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Jordan R Smith, Juwon Yim, Seth Rice, Kyle Stamper, Razie Kebriaei, Michael J Rybak
Background: Methicillin-resistant Staphylococcus aureus (MRSA) is a major pathogen responsible for healthcare-associated infections, and treatment options are limited. Tedizolid (TZD), is a novel, oxazolidinone antibiotic with activity against MRSA. Previously, daptomycin (DAP), has demonstrated synergy with other antibiotics against MRSA. We sought to determine the efficacy of the combination of TZD + DAP against MRSA in an in vitro model of simulated endocardial vegetations (SEVs). Methods: TZD simulations of 200 mg once daily and DAP simulations of 6-mg/kg and 10-mg/kg once daily were tested alone and in the combinations of TZD + DAP 6-mg/kg or DAP 10-mg/kg against two clinical strains of MRSA, 494 and 67...
March 12, 2018: Antimicrobial Agents and Chemotherapy
Jeong-Hwa Yoon, Se Hee Min, Chang Ho Ahn, Young Min Cho, Seokyung Hahn
We aimed to evaluate the comparative efficacy and safety of dipeptidyl peptidase-4 inhibitors (DPP4i), glucagon-like peptide-1 receptor agonists (GLP-1RA), sodium-glucose co-transporter 2 inhibitors (SGLT2i), or thiazolidinedione (TZD) as an adjunctive treatment in patients with poorly controlled type 2 diabetes mellitus (T2DM) on insulin therapy. We searched Medline, Embase, the Cochrane Library, and through April 2016. Bayesian network meta-analyses were performed with covariate adjustment...
March 6, 2018: Scientific Reports
Guendalina Olivero, Massimo Grilli, Matteo Vergassola, Tommaso Bonfiglio, Cristina Padolecchia, Beatrice Garrone, Francesco Paolo Di Giorgio, Stefania Tongiani, Cesare Usai, Mario Marchi, Anna Pittaluga
Presynaptic mGlu2/3 autoreceptors exist in rat spinal cord nerve terminals as suggested by the finding that LY379268 inhibited the 15 mM KCl-evoked release of [3 H]D-aspartate ([3 H]D-Asp) in a LY341495-sensitive manner. Spinal cord glutamatergic nerve terminals also possess presynaptic release-regulating 5-HT2A heteroreceptors. Actually, the 15 mM KCl-evoked [3 H]D-Asp exocytosis from spinal cord synaptosomes was reduced by the 5-HT2A agonist (±)DOI, an effect reversed by the 5-HT2A antagonists MDL11,939, MDL100907, ketanserin and trazodone (TZD)...
February 27, 2018: Neuropharmacology
Mengle Shao, Lavanya Vishvanath, Napoleon C Busbuso, Chelsea Hepler, Bo Shan, Ankit X Sharma, Shiuhwei Chen, Xinxin Yu, Yu A An, Yi Zhu, William L Holland, Rana K Gupta
Pathologic expansion of white adipose tissue (WAT) in obesity is characterized by adipocyte hypertrophy, inflammation, and fibrosis; however, factors triggering this maladaptive remodeling are largely unknown. Here, we test the hypothesis that the potential to recruit new adipocytes from Pdgfrβ+ preadipocytes determines visceral WAT health in obesity. We manipulate levels of Pparg, the master regulator of adipogenesis, in Pdgfrβ+ precursors of adult mice. Increasing the adipogenic capacity of Pdgfrβ+ precursors through Pparg overexpression results in healthy visceral WAT expansion in obesity and adiponectin-dependent improvements in glucose homeostasis...
March 1, 2018: Nature Communications
Qiong A Wang, Fang Zhang, Lei Jiang, Risheng Ye, Yu An, Mengle Shao, Caroline Tao, Rana K Gupta, Philipp E Scherer
Adipose tissue is a dynamic organ that makes critical contributions to whole body metabolic homeostasis. Although recent studies have revealed that different fat depots have distinct molecular signatures, metabolic functions and adipogenic mechanisms, PPARγ is still widely viewed as the master regulator of adipogenesis and critical for maintaining mature adipocyte function. Using an inducible, adipocyte-specific knockout system, we explored the role of PPARγ in mature adipocytes in vivo Short-term PPARγ deficiency in adipocytes reduces whole body insulin sensitivity, but adipocytes are viable both in vitro and in vivo However, after high fat diet exposure, even short-term PPARγ deficiency leads to rapid adipocyte death...
February 26, 2018: Molecular and Cellular Biology
Khanh-Van Tran, Timothy Fitzgibbons, So Yun Min, Tiffany DeSouza, Silvia Corvera
OBJECTIVE: Perivascular adipose tissue depots around the aorta are regionally distinct and have specific functional properties. Thoracic aorta perivascular adipose tissue (tPVAT) expresses higher levels of thermogenic genes and lower levels of inflammatory genes than abdominal aorta perivascular adipose tissue (aPVAT). It is not known whether this distinction is due to the in-vivo functional environment or to cell-autonomous traits that persist outside the in-vivo setting. In this study, we asked whether the progenitor cells in tPVAT and aPVAT have cell-autonomous traits that lead to formation of regionally distinct PVAT...
January 10, 2018: Molecular Metabolism
Abhiroop Chakravarty, Mohini Rastogi, Praveen Dhankhar, Kelly Bell
OBJECTIVE: To compare 1-year costs and benefits of dapagliflozin (DAPA), a sodium-glucose cotransporter-2 (SGLT-2) inhibitor, with those of other treatments for type 2 diabetes (T2D), such as glucagon-like peptide-1 receptor agonists (GLP-1RAs), sulfonylureas (SUs), thiazolidinediones (TZDs), and dipeptidyl peptidase-4 inhibitors (DPP-4i), all combined with metformin. METHODS: A short-term decision-analytic model with a 1-year time horizon was developed from a payer's perspective in the United States (US) setting...
January 29, 2018: Journal of Medical Economics
Maya Korem, Sarah Kagan, Itzhack Polacheck
Biofilm formation by microorganisms depends on their communication by quorum sensing, which is mediated by small diffusible signaling molecules that accumulate in the extracellular environment. During human infection, the pathogenic yeast Cryptococcus neoformans can form biofilm on medical devices, which protects the organism and increases its resistance to antifungal agents. The aim of this study was to test two novel heterocyclic compounds, S-8 (thiazolidinedione derivative, TZD) and NA-8 (succinimide derivative, SI), for their anti-biofilm activity against strains of Cryptococcus neoformans and Cryptococcus gattii...
July 20, 2017: Journal of Fungi (Basel, Switzerland)
Alan J Garber, Martin J Abrahamson, Joshua I Barzilay, Lawrence Blonde, Zachary T Bloomgarden, Michael A Bush, Samuel Dagogo-Jack, Ralph A DeFronzo, Daniel Einhorn, Vivian A Fonseca, Jeffrey R Garber, W Timothy Garvey, George Grunberger, Yehuda Handelsman, Irl B Hirsch, Paul S Jellinger, Janet B McGill, Jeffrey I Mechanick, Paul D Rosenblit, Guillermo E Umpierrez
A1C = hemoglobin A1C; AACE = American Association of Clinical Endocrinologists; ACCORD = Action to Control Cardiovascular Risk in Diabetes; ACCORD BP = Action to Control Cardiovascular Risk in Diabetes Blood Pressure; ACEI = angiotensin-converting enzyme inhibitor; ADVANCE = Action in Diabetes and Vascular Disease: Preterax and Diamicron MR Controlled Evaluation; AGI = alpha-glucosidase inhibitor; apo B = apolipoprotein B; ASCVD = atherosclerotic cardiovascular disease; BAS = bile acid sequestrant; BCR-QR = bromocriptine quick release; BMI = body mass index; BP = blood pressure; CCB = calcium channel blocker; CHD = coronary heart disease; CKD = chronic kidney disease; CVD = cardiovascular disease; DASH = Dietary Approaches to Stop Hypertension; DPP4 = dipeptidyl peptidase 4; eGFR = estimated glomerular filtration rate; ER = extended release; FDA = Food and Drug Administration; GLP1 = glucagon-like peptide 1; HDL-C = high-density lipoprotein cholesterol; IMPROVE-IT = Improved Reduction of Outcomes: Vytorin Efficacy International Trial; LDL-C = low-density lipoprotein cholesterol; LDL-P = low-density lipoprotein particle; Look AHEAD = Look Action for Health in Diabetes; NPH = neutral protamine Hagedorn; OSA = obstructive sleep apnea; RCT = randomized controlled trial; SU = sulfonylurea; SGLT2 = sodium glucose cotransporter-2; SMBG = self-monitoring of blood glucose; T2D = type 2 diabetes; TZD = thiazolidinedione; VADT = Veterans Affairs Diabetes Trial...
January 2018: Endocrine Practice
Cheng-Wei Chan, Chu-Leng Yu, Jiunn-Cherng Lin, Yu-Cheng Hsieh, Che-Chen Lin, Chen-Ying Hung, Cheng-Hung Li, Ying-Chieh Liao, Chu-Pin Lo, Jin-Long Huang, Ching-Heng Lin, Tsu-Juey Wu
OBJECTIVE: Metformin is the standard first-line drug for patients with Type 2 diabetes (T2DM). However, the optimal second-line oral anti-diabetic agent (ADA) remains unclear. We investigated the cardiovascular risk of various ADAs used as add-on medication to metformin in T2DM patients from a nationwide cohort. METHODS: T2DM patients using different add-on oral ADAs after an initial metformin therapy of > 90 days were identified from the Taiwan National Health Insurance Database...
January 24, 2018: Cardiovascular Diabetology
Gagandeep Singh, Amanjot Singh, Raman K Verma, Rajiv Mall, Uzma Azeem
A novel series of N-substituted-benzimidazolyl linked para substituted benzylidene based molecules containing three pharmacologically potent hydrogen bonding parts namely; 2,4-thiazolidinedione (TZD: a 2,4-dicarbonyl), diethyl malonate (DEM: a 1,3-diester and an isooxazolidinedione analog) and methyl acetoacetate (MAA: a β-ketoester) (6a-11b) were synthesized and evaluated for in vitro α-glucosidase inhibition. The structure of the novel synthesized compounds was confirmed through the spectral studies (LC-MS, 1H NMR, 13C NMR, FT-IR)...
December 30, 2017: Computational Biology and Chemistry
Elizabeth P Mills, K Paige D Brown, Jennifer D Smith, Phillip W Vang, Katie Trotta
Objective: To review current literature for the efficacy and safety of treatment for nonalcoholic fatty liver disease (NAFLD) in patients with type 2 diabetes mellitus (T2DM). Data sources: A PubMed literature search from January 1990 to June 2017 was conducted using the search terms nonalcoholic fatty liver disease, diabetes mellitus, type 2, therapy, treatment, treat, therapeutics, nonalcoholic fatty liver, nonalcoholic hepatosteatosis, NASH, NAFLD, metformin, and statin...
January 2018: Therapeutic Advances in Endocrinology and Metabolism
Jun Young Jang, Hwan Bae, Yong Jae Lee, Young Il Choi, Hyun-Jung Kim, Seung Bum Park, Se Won Suh, Sang Wan Kim, Byung Woo Han
Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, insulin resistance, and inflammation. Here, we report the crystal structures of PPARγ in complex with lobeglitazone, a novel PPARγ agonist, and with rosiglitazone for comparison. The thiazolidinedione (TZD) moiety of lobeglitazone occupies the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i...
January 8, 2018: Scientific Reports
Marie-Laure Plissonnier, Sylvie Fauconnet, Hugues Bittard, Christiane Mougin, Jean Rommelaere, Isabelle Lascombe
Known activators of the Peroxisome Proliferator-Activated Receptor γ (PPARγ), thiazolidinediones (TZD) induce apoptosis in a variety of cancer cells through dependent and/or independent mechanisms of the receptor. We tested a panel of TZD (Rosiglitazone, Pioglitazone, Ciglitazone) to shed light on their potential therapeutic effects on three cervical cancer cell lines (HeLa, Ca Ski, C-33 A). In these cells, only ciglitazone triggered apoptosis through PPARγ-independent mechanisms and in particular via both extrinsic and intrinsic pathways in Ca Ski cells containing Human PapillomaVirus (HPV) type 16...
December 8, 2017: Oncotarget
Xuan-Kang Wang, Ting Sun, Yu-Jiao Li, Yu-Hong Wang, Yan-Jiao Li, Liu-Di Yang, Dan Feng, Ming-Gao Zhao, Yu-Mei Wu
Type 2 diabetes (T2DM) has been associated with learning and memory impairment; however, drugs for diabetes could not prevent the development of cognitive decline in T2DM patients. In the present study, compounds derived from thiazolidinediones (TZD), a PPAR-γ agonist, were synthesized by conjuncting the alkyl-substituted benzimidazole group to TZD group (ATZDs). Based on the in vitro evaluation, the neuroprotection of ATZD2 was further investigated using a streptozotocin-induced T2DM rat model. Pharmacokinetic study showed that ATZD2 could pass the blood-brain barrier (BBB) while the rosiglitazone (RSG, the precursor compound of ATZD2) not...
December 8, 2017: Oncotarget
Emily W Gower, James F Lovato, Walter T Ambrosius, Emily Y Chew, Ronald P Danis, Matthew D Davis, David C Goff, Craig M Greven
PURPOSE: To report the longitudinal association between use of thiazolidinediones (TZDs), visual acuity (VA) change and diabetic eye disease incidence and progression. DESIGN: Cohort study ancillary to a randomized clinical trial METHODS: We analyzed baseline and four-year follow up data of 2,856 ACCORD trial participants with no history of proliferative diabetic retinopathy. Based on stereoscopic fundus photographs, we evaluated diabetic macular edema (DME) progression and DR progression...
December 21, 2017: American Journal of Ophthalmology
Fathalla Belal, Mahmoud A Omar, Sayed Derayea, Mohamed A Hammad, Sahar Zayed, Safaa F Saleh
A simple, sensitive and rapid micellar liquid chromatographic method was developed and validated for simultaneous determination of four drugs, namely, paracetamol (PAR), tizanidine (TZD), aceclofenac (ACF) and nimesulide (NMD). Good chromatographic separation was achieved using Cyano column and micellar mobile phase consisting of 120 mM sodium dodecyl sulfate, 25 mM phosphate buffer and 10% (V/V) butanol. The pH was adjusted to three using phosphoric acid. The total retention time was below 10 min. The analysis was performed at a flow rate of 1 mL/min and a column temperature of 40°C with direct UV detection at 230 nm...
December 11, 2017: Journal of Chromatographic Science
Francesco Zaccardi, Nafeesa N Dhalwani, Jolyon Dales, Hamid Mani, Kamlesh Khunti, Melanie J Davies, David R Webb
AIMS: To assess the evidence supporting the choice of third-line agents in adults with inadequately controlled type 2 diabetes. MATERIALS AND METHODS: We searched randomized controlled trials (RCTs) published between January 2000 and July 2017 that reported data on cardiometabolic outcomes and hypoglycaemia for glucose-lowering agents added to metformin-based dual treatments. Data were stratified by background therapy and RCT duration, and synthesized, when possible, with network meta-analyses...
December 5, 2017: Diabetes, Obesity & Metabolism
Min A Lee, Lingchen Tan, Huiseon Yang, Yeong-Gwan Im, Young Jun Im
Peroxisome proliferator-activator receptor (PPAR) γ is a nuclear hormone receptor that regulates glucose homeostasis, lipid metabolism, and adipocyte function. PPARγ is a target for thiazolidinedione (TZD) class of drugs which are widely used for the treatment of type 2 diabetes. Recently, lobeglitazone was developed as a highly effective TZD with reduced side effects by Chong Kun Dang Pharmaceuticals. To identify the structural determinants for the high potency of lobeglitazone as a PPARγ agonist, we determined the crystal structures of the PPARγ ligand binding domain (LBD) in complex with lobeglitazone and pioglitazone at 1...
December 4, 2017: Scientific Reports
Rakesh Gupta, Hardik Joshi, C S Ramaa
Thiazolidine-2,4-dione (TZD), one of the most frequently encountered heterocyclic ring which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discoveryvarious substitutions at 5th position has been carried out and reviewed. Various substitutions at 5th position has led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery.Acidichydrogen (-NH) of TZD is prime pharmacophoric requirement for activation of PPARγ...
November 29, 2017: Mini Reviews in Medicinal Chemistry
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