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https://www.readbyqxmd.com/read/29130039/a-sustained-release-membrane-of-thiazolidinedione-8-effect-on-formation-of-a-candida-bacteria-mixed-biofilm-on-hydroxyapatite-in-a-continuous-flow-model
#1
Mark Feldman, Julia Shenderovich, Eran Lavy, Michael Friedman, Doron Steinberg
Thiazolidinediones (TZDs) have been found to act as effective quorum sensing quenchers, capable of preventing biofilm formation. Our previous studies demonstrated a profound antibiofilm effect of the TZD derivative thiazolidinedione-8 (S-8), either in solution or incorporated into a sustained-release membrane (SRM-S-8) under batch conditions. In the present study, we used a constant depth film fermenter model in order to investigate the impact of SRM-S-8 on mixed C. albicans-S. mutans biofilm development, under flow conditions...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29125710/thiazolidinedione-therapy-and-breast-cancer-risk-in-diabetic-women-a-systematic-review-and-meta-analysis
#2
REVIEW
Rui Du, Lin Lin, Di Cheng, Yu Xu, Min Xu, Yuhong Chen, Weiqing Wang, Yufang Bi, Donghui Li, Jieli Lu
BACKGROUND: Rising experimental evidence suggests that thiazolidinediones (TZDs) exert a protective effect on breast cancer. However, studies concerning this issue were inconsistent and limited. Hence, we performed a meta-analysis with data from currently available studies to evaluate the effect of TZDs on breast cancer risk among diabetic women. METHODS: We comprehensively searched for all pertinent studies addressing TZDs use and breast cancer risk published before January 1, 2016 in PubMed, Clinical Trials and Cochrane library...
November 10, 2017: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/29122042/peroxisome-proliferator-activated-receptor-gamma-ppar%C3%AE-agonist-fails-to-overcome-trans-10-cis-12-conjugated-linoleic-acid-cla-inhibition-of-milk-fat-in-dairy-sheep
#3
E C Sandri, M Camêra, E M Sandri, K J Harvatine, D E De Oliveira
The trans-10, cis-12 conjugated linoleic acid (CLA) causes milk fat depression by downregulating expression of genes and transcription factors involved in lipogenesis and it has been proposed that peroxisome proliferator-activated receptor gamma (PPARγ) can be inhibited by trans-10, cis-12 CLA. The PPARγ is a nuclear receptor activated by natural or synthetic ligands and promotes expression of lipogenic genes and its effect on mammary lipogenesis and the interaction with trans-10, cis-12 CLA in lactating ewes was evaluated using thiazolidinedione (TZD), a chemical PPARγ agonist...
November 10, 2017: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/29108837/factors-associated-with-type-2-diabetes-mellitus-treatment-choice-across-four-european-countries
#4
Edith M Heintjes, Jetty A Overbeek, Gillian C Hall, Daniel Prieto-Alhambra, Francesco Lapi, Niklas Hammar, Irene D Bezemer
PURPOSE: The aim of this analysis was to identify factors associated with the choice of type 2 diabetes mellitus (T2DM) therapy at the time of intensification of antidiabetic treatment across 4 European countries. METHODS: Antidiabetic drug prescription/dispensing records and patients' characteristics were obtained from the electronic health care records of patients with T2DM from the Netherlands (NL), Italy, and Spain (ES) (all, 2007-2011); and the United Kingdom (UK; 2008-2012)...
November 3, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/29089569/novel-benzylidene-thiazolidinedione-derivatives-as-partial-ppar%C3%AE-agonists-and-their-antidiabetic-effects-on-type-2-diabetes
#5
Sabina Yasmin, Fabio Capone, Antonio Laghezza, Fabrizio Dal Piaz, Fulvio Loiodice, Viswanathan Vijayan, Velmurugan Devadasan, Susanta K Mondal, Özlem Atlı, Merve Baysal, Ashok K Pattnaik, Venkatesan Jayaprakash, Antonio Lavecchia
Peroxisome proliferator-activated receptor γ (PPARγ) has received significant attention as a key regulator of glucose and lipid homeostasis. In this study, we synthesized and tested a library of novel 5-benzylidene-thiazolidin-2,4-dione (BTZD) derivatives bearing a substituent on nitrogen of TZD nucleus (compounds 1a-1k, 2i-10i, 3a, 6a, and 8a-10a). Three compounds (1a, 1i, and 3a) exhibited selectivity towards PPARγ and were found to be weak to moderate partial agonists. Surface Plasmon Resonance (SPR) results demonstrated binding affinity of 1a, 1i and 3a towards PPARγ...
October 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29071111/impact-of-pioglitazone-and-bradykinin-type-1-receptor-antagonist-on-type-2-diabetes-in-high-fat-diet-fed-c57bl-6j-mice
#6
S El Akoum, Y Haddad, R Couture
AIM: Type 2 diabetes (T2D) is a major complication of obesity and a leading cause of morbidity and mortality. Antagonizing bradykinin type 1 receptor (B1R) improved body and tissue fat mass and reversed vascular and adipose tissue inflammation in a rat model of insulin resistance. This study aimed at evaluating further the role of B1R in a mouse model of T2D by comparing the antidiabetic and anti-inflammatory effects of the B1R antagonist SSR240612 (SSR) in adipose tissue with those of pioglitazone (TZD), an activator of peroxisome proliferator-activated receptor gamma...
September 2017: Obesity Science & Practice
https://www.readbyqxmd.com/read/29056962/chiglitazar-preferentially-regulates-gene-expression-via-configuration-restricted-binding-and-phosphorylation-inhibition-of-ppar%C3%AE
#7
De-Si Pan, Wei Wang, Nan-Song Liu, Qian-Jiao Yang, Kun Zhang, Jing-Zhong Zhu, Song Shan, Zhi-Bin Li, Zhi-Qiang Ning, Laiqiang Huang, Xian-Ping Lu
Type 2 diabetes mellitus is often treated with insulin-sensitizing drugs called thiazolidinediones (TZD), which improve insulin resistance and glycemic control. Despite their effectiveness in treating diabetes, these drugs provide little protection from eminent cardiovascular disease associated with diabetes. Here we demonstrate how chiglitazar, a configuration-restricted non-TZD peroxisome proliferator-activated receptor (PPAR) pan agonist with moderate transcription activity, preferentially regulates ANGPTL4 and PDK4, which are involved in glucose and lipid metabolism...
2017: PPAR Research
https://www.readbyqxmd.com/read/29047219/addition-of-dipeptidyl-peptidase-4-inhibitors-to-insulin-treatment-in-type-2-diabetes-patients-a-meta-analysis
#8
Wenjia Yang, Xiaoling Cai, Xueying Gao, Yifei Chen, Chen Ling, Linong Ji
AIMS: To evaluate the efficacy and safety of combining insulin therapy with dipeptidyl peptidase 4 (DPP-4) inhibitors compared to combining insulin therapy with placebo or other antihyperglycaemic agents. MATERIALS AND METHODS: A literature search was conducted via electronic databases. The inclusion criteria were randomized controlled trials (RCTs) comparing the addition of DPP-4 inhibitors to insulin with the addition of placebo or other active hypoglycaemic agents to insulin therapy, study duration of no less than 12 weeks performed in type 2 diabetes patients, and the availability of outcome data to evaluate a change in the HbA1c ...
October 19, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/29046921/pioglitazone-reduces-cold-induced-brown-fat-glucose-uptake-despite-induction-of-browning-in-cultured-human-adipocytes-a-randomised-controlled-trial-in-humans
#9
Rebecca K C Loh, Melissa F Formosa, Nina Eikelis, David A Bertovic, Mitchell J Anderson, Shane A Barwood, Shane Nanayakkara, Neale D Cohen, Andre La Gerche, Anne T Reutens, Kenneth S Yap, Thomas W Barber, Gavin W Lambert, Martin H Cherk, Stephen J Duffy, Bronwyn A Kingwell, Andrew L Carey
AIMS/HYPOTHESIS: Increasing brown adipose tissue (BAT) activity is a possible therapeutic strategy to increase energy expenditure and glucose and lipid clearance to ameliorate obesity and associated comorbidities. The thiazolidinedione (TZD) class of glucose-lowering drugs increase BAT browning in preclinical experimental models but whether these actions extend to humans in vivo is unknown. The aim of this study was to determine the effect of pioglitazone treatment on adipocyte browning and adaptive thermogenesis in humans...
October 18, 2017: Diabetologia
https://www.readbyqxmd.com/read/29023313/mini-scleral-lenses-for-correction-of-refractive-errors-after-radial-keratotomy
#10
Hsiao-Sang Chu, I-Jong Wang, Grace A Tseng, Wei-Li Chen, Yu-Chih Hou, Fung-Rong Hu
OBJECTIVE: To evaluate the factors affecting clinical outcomes of correcting cumulative refractive errors or irregular astigmatism after radial keratotomy (RK) using mini-scleral lenses. METHODS: We retrospectively analyzed 36 eyes receiving mini-scleral lenses after RK from July 2011 to June 2016. Analyses included age, refractive errors, best spectacle-corrected visual acuity (BSCVA), best contact lens-corrected visual acuity (BCLCVA), topographic indices, RK treatment zone diameter (TZD), power difference (PrD) within the RK treatment zone, and decentration distance (DD) of the RK treatment zone center...
October 11, 2017: Eye & Contact Lens
https://www.readbyqxmd.com/read/28979777/changes-in-treatment-of-hyperglycemia-in-a-hypertensive-type-2-diabetes-population-as-renal-function-declines
#11
Larry A Weinrauch, Alissa R Segal, George P Bayliss, Jiankang Liu, Eric Wisniewski, John A D'Elia
BACKGROUND: Cardiovascular complications associated with expensive noninsulin agents for type 2 diabetes are the focus of concern in light of the risk of kidney dysfunction with aging. Head-to-head comparisons are unavailable to guide the choice of new drugs for hyperglycemia in patients with type 2 diabetes, decreased estimated glomerular filtration rate (eGFR) and increased cardiovascular risk. A first approach would be to document current medication choices. METHODS: All prescriptions for 10 151 patients (5623 males/4528 females) with both type 2 diabetes and hypertension seen two or  more times during a 5-year period (2007-12) at Joslin Diabetes Center were evaluated...
October 2017: Clinical Kidney Journal
https://www.readbyqxmd.com/read/28956370/effects-of-lobeglitazone-a-new-thiazolidinedione-on-osteoblastogenesis-and-bone-mineral-density-in-mice
#12
Kyoung Min Kim, Hyun Jin Jin, Seo Yeon Lee, Hyo Jin Maeng, Gha Young Lee, Tae Jung Oh, Sung Hee Choi, Hak Chul Jang, Soo Lim
BACKGROUND: Bone strength is impaired in patients with type 2 diabetes mellitus despite an increase in bone mineral density (BMD). Thiazolidinedione (TZD), a peroxisome proliferator activated receptor γ agonist, promotes adipogenesis, and suppresses osteoblastogenesis. Therefore, its use is associated with an increased risk of fracture. The aim of this study was to examine the in vitro and in vivo effects of lobeglitazone, a new TZD, on bone. METHODS: MC3T3E1 and C3H10T1/2 cells were cultured in osteogenic medium and exposed to lobeglitazone (0...
September 2017: Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28928054/effect-of-the-antidiabetic-agent-pioglitazone-on-bone-metabolism-in-rats
#13
Junkichi Kanda, Nobuo Izumo, Yoshiko Kobayashi, Kenji Onodera, Taketoshi Shimakura, Noriaki Yamamoto, Hideaki E Takahashi, Hiroyuki Wakabayashi
Thiazolidinediones (TZDs) are synthetic peroxisome proliferator-activated receptor gamma (PPARγ) agonists used as therapy for type 2 diabetes. However, clinical studies reported that the therapeutic modulation of PPARγ activity using TZDs may induce negative effects on bone metabolism. This study aimed to evaluate the effect of the TZD pioglitazone on bone metabolism in rats. Male Wistar rats were treated orally with pioglitazone 5 or 20 mg/kg daily for 24 weeks. Bone strength was evaluated using a 3-point bending method, and bone histomorphometry was analyzed...
August 26, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28920418/myogenic-satellite-cells-differentiation-with-linolenic-and-retinoic-and-thiazolidenediones-from-prepubertal-korean-black-goat
#14
Sugathan Subi, Sungjin Lee, Supriya Shiwani, Naresh Kumar Singh
Objective: Myogenic satellite cells were isolated from semitendinosus muscle of prepubertal Korean black goat to observe the differential effect of linolenic and retinoic acid in thepresence of thiazolidinediones and also to observe the production insulin sensitive preadipocyte. Methods: Cells were characterized for its stemness with CD 34, CD 13, CD 106, CD44, Vimentin surface markers using flow cytometry. Cells characterized themselves to possess significant (p<0...
September 18, 2017: Asian-Australasian Journal of Animal Sciences
https://www.readbyqxmd.com/read/28872778/effects-of-thiazolidinedione-in-patients-with-active-bladder-cancer
#15
Roger Li, Michael J Metcalfe, James E Ferguson, Sharada Mokkapati, Graciela M Nogueras González, Colin P Dinney, Neema Navai, David J McConkey, Sunil K Sahai, Ashish M Kamat
OBJECTIVE: To examine the influence of perioperative thiazolidinedione (TZD) on cancer-specific outcomes in patients with diabetes mellitus (DM) undergoing radical cystectomy (RC) for urothelial carcinoma (UC). PATIENTS AND METHODS: A retrospective cohort of 173 patients with DM undergoing RC from 2005 to 2010 was identified. Of those, 53 were on TZD treatment at the time of RC, with 33 patients taking pioglitazone. Baseline clinicopathological characteristics, as well as cancer-specific survival (CSS), recurrence-free survival (RFS), and overall survival (OS) were compared between the patients on and off TZD therapy at the time of RC...
September 5, 2017: BJU International
https://www.readbyqxmd.com/read/28854981/rosiglitazone-increases-endothelial-cell-migration-and-vascular-permeability-through-akt-phosphorylation
#16
Yun Hyi Ku, Bong-Jun Cho, Min Joo Kim, Soo Lim, Young Joo Park, Hak C Jang, Sung Hee Choi
BACKGROUND: Thiazolidinediones (TZDs), peroxisome proliferator-activated receptor-γ (PPAR-γ) agonists, exhibit anti-inflammatory and antioxidant properties and inhibit endothelial inflammation and dysfunction, which is anti-atherogenic. However, fluid retention, which may lead to congestive heart failure and peripheral edema, is also a concern, which may result from endothelial cell leakage. In the current study, we examined the effects of PPAR-γ agonists on vascular endothelial cell migration and permeability in order to determine its underlying mechanisms...
August 30, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28853334/identification-of-novel-ppar%C3%AE-%C3%AE-dual-agonists-by-virtual-screening-admet-prediction-and-molecular-dynamics-simulations
#17
Xin Liu, Zhi Jing, Wen-Qing Jia, Shu-Qing Wang, Ying Ma, Wei-Ren Xu, Xian-Chao Cheng
PPARα and PPARγ have been the most widely studied Peroxisome Proliferator-Activated Receptor (PPAR) subtypes due to their important roles in regulating glucose, lipids and cholesterol metabolism. By combining the lowering serum triglyceride levels benefit of PPARα agonists (such as fibrates) with the glycemic advantages of the PPARγ agonists (such as TZD), the dual PPAR agonists approach can both improve the metabolic effects and minimize the side effects caused by either agent alone, and hence has become a promising strategy for designing effective drugs against type-2 diabetes...
August 30, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28816105/thiazolidinedione-drugs-in-the-treatment-of-type-2-diabetes-mellitus-past-present-and-future
#18
Melissa A Davidson, Donald R Mattison, Laurent Azoulay, Daniel Krewski
Thiazolidinedione (TZD) drugs used in the treatment of type 2 diabetes mellitus (T2DM) have proven effective in improving insulin sensitivity, hyperglycemia, and lipid metabolism. Though well tolerated by some patients, their mechanism of action as ligands of peroxisome proliferator-activated receptors (PPARs) results in the activation of several pathways in addition to those responsible for glycemic control and lipid homeostasis. These pathways, which include those related to inflammation, bone formation, and cell proliferation, may lead to adverse health outcomes...
August 17, 2017: Critical Reviews in Toxicology
https://www.readbyqxmd.com/read/28781774/level-of-dietary-energy-and-2-4-thiazolidinedione-alter-molecular-and-systemic-biomarkers-of-inflammation-and-liver-function-in-holstein-cows
#19
Afshin Hosseini, Mustafa Salman, Zheng Zhou, James K Drackley, Erminio Trevisi, Juan J Loor
BACKGROUND: The objective of the study was to evaluate the effect of overfeeding a moderate energy diet and a 2,4-thiazolidinedione (TZD) injection on blood and hepatic tissue biomarkers of lipid metabolism, oxidative stress, and inflammation as it relates to insulin sensitivity. RESULTS: Fourteen dry non-pregnant cows were fed a control (CON) diet to meet 100% of NRC requirements for 3 wk, after which half of the cows were assigned to a moderate-energy diet (OVE) and half of the cows continued on CON for 6 wk...
2017: Journal of Animal Science and Biotechnology
https://www.readbyqxmd.com/read/28780749/testing-the-ability-of-rhodanine-and-2-4-thiazolidinedione-to-interact-with-the-human-pancreatic-alpha-amylase-electron-density-descriptors-complement-molecular-docking-qm-and-qm-mm-dynamics-calculations
#20
Rajendran Niranjana Devi, Maria G Khrenova, Samuel Israel, Chellam Anzline, Andrey A Astakhov, Vladimir G Tsirelson
A combined molecular docking, QM, and QM/MM dynamics modeling complemented with electron-density based descriptors computed at the B3LYP/6-311G++(d,p) level of theory have been carried out in order to understand the ability of the drugs rhodanine (RD) and 2,4-thiazolidinedione (TZD) in the effective treatment of type 2 diabetes mellitus. The global HOMO/LUMO descriptors provided just a very rough estimate of the chemical reactivity of both molecules, while the features of electron density studied in terms of its Laplacian and electrostatic potential allowed identifying the local electron rich/poor sites which were associated with the regions of electrophilic/nucleophilic attacks in RD and TZD...
September 2017: Journal of Molecular Modeling
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