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https://www.readbyqxmd.com/read/28810651/kanglaite-inhibits-the-expression-of-drug-resistance-genes-through-suppressing-pvt1-in-cisplatin-resistant-gastric-cancer-cells
#1
Xian-Wen Zhang, Liang Liu, Xi-Zhi Zhang, Ping Bo
Kanglaite (KLT) was shown to alleviate the development of multidrug resistance (MDR) clinically. The purpose of this study is to examine the mechanism of KLT for chemotherapy resistance in gastric cancer cells involving the regulation of MDR-related proteins. The cisplatin-resistant BGC823/DPP and SGC7901/DDP cells were treated with 1, 2.5 and 5 µl/ml of KLT for 24, 36 and 48 h. Cell Counting Kit-8 (CCK-8) assay and flow cytometry were performed to detect the cell viability and cell apoptosis, respectively...
August 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28807765/sglt2-inhibitor-and-dpp-4-inhibitor-improve-brain-function-via-attenuating-mitochondrial-dysfunction-insulin-resistance-inflammation-and-apoptosis-in-hfd-induced-obese-rats
#2
Piangkwan Sa-Nguanmoo, Pongpan Tanajak, Sasiwan Kerdphoo, Thidarat Jaiwongkam, Wasana Pratchayasakul, Nipon Chattipakorn, Siriporn C Chattipakorn
Dipeptidyl peptidase-4 inhibitor (vildagliptin) has been shown to exert beneficial effects on insulin sensitivity and neuroprotection in obese-insulin resistance. Recent studies demonstrated the neuroprotection of the sodium-glucose co-transporter 2 inhibitor (dapagliflozin) in diabetes. However, the comparative effects of both drugs and a combination of two drugs on metabolic dysfunction and brain dysfunction impaired by the obese-insulin resistance have never been investigated. Forty male Wistar rats were divided into two groups, and received either a normal-diet (ND, n=8) or a high-fat diet (HFD, n=32) for 16weeks...
August 11, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28807739/community-based-participatory-research-to-design-a-faith-enhanced-diabetes-prevention-program-the-better-me-within-randomized-trial
#3
Heather Kitzman, Leilani Dodgen, Abdullah Mamun, J Lee Slater, George King, Donna Slater, Alene King, Surendra Mandapati, Mark DeHaven
Reducing obesity positively impacts diabetes and cardiovascular risk; however, evidence-based lifestyle programs, such as the diabetes prevention program (DPP), show reduced effectiveness in African American (AA) women. In addition to an attenuated response to lifestyle programs, AA women also demonstrate high rates of obesity, diabetes, and cardiovascular disease. To address these disparities, enhancements to evidence-based lifestyle programs for AA women need to be developed and evaluated with culturally relevant and rigorous study designs...
August 11, 2017: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/28807660/the-changing-cost-to-prevent-diabetes-a-retrospective-analysis-of-the-diabetes-prevention-program
#4
Nicholas W Carris, Feng Cheng, William N Kelly
OBJECTIVES: Diabetes prevention interventions are poorly implemented. While health care costs generally increase, 2 factors affect the relative cost of diabetes prevention interventions: the declining cost of metformin (even without insurance) and the new recommendation for vitamin B12 monitoring during metformin treatment. The study's objective was to update the relative health system cost estimate of metformin for diabetes prevention by incorporating the current health system cost of metformin and the cost of addressing potential metformin-associated vitamin B12 deficiency...
August 11, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28806472/effects-of-clarithromycin-on-the-pharmacokinetics-of-evogliptin-in-healthy-volunteers
#5
E S Oh, C Choi, C O Kim, K H Kim, Y N Kim, S J Kim, M S Park
WHAT IS KNOWN AND OBJECTIVE: Evogliptin (DA-1229), a novel dipeptidyl peptidase (DPP)-4 inhibitor with high potency and selectivity, was approved in Korea for the treatment of type 2 diabetes. Preclinical studies suggest that it is metabolized by cytochrome (CYP) P450 isozymes. Based on these findings, a clinical study was designed to investigate the pharmacokinetic (PK) interaction of evogliptin with a CYP inhibitor, clarithromycin. METHODS: An open-label, two-phase, crossover study was conducted with 12 healthy subjects...
August 14, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28802241/the-9-d-cidr-pg-protocol-ii-characterization-of-endocrine-parameters-ovarian-dynamics-and-pregnancy-rates-to-fixed-time-ai-following-use-of-long-term-cidr-based-estrus-synchronization-among-mature-beef-cows
#6
J M Thomas, J W C Locke, B E Bishop, J M Abel, M R Ellersieck, S E Poock, M F Smith, D J Patterson
An experiment was designed to evaluate endocrine parameters, ovarian dynamics, and pregnancy rates to fixed-time artificial insemination (FTAI) following the 9-d CIDR-PG protocol in comparison to the 14-d CIDR-PG protocol. While both are long-term protocols using CIDR treatment for presynchronization, the 9-d CIDR-PG protocol differs from the 14-d CIDR-PG protocol in that prostaglandin F2α (PG) is administered at CIDR insertion and removal to facilitate a decreased length of progestin treatment and potentially enhance response to the presynchronization treatment...
August 3, 2017: Theriogenology
https://www.readbyqxmd.com/read/28801559/differential-effects-of-linagliptin-on-the-function-of-human-islets-isolated-from-non-diabetic-and-diabetic-donors
#7
Yanqing Zhang, Meifen Wu, Wynn Htun, Emily W Dong, Franck Mauvais-Jarvis, Vivian A Fonseca, Hongju Wu
Linagliptin is a dipeptidyl Peptidase-4 (DPP-4) inhibitor that inhibits the degradation of glucagon-like peptide 1 (GLP-1), and has been approved for the treatment of type 2 diabetes (T2D) in clinic. Previous studies have shown linagliptin improves β cell function using animal models and isolated islets from normal subjects. Since β cell dysfunction occurs during diabetes development, it was not clear how human islets of T2D patients would respond to linagliptin treatment. Therefore, in this study we employed human islets isolated from donors with and without T2D and evaluated how they responded to linagliptin treatment...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28799229/sitagliptin-mediated-preservation-of-endothelial-progenitor-cell-function-via-augmenting-autophagy-enhances-ischaemic-angiogenesis-in-diabetes
#8
Xiaozhen Dai, Jun Zeng, Xiaoqing Yan, Qian Lin, Kai Wang, Jing Chen, Feixia Shen, Xuemei Gu, Yuehui Wang, Jun Chen, Kejian Pan, Lu Cai, Kupper A Wintergerst, Yi Tan
Recently, the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin, a major anti-hyperglycaemic agent, has received substantial attention as a therapeutic target for cardiovascular diseases via enhancing the number of circulating endothelial progenitor cells (EPCs). However, the direct effects of sitagliptin on EPC function remain elusive. In this study, we evaluated the proangiogenic effects of sitagliptin on a diabetic hind limb ischaemia (HLI) model in vivo and on EPC culture in vitro. Treatment of db/db mice with sitagliptin (Januvia) after HLI surgery efficiently enhanced ischaemic angiogenesis and blood perfusion, which was accompanied by significant increases in circulating EPC numbers...
August 10, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28796490/amorphous-ternary-charge-cascade-molecules-for-bulk-heterojunction-photovoltaics
#9
Xavier A Jeanbourquin, Aiman Rahmanudin, Xiaoyun Yu, Melissa Johnson, Néstor Guijarro, Liang Yao, Kevin Sivula
Ternary bulk heterojunctions with cascade-type energy-level configurations are of significant interest for further improving the power conversion efficiency (PCE) of organic solar cells. However, controlling the self-assembly in solution-processed ternary blends remains a key challenge. Herein, we leverage the ability to control the crystallinity of molecular semiconductors via a spiro linker to demonstrate a simple strategy suggested to drive the self-assembly of an ideal charge-cascade morphology. Spirobifluorene (SF) derivatives with optimized energy levels from diketopyrrolopyrrole (DPP) or perylenediimide (PDI) components, coded as SF-(DPP)4 and SF-(PDI)4, are synthesized and investigated for application as ternary components in the host blend of poly(3-hexylthiophene-2,5-diyl):[6,6]phenyl-C61-butyric acid methyl ester (P3HT:PCBM)...
August 10, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28794822/overview-of-glucagon-like-peptide-1-receptor-agonists-for-the-treatment-of-patients-with-type-2-diabetes
#10
Kelvin Lingjet Tran, Young In Park, Shalin Pandya, Navin John Muliyil, Brandon David Jensen, Kovin Huynh, Quang T Nguyen
BACKGROUND: It is estimated that 29.1 million people or 9.3% of the US population have diabetes, which contributes to considerable medical and financial burden. Type 2 diabetes mellitus is characterized by insulin resistance and insulin secretion impairment leading to hyperglycemia. The presence of insulin resistance is strongly correlated with obesity. OBJECTIVE: This article reviews the available glucagon-like peptide-1 (GLP-1) receptor agonists and their role in the management of patients with diabetes, to help guide the selection of the most suitable agent for the individualized treatment of patients with type 2 diabetes...
June 2017: American Health & Drug Benefits
https://www.readbyqxmd.com/read/28790917/effect-of-dipeptidyl-peptidase-4-inhibitors-on-bone-metabolism-and-the-possible-underlying-mechanisms
#11
REVIEW
Yinqiu Yang, Chenhe Zhao, Jing Liang, Mingxiang Yu, Xinhua Qu
Diabetes mellitus has been demonstrated to be closely associated with osteoporosis. Accordingly, hypoglycemic therapy is considered effective in treating metabolic bone disease. Recently, the effects of dipeptidyl peptidase-4 (DPP-4) inhibitors, a new type of antidiabetic drug, on bone metabolism have been widely studied. This review mainly describes the effects of DPP-4 inhibitors on bone metabolism, including their effects on bone mineral density, bone quality, and fracture risk. In addition, the potential underlying mechanisms are discussed...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28790395/knockdown-of-hif-1%C3%AE-by-sirna-expressing-plasmid-delivered-by-attenuated-salmonella-enhances-the-antitumor-effects-of-cisplatin-on-prostate-cancer
#12
Junlian Gu, Yang Li, Jun Zeng, Bo Wang, Kun Ji, Yufeng Tang, Qing Sun
Resistance to cisplatin (DDP) and dose-related toxicity remain two important obstacles in the treatment of prostate cancer (PCa) patients with DDP-based chemotherapy. We have investigated whether the knockdown of hypoxia-inducible factor-1 alpha (HIF-1α) by siRNA could enhance the antitumor activity of DDP, and aimed to determine the underlying mechanisms. Intravenous injection of attenuated Salmonella carrying a HIF-1α siRNA-expressing plasmid was used to knockdown HIF-1α in a PC-3 xenograft model. The in vitro and in vivo effects of HIF-1α siRNA treatment and/or DPP on PCa cell proliferation, apoptosis, glycolysis, and production of reactive oxygen species (ROS) were assessed by examining molecular markers specific to each process...
August 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28780482/profiling-inflammatory-biomarkers-in-cervico-vaginal-mucus-cvm-postpartum-potential-early-indicators-of-bovine-clinical-endometritis
#13
Mounir Adnane, Aspinas Chapwanya, Rachid Kaidi, Kieran G Meade, Cliona O'Farrelly
Endometritis significantly impacts fertility and milk yield, thus reducing profitability of the dairy production. In cows that develop endometritis, normal postpartum endometrial inflammation is dysregulated. Here, we propose that endometrial inflammation is reflected in cervico-vaginal mucus (CVM) which could therefore be used as a prognostic tool. CVM was collected from 20 dairy cows (10 with clinical endometritis and 10 healthy) 7 and 21 days postpartum (DPP). Polymorphonuclear (PMN), mononuclear leukocyte and epithelial cells were counted, total protein levels were estimated and levels of IL-1β, IL-6, IL-8, serum amyloid A (SAA), haptoglobin (Hp) and C5b were analyzed by ELISA in CVM...
July 29, 2017: Theriogenology
https://www.readbyqxmd.com/read/28777292/influence-of-a-virgin-olive-oil-versus-butter-plus-cholesterol-enriched-diet-on-testicular-enzymatic-activities-in-adult-male-rats
#14
Germán Domínguez-Vías, Ana Belén Segarra, Magdalena Martínez-Cañamero, Manuel Ramírez-Sánchez, Isabel Prieto
The aim of the present work was to improve our knowledge on the mechanisms underlying the beneficial or deleterious effects on testicular function of the so-called Mediterranean and Western diet by analyzing glutamyl aminopeptidase (GluAP), gamma glutamyl transpeptidase (GGT) and dipeptidyl peptidase IV (DPP IV) activities in testis, as enzymes involved in testicular function. Male Wistar rats (6 months old) were fed for 24 weeks with three different diets: standard (S), an S diet supplemented with virgin-olive-oil (20%) (VOO), or a S diet enriched with butter (20%) plus cholesterol (0...
August 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28776371/asymmetric-formal-synthesis-of-the-long-acting-dpp-4-inhibitor-omarigliptin
#15
Feng Peng, Yonggang Chen, Cheng-Yi Chen, Peter G Dormer, Amude Kassim, Mark McLaughlin, Robert A Reamer, Edward C Sherer, Zhiguo Jake Song, Lushi Tan, Matthew T Tudge, Baoqiang Wan, John Y L Chung
A highly efficient asymmetric synthesis of the key tetrahydropyranol intermediate of DPP-4 inhibitor omarigliptin (1) is described. The successful development of a protecting group- and precious metal-free synthesis was achieved via the discovery of a practical asymmetric Henry reaction and the application of a one-pot nitro-Michael-lactolization-dehydration through-process. Other features of the synthesis include a highly efficient MsCl-mediated dehydration and a crystallization-induced dynamic resolution for exceptional ee and dr upgrade...
August 4, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28773977/gold-nanoparticle-based-colorimetric-and-electrochemical-methods-for-dipeptidyl-peptidase-iv-activity-assay-and-inhibitor-screening
#16
Ning Xia, Xin Wang, Xiaojin Wang, Binbin Zhou
We presented the colorimetric and electrochemical methods for determination of the dipeptidyl peptidase-IV (DPP-IV) activity and screening of its inhibitor using gold nanoparticle (AuNP) as the probe. In the colorimetric assay, the substrate peptide with a sequence of Arg-Pro-Arg induced the aggregation and color change of AuNPs, whereas cleavage of the peptide by DPP-IV prevented the aggregation of AuNPs. Furthermore, the aggregation of AuNPs in the solution was easily initiated on a solid/liquid (electrode/electrolyte) surface, which induced a decrease in the electron-transfer resistance...
October 21, 2016: Materials
https://www.readbyqxmd.com/read/28771933/impact-of-clinical-evidence-communications-and-drug-regulation-changes-concerning-rosiglitazone-on-prescribing-patterns-of-antidiabetic-therapies
#17
Yoojin Noh, Dae Ryong Kang, Dae Jung Kim, Kwang Jae Lee, Sukhyang Lee, Sooyoung Shin
PURPOSE: Cardiovascular safety alerts about rosiglitazone resulted in regulatory actions in several countries in 2010, but the Food and Drug Administration eliminated access restrictions in 2013, reflecting new evidence concerning the drug safety. We investigated the effects of safety signals and regulation shifts concerning rosiglitazone on prescribing of antidiabetic drugs (ADs). METHODS: Patient data were extracted from the Korean health insurance claims database for 2007 to 2015...
August 3, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28771923/dapagliflozin-compared-to-dpp-4-inhibitors-is-associated-with-lower-risk-of-cardiovascular-events-and-all-cause-mortality-in-type-2-diabetes-patients-cvd-real-nordic-a-multinational-observational-study
#18
F Persson, T Nyström, M E Jørgensen, B Carstensen, H L Gulseth, M Thuresson, P Fenici, D Nathanson, J W Eriksson, A Norhammar, J Bodegard, K I Birkeland
AIMS: To compare the sodium glucose-cotransporter-2-inhibitor (SGLT-2i) dapagliflozin versus dipeptidyl peptidase-4 inhibitors (DPP-4i) regarding risk associations of MACE (nonfatal myocardial infarction, nonfatal stroke or cardiovascular [CV] mortality), hospital events for heart failure (HHF), atrial fibrillation, and severe hypoglycemia for type 2 diabetes (T2D) patients in a real-world setting. METHODS: All T2D patients dispensed with glucose lowering drugs (GLDs) during 2012-2015 were identified in nationwide registries in Denmark, Norway and Sweden...
August 3, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28771625/inhibition-of-dipeptidyl-peptidase-4-ameliorates-cardiac-ischemia-and-systolic-dysfunction-by-up-regulating-the-fgf-2-egr-1-pathway
#19
Masayoshi Suda, Ippei Shimizu, Yohko Yoshida, Yuka Hayashi, Ryutaro Ikegami, Goro Katsuumi, Takayuki Wakasugi, Yutaka Yoshida, Shujiro Okuda, Tomoyoshi Soga, Tohru Minamino
Dipeptidyl peptidase 4 inhibitors are used worldwide in the management of diabetes, but their role in the prevention or treatment of cardiovascular disorders has yet to be defined. We found that linagliptin, a DPP-4 inhibitor, suppressed capillary rarefaction in the hearts of mice with dietary obesity. Metabolomic analysis performed with capillary electrophoresis/mass spectrometry (LC-MS/MS) showed that linagliptin promoted favorable metabolic remodeling in cardiac tissue, which was characterized by high levels of citrulline and creatine...
2017: PloS One
https://www.readbyqxmd.com/read/28770322/metformin-for-diabetes-prevention-insights-gained-from-the-diabetes-prevention-program-diabetes-prevention-program-outcomes-study
#20
REVIEW
Vanita R Aroda, William C Knowler, Jill P Crandall, Leigh Perreault, Sharon L Edelstein, Susan L Jeffries, Mark E Molitch, Xavier Pi-Sunyer, Christine Darwin, Brandy M Heckman-Stoddard, Marinella Temprosa, Steven E Kahn, David M Nathan
The largest and longest clinical trial of metformin for the prevention of diabetes is the Diabetes Prevention Program/Diabetes Prevention Program Outcomes Study (DPP/DPPOS). In this review, we summarise data from the DPP/DPPOS, focusing on metformin for diabetes prevention, as well as its long-term glycaemic and cardiometabolic effects and safety in people at high-risk of developing diabetes. The DPP (1996-2001) was a RCT of 3234 adults who, at baseline, were at high-risk of developing diabetes. Participants were assigned to masked placebo (n = 1082) or metformin (n = 1073) 850 mg twice daily, or intensive lifestyle intervention (n = 1079)...
August 2, 2017: Diabetologia
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