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https://www.readbyqxmd.com/read/28087908/-berberine-regulates-glycemia-via-local-inhibition-of-intestinal-dipeptidyl-peptidase-%C3%A2
#1
Jiesheng Wang, Guanhai Dai, Weijia Li
Objective: To investigate the effect of berberine on glycemia regulation in rats with diabetes and the related mechanisms. Methods: Diabetic-like rat model was successfully induced by intraperitoneal injection of streptozotocin in 50 out of 60 male SD rats, which were then randomly divided into 5 groups with 10 rats in each:control group (received vehicle only), positive drug control group (sitagliptin 10 mg·kg(-1)·d(-1)), low-dose berberine group (30 mg·kg(-1)·d(-1)), moderate-dose berberine group (60 mg·kg(-1)·d(-1)), and high-dose berberine group (120 mg·kg(-1)·d(-1))...
May 25, 2016: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28086872/dapagliflozin-decreases-small-dense-low-density-lipoprotein-cholesterol-and-increases-high-density-lipoprotein-2-cholesterol-in-patients-with-type-2-diabetes-comparison-with-sitagliptin
#2
Toshiyuki Hayashi, Tomoyasu Fukui, Noriko Nakanishi, Saki Yamamoto, Masako Tomoyasu, Anna Osamura, Makoto Ohara, Takeshi Yamamoto, Yasuki Ito, Tsutomu Hirano
BACKGROUND: The sodium-glucose co-transporter-2 (SGLT-2) inhibitors have been reported to increase both low-density lipoprotein (LDL) and high-density lipoprotein (HDL)-cholesterol (C). This study aimed to determine how SGLT-2 inhibitors affect LDL and HDL-C subspecies. METHODS: This single center, open-label, randomized, prospective study included 80 patients with type 2 diabetes taking prescribed oral hypoglycemic agents. Patients were allocated to receive dapagliflozin (n = 40) or sitagliptin (n = 40) as add-on treatment...
January 13, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28078647/sitagliptin-a-review-in-type-2-diabetes
#3
Lesley J Scott
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia(®); Glactiv(®); Tesavel(®); Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD)...
January 11, 2017: Drugs
https://www.readbyqxmd.com/read/28067320/relationship-between-frequency-of-hypoglycemic-episodes-and-changes-in-carotid-atherosclerosis-in-insulin-treated-patients-with-type-2-diabetes-mellitus
#4
Tomoya Mita, Naoto Katakami, Toshihiko Shiraiwa, Hidenori Yoshii, Nobuichi Kuribayashi, Takeshi Osonoi, Hideaki Kaneto, Keisuke Kosugi, Yutaka Umayahara, Masahiko Gosho, Iichiro Shimomura, Hirotaka Watada
The effect of hypoglycemia on the progression of atherosclerosis in patients with type 2 diabetes mellitus (T2DM) remains largely unknown. This is a post hoc analysis of a randomized trial to investigate the relationship between hypoglycemic episodes and changes in carotid intima-media thickness (IMT). Among 274 study subjects, 104 patients experienced hypoglycemic episodes. Increases in the mean IMT and left maximum IMT of the common carotid arteries (CCA) were significantly greater in patients with hypoglycemia compared to those without hypoglycemia...
January 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28065853/sitagliptin-inhibit-human-lymphocytes-proliferation-and-th1-th17-differentiation-in-vitro
#5
Marcelo Maia Pinheiro, Caroline Lais Stoppa, Claudete Justina Valduga, Cristina Eunice Okuyama, Renata Gorjão, Regina Mara Silva Pereira, Susana Nogueira Diniz
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of anti-diabetic agents that are widely used in clinical practice to improve glycemic control in patients with type 2 diabetes. DPP-4 is also known as lymphocyte cell surface protein, CD26, and plays an important role in T-cell immunity. Recent studies suggest that DPP-4 inhibitors improve beta-cell function and attenuate autoimmunity in type 1 diabetic mouse models. To investigate the direct effect of DPP4 in immune response, human peripheral blood mononuclear cells (PBMC) from healthy volunteers were obtained by Ficoll gradient and cultivated in the absence (control) or presence of phytohemagglutinin (PHA), or stimulated with PHA and treated with sitagliptin...
January 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28060721/dppiv-promotes-endometrial-carcinoma-cell-proliferation-invasion-and-tumorigenesis
#6
Xiaoqing Yang, Xinhua Zhang, Rongrong Wu, Qicheng Huang, Yao Jiang, Jianbing Qin, Feng Yao, Guohua Jin, Yuquan Zhang
Dipeptidyl peptidase IV (DPPIV), also known as CD26, is a 110-kDa cell surface glycoprotein expressed in various tissues. DPPIV reportedly plays a direct role in the progression of several human malignancies. DPPIV specific inhibitors are employed as antidiabetics and could potentially be repurposed to enhance anti-tumor immunotherapies. In the present study, we investigated the correlation between DPPIV expression and tumor progression in endometrial carcinoma (EC). DPPIV overexpression altered cell morphology and stimulated cell proliferation, invasion and tumorigenesis in vitro and in vivo...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28058753/effect-of-gemigliptin-on-glycemic-variability-in-patients-with-type-2-diabetes
#7
Se E Park, Byung W Lee, Jae H Kim, Woo J Lee, Jae H Cho, Chang H Jung, Seung H Lee, Sunghwan Suh, Gwong C Hur, Sung H Kim, Young H Jang, Cheol Y Park
The aim of this study was to evaluate the effect of gemigliptin vs sitagliptin or glimepiride as initial combination therapy with metformin on glycemic variability and to assess the correlation between glycemic variability reduction and the dipeptidyl peptidase-4 (DPP-4) inhibition in patients with type 2 diabetes. This multicenter, randomized, active-controlled, open-label exploratory study included 69 patients with HbA1c >7.5%. Subjects were randomized to receive gemigliptin 50 mg (n = 24), sitagliptin 100 mg (n = 23), or glimepiride 2 mg (n = 22) for 12 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28058750/efficacy-and-safety-of-adding-evogliptin-versus-sitagliptin-in-metformin-treated-patients-with-type-2-diabetes-a-24-week-randomised-controlled-trial-with-open-label-extension
#8
Sang-Mo Hong, Cheol-Young Park, Dong-Min Hwang, Kyung Ah Han, Chang Beom Lee, Choon Hee Chung, Kun-Ho Yoon, Ji-Oh Mok, Kyong Soo Park, Sung-Woo Park
AIMS: This trial consisted of a 24-week multicenter, randomised, double-blind, double-dummy, active-controlled study and a 52-week open label extension study to assess the efficacy and safety of evogliptin, a novel dipeptidyl peptidase-4 inhibitor, compared to sitagliptin in patients with type 2 diabetes who have inadequate glycaemic control with metformin alone. MATERIALS AND METHODS: Adult type 2 diabetes mellitus patients (N = 222) with HbA1c 6.5-11% on stable metformin doses (≥1000 mg/day) were randomised 1:1 to add-on 5 mg evogliptin (N = 112) or 100 mg sitagliptin (N = 110) once daily for 24 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28057693/assessing-the-safety-of-sitagliptin-in-older-participants-in-the-trial-evaluating-cardiovascular-outcomes-with-sitagliptin-tecos
#9
M Angelyn Bethel, Samuel S Engel, Jennifer B Green, Zhen Huang, Robert G Josse, Keith D Kaufman, Eberhard Standl, Shailaja Suryawanshi, Frans Van de Werf, Darren K McGuire, Eric D Peterson, Rury R Holman
OBJECTIVE: Limited data exist regarding safety and efficacy of antihyperglycemic drugs in older patients with type 2 diabetes. The Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS) was a randomized, double-blind, placebo-controlled trial assessing the impact of sitagliptin on a primary composite outcome of cardiovascular death, nonfatal stroke, nonfatal myocardial infarction, or unstable angina hospitalizations in patients with type 2 diabetes (HbA1c ≥6.5% [48 mmol/mol] and ≤8...
January 5, 2017: Diabetes Care
https://www.readbyqxmd.com/read/28056430/the-effects-of-sitagliptin-a-dpp-4-inhibitor-on-cognitive-functions-in-elderly-diabetic-patients-with-or-without-alzheimer-s-disease
#10
Ahmet Turan Isik, Pinar Soysal, Adnan Yay, Cansu Usarel
AIMS: The present study aimed to evaluate effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor (DPP-4I), on cognitive functions in elderly diabetic patients with and without cognitive impairment. METHODS: 253 elderly patients with type 2DM, were enrolled in this prospective and observational study. After comprehensive geriatric assessment, the patients were divided into either sitagliptin or non-sitagliptin group. RESULTS: A total of 205 patients who completed the study (52 with Alzheimer's Disease (AD)) were re-evaluated 6months later...
December 21, 2016: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28053048/identifying-new-antiepileptic-drugs-through-genomics-based-drug-repurposing
#11
Nasir Mirza, Greame J Sills, Munir Pirmohamed, Anthony G Marson
Currently available antiepileptic drugs (AEDs) fail to control seizures in 30% of patients. Genomics-based drug repurposing (GBR) offers the potential of savings in the time and cost of developing new AEDs. In the current study, we used published data and software to identify the transcriptomic signature of chornic temporal lobe epilepsy and the drugs that reverse it. After filtering out compounds based on exclusion criteria, such as toxicity, 36 drugs were retained. 11 of the 36 drugs identified (>30%) have published evidence of antiepileptic efficacy (for example, curcumin) or antiepileptogenic affect (for example, atorvastatin) in recognised rodent models or patients...
January 4, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28039605/pharmacokinetic-characteristics-and-clinical-efficacy-of-an-sglt2-inhibitor-plus-dpp-4-inhibitor-combination-therapy-in-type-2-diabetes
#12
REVIEW
André J Scheen
Type 2 diabetes (T2D) generally requires a combination of several pharmacological approaches to control hyperglycaemia. Combining a sodium-glucose cotransporter type 2 inhibitor (SGLT2I, also known as gliflozin) and a dipeptidyl peptidase-4 inhibitor (DPP-4I, also known as gliptin) appears to be an attractive strategy because of complementary modes of action. This narrative review analyzes the pharmacokinetics and clinical efficacy of different combined therapies with an SGLT2I (canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, ipragliflozin, luseogliflozin, tofogliflozin) and DPP-4I (linagliptin, saxagliptin, sitagliptin, teneligliptin)...
December 30, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28035868/a-randomized-clinical-trial-of-the-safety-and-efficacy-of-sitagliptin-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-by-acarbose-alone
#13
Weiqing Wang, Guang Ning, Jianhua Ma, Xiaomin Liu, Shaoxiong Zheng, Fan Wu, Lei Xu, Edward A O'Neill, Kenji P Fujita, Samuel S Engel, Keith D Kaufman, R Ravi Shankar
OBJECTIVE: To evaluate the safety and efficacy of sitagliptin when added to the treatment of patients with type 2 diabetes mellitus (T2DM) and inadequate glycemic control on acarbose monotherapy. RESEARCH DESIGN AND METHODS: This was a multicenter, randomized, placebo-controlled, double-blind clinical trial. Patients (N = 381) with T2DM and inadequate glycemic control (glycated hemoglobin [HbA1c] ≥7.0% and ≤10.0%) on acarbose monotherapy (at least 50 mg three times daily) were randomized in a 1:1 ratio to receive the addition of sitagliptin 100 mg or matching placebo once daily for 24 weeks...
December 30, 2016: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28029729/combination-treatment-of-dipeptidyl-peptidase-iv-inhibitor-sitagliptin-and-angiotensin-ii-type-1-receptor-blocker-losartan-suppresses-progression-in-a-nondiabetic-rat-model-of-steatohepatitis
#14
Yasushi Okura, Tadashi Namisaki, Kei Moriya, Mitsuteru Kitade, Kosuke Takeda, Kosuke Kaji, Ryuichi Noguchi, Norihisa Nishimura, Kenichiro Seki, Hideto Kawaratani, Hiroaki Takaya, Shinya Sato, Yasuhiko Sawada, Naotaka Shimozato, Masanori Furukawa, Keisuke Nakanishi, Saikawa Soichiro, Takuya Kubo, Kiyoshi Asada, Hitoshi Yoshiji
AIM: Dipeptidyl peptidase-4 (DPP4) inhibitors (DPP4-I) are oral glucose-lowering drugs for type 2 diabetes mellitus. Previously, we demonstrated that DPP4-I (sitagliptin) exerted suppressive effects on experimental liver fibrosis in rats. Blockade of the renin-angiotensin system by angiotensin-II type 1 receptor blocker (ARB: losartan), commonly used in the management of hypertension, has been shown to significantly alleviate hepatic fibrogenesis and carcinogenesis. We aimed to elucidate the effects and possible mechanisms of a sitagliptin + losartan combination on the progression of nondiabetic nonalcoholic steatohepatitis (NASH) in a rat model...
December 28, 2016: Hepatology Research: the Official Journal of the Japan Society of Hepatology
https://www.readbyqxmd.com/read/28000562/synchronized-fast-spe-and-uflc-methods-for-the-analyses-of-eight-antidiabetic-drugs-in-human-plasma
#15
Imran Ali, Kamlesh Dutta, A K Jain
The number of the diabetic patients is increasing rapidly globally. The treatment of these patients is a complex phenomenon due to the use of the different drugs. The present article reports a synchronized fast SPE-UFLC separation of eight antidiabetic drugs in human plasma. The separated drugs include metformin HCl, vildagliptin, gliclazide, linagliptin, sitagliptin, pioglitazone, glimepiride and repaglinide. The column used was Sunshell C18 (150 x 4.6 mm, 2.6 µm) with mobile phase of acetate buffer (0.05% TEA in 0...
December 20, 2016: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/27998910/pancreatic-effects-of-liraglutide-or-sitagliptin-in-overweight-patients-with-type-2-diabetes-a-12-week-randomized-placebo-controlled-trial
#16
Mark M Smits, Lennart Tonneijck, Marcel H A Muskiet, Mark H H Kramer, Indra C Pieters-van den Bos, Karuna E W Vendrik, Trynke Hoekstra, Marco J Bruno, Michaela Diamant, Daniël H van Raalte, Djuna L Cahen
OBJECTIVE: To assess the mechanistic effects of the glucagon-like peptide 1 (GLP-1) receptor agonist liraglutide and the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin on (exocrine) pancreatic physiology and morphology. RESEARCH DESIGN AND METHODS: For this randomized, double-blind, parallel-group trial, 55 patients with type 2 diabetes treated with metformin and/or sulfonylurea agents were included. Participants received liraglutide 1.8 mg (n = 19), sitagliptin 100 mg (n = 19), or matching placebos (n = 17) once daily for 12 weeks...
December 20, 2016: Diabetes Care
https://www.readbyqxmd.com/read/27995594/liraglutide-versus-sglt-2-inhibitors-in-people-with-type-2-diabetes-a-network-meta-analysis
#17
Maria Lorenzi, Uffe Jon Ploug, Jakob Langer, Rasmus Skovgaard, Michael Zoratti, Jeroen Jansen
INTRODUCTION: For people with type 2 diabetes (T2DM) inadequately controlled with oral antidiabetic drugs (OADs), evidence from both randomized controlled trials (RCTs) and real-world studies has demonstrated that treatment intensification with liraglutide offers effective glycemic control, weight reduction, and a lower risk of hypoglycemia compared to treatment intensification with insulin or additional OADs. Sodium glucose cotransporter 2 (SGLT-2) inhibitors are a new class of OADs that have also been shown to be effective in T2DM patients inadequately controlled with OADs...
December 19, 2016: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/27990119/oral-administration-of-sitagliptin-activates-creb-and-is-neuroprotective-in-murine-model-of-brain-trauma
#18
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/27986440/sitagliptin-may-reduce-breast-cancer-risk-in-women-with-type-2-diabetes
#19
Chin-Hsiao Tseng
BACKGROUND: Whether sitagliptin may affect breast cancer risk remains to be answered. This study evaluated such an association in Taiwanese female patients with type 2 diabetes. METHODS: A retrospective cohort of female patients with newly diagnosed type 2 diabetes at an age ≥ 25 years between 1999 and 2010 was recruited from the National Health Insurance database. A total of 32,457 ever-users and 396,021 never-users of sitagliptin were followed until December 31, 2011...
November 23, 2016: Clinical Breast Cancer
https://www.readbyqxmd.com/read/27979881/an-update-on-the-gliptins
#20
(no author information available yet)
Progressive impairment of insulin secretion in people with type 2 diabetes leads to blood glucose concentrations worsening over time, often resulting in escalation of blood glucose lowering therapy.(1) In 2015/2016, more money was spent on dipeptidyl peptidase-4 (DPP-4) inhibitors ('gliptins') than on any other class of antidiabetic drug except for insulins.(2) In 2008, we reviewed sitagliptin and vildagliptin.(3) Here, we briefly review three other DPP-4 inhibitors, saxagliptin (Onglyza-AstraZeneca), linagliptin (Trajenta-Boehringer Ingelheim) and ▼alogliptin (Vipidia-Takeda), and consider data from recent cardiovascular outcomes studies...
December 2016: Drug and Therapeutics Bulletin
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