrome
Jun Yang, Chao Huang, Shanshan Wu, Yang Xu, Ting Cai, Sanbao Chai, Zhirong Yang, Feng Sun, Siyan Zhan
AIM: The association between dipeptidyl peptidase-4 inhibitors (DPP-4is), a class of anti-diabetes, and bone fracture in patients with type 2 diabetes mellitus (T2DM) is unknown. This meta-analysis aimed to systematically evaluate the effects of DPP-4is on bone fracture in T2DM patients. METHODS: We searched the Cochrane Library, Embase, Medline and from inception through April 28th, 2016 to identify randomized controlled trials (RCTs) that compared DPP-4is with placebo or other anti-diabetes in T2DM patients...
2017: PloS One
Ana Patrícia Marques, Janete Cunha-Santos, Helena Leal, Lígia Sousa-Ferreira, Luís Pereira de Almeida, Cláudia Cavadas, Joana Rosmaninho-Salgado
BACKGROUND: During the development of obesity the expansion of white adipose tissue (WAT) leads to a dysregulation and an excessive remodeling of extracellular matrix (ECM), leading to fibrosis formation. These ECM changes have high impact on WAT physiology and may change obesity progression. Blocking WAT fibrosis may have beneficial effects on the efficacy of diet regimen or therapeutical approaches in obesity. Since dipeptidyl peptidase IV (DPP-IV) inhibitors prevent fibrosis in tissues, such as heart, liver and kidney, the objective of this study was to assess whether vildagliptin, a DPP-IV inhibitor, prevents fibrosis in WAT in a mouse model of obesity, and to investigate the mechanisms underlying this effect...
March 2018: Biochimica et Biophysica Acta
Mirza Muhammad Faran Ashraf Baig, Sara Khan, Muhammad Ahsan Naeem, Ghulam Jilany Khan, Muhammad Tayyab Ansari
Diabetes mellitus type 2 is a multidimensional disease associated with poor glycemic control through compromised sensitivity of pancreatic islet α and β cells against glucose and dwindled secretion of insulin which is linked with the quantity of incretin hormones that are abridged by dipeptidyl peptidase-4 (DPP-4) in diseased condition. Vildagliptin (VG) inhibits DPP-4 therefore regulates the incretins that conversely maintains glycemic control. The safe reach and absorption of VG from intestine was dubious...
November 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Pongpan Tanajak, Piangkwan Sa-Nguanmoo, Sivaporn Sivasinprasan, Savitree Thummasorn, Natthaphat Siri-Angkul, Siriporn Chattipakorn, Nipon Chattipakorn
Sodium-glucose cotransporter 2 inhibitor (SGLT2-i) effects on cardiac ischemia/reperfusion (I/R) injury are unclear. Unlike SGLT2-i, dipeptidyl peptidase 4 inhibitors (DPP4-i) have shown effective cardioprotection in cardiac I/R injury. We aimed to investigate whether SGLT2-i reduces myocardial dysfunction and myocardial injury to a greater extent than DPP4-i in obese-insulin resistant rats with/without cardiac I/R injury. The high fat (HF) diet induced obese-insulin resistant rats were divided into 4 groups and received the following treatments for 28 days: vehicle (HFV); vildagliptin at a dosage of 3 mg/kg/day (HFVil); dapagliflozin at a dosage of 1 mg/kg/day (HFDa); and combination drugs (HFDaVil)...
November 15, 2017: Journal of Endocrinology
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