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Pioglitazone AND PPAR gamma

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https://www.readbyqxmd.com/read/28744220/rosmarinic-acid-protects-against-inflammation-and-cardiomyocyte-apoptosis-during-myocardial-ischemia-reperfusion-injury-by-activating-peroxisome-proliferator-activated-receptor-gamma
#1
Jichun Han, Dong Wang, Lei Ye, Peng Li, Wenjin Hao, Xiaoyu Chen, Jun Ma, Bo Wang, Jing Shang, Defang Li, Qiusheng Zheng
The cardiac ischemia-reperfusion (I/R) injury greatly influences the therapeutic effect and remains an urgent challenge in clinical therapy. Polypharmacology opens a new therapeutic opportunity to design drugs with a specific target for improving the efficacy. In this study, we first forecasted that Rosmarinic acid (RosA) could be used for the treatment of cardiovascular disease using text mining, chemometric and chemogenomic methods. Consistent with the effect of the positive drug (pioglitazone, PIO), we subsequently validated that RosA pretreatment could restore the decreased cardiac hemodynamic parameters (LVDP, ± dp/dtmin, ± dp/dtmax and CF), decreased the infarct size and the cardiomyocyte apoptosis in a rat model of cardiac I/R injury...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28716729/study-of-new-interactions-of-glitazone-s-stereoisomers-and-the-endogenous-ligand-15d-pgj2-on-six-different-ppar-gamma-proteins
#2
Samuel Álvarez-Almazán, Martiniano Bello, Feliciano Tamay-Cach, Marlet Martínez-Archundia, Diana Alemán-González-Duhart, José Correa-Basurto, Jessica Elena Mendieta-Wejebe
Diabetes mellitus is a chronic disease characterized by hyperglycemia, insulin resistance and hyperlipidemia. Glitazones or thiazolidinediones (TZD) are drugs that act as insulin-sensitizing agents whose molecular target is the peroxisome proliferator-activated receptor gamma (PPARγ). The euglycemic action of TZD has been linked with the induction of type 4 glucose transporter. However, it has been shown that the effect of TZD depends on the specific stereoisomer that interacts with PPARγ. Therefore, this work is focused on exploring the interactions and geometry adopted by glitazone's stereoisomers and one endogenous ligand on different conformations of the six crystals of the PPARγ protein using molecular docking and molecular dynamics (MD) simulations accompanied by the MMGBSA approach...
July 14, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28716464/modulating-effects-of-omega-3-fatty-acids-and-pioglitazone-combination-on-insulin-resistance-through-toll-like-receptor-4-in-type-2-diabetes-mellitus
#3
Salma M Eraky, Noha Abdel-Rahman, Laila A Eissa
Toll-like receptor 4 (TLR-4) plays important roles in innate immunity. Changes in the reduction-oxidation balance of tissues can lead to a pro-inflammatory state and insulin resistance. An action thought to be mediated by TLRs. Omega-3 fatty acids and Peroxisome Proliferator Activated Receptor gamma (PPAR-γ) agonists as pioglitazone are used for decreasing inflammation. The aim of this study is to investigate the anti-diabetic effects of combining omega -3 fatty acid with pioglitazone on type 2 diabetes, and the modifying effects on TLR-4...
June 17, 2017: Prostaglandins, Leukotrienes, and Essential Fatty Acids
https://www.readbyqxmd.com/read/28656266/peroxisome-proliferator-activated-receptor-%C3%AE-agonist-suppresses-mast-cell-maturation-and-induces-apoptosis
#4
Yu Zhang, Xinqian Li, Shengjian Fang, Zhenghua Zhu, Min Yao, Liyun Ying, Liwei Zhu, Zhaoxin Ma, Weihua Wang
Peroxisome proliferator-activated receptor gamma (PPAR γ), is important in the immunoregulation of the allergic response. Mast cells are the most important inflammatory cells in immediate hypersensitivity and allergic diseases. However, there is limited information regarding the effects of PPAR γ on mast cell maturation. In the present study, mouse bone marrow‑derived mast cells (BMMCs) were cultured in interleukin (IL)‑3 and stem cell factor (SCF), in the presence or absence of the PPAR γ agonist, pioglitazone (PIO)...
August 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28595081/pioglitazone-attenuates-lipopolysaccharide-induced-depression-like-behaviors-modulates-nf-%C3%AE%C2%BAb-il-6-stat3-creb-bdnf-pathways-and-central-serotonergic-neurotransmission-in-mice
#5
L Liao, X D Zhang, J Li, Z W Zhang, C C Yang, C L Rao, C J Zhou, L Zeng, L B Zhao, L Fang, D Y Yang, P Xie
Immune activation and inflammation are closely associated with the development of depression. Pioglitazone (PIO), a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist, has exhibited antidepressant-like effects in a couple of studies. However, the underlying mechanisms are far from being fully elucidated. The study aimed to investigate the effects of PIO on depression-like behaviors induced by lipopolysaccharide (LPS) and to explore the possible underlying mechanisms. The results showed that PIO pretreatment attenuated the depression-like behaviors in mice challenged with intracerebroventricular (i...
June 5, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28499821/x-ray-crystal-structure-of-rivoglitazone-bound-to-ppar%C3%AE-and-ppar-subtype-selectivity-of-tzds
#6
Harinda Rajapaksha, Harpreet Bhatia, Kate Wegener, Nikolai Petrovsky, John B Bruning
Thiazolidinedione (TZD) compounds targeting the nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) demonstrate unique benefits for the treatment of insulin resistance and type II diabetes. TZDs include rosiglitazone, pioglitazone and rivoglitazone, with the latter being the most potent. The TZDs are only marginally selective for the therapeutic target PPARγ as they also activate PPARα and PPARδ homologues to varying degrees, causing off-target effects. While crystal structures for TZD compounds in complex with PPARγ are available, minimal structural information is available for TZDs bound to PPARα and PPARδ...
August 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28498501/ppar-gamma-agonist-pioglitazone-modifies-craving-intensity-and-brain-white-matter-integrity-in-patients-with-primary-cocaine-use-disorder-a-double-blind-randomized-controlled-pilot-trial
#7
Joy M Schmitz, Charles E Green, Khader M Hasan, Jessica Vincent, Robert Suchting, Michael F Weaver, F Gerard Moeller, Ponnada A Narayana, Kathryn A Cunningham, Kelly T Dineley, Scott D Lane
BACKGROUND AND AIMS: Pioglitazone (PIO), a potent agonist of PPAR-gamma, is a promising candidate treatment for cocaine use disorder (CUD). We tested the effects of PIO on targeted mechanisms relevant to CUD: cocaine craving and brain white matter (WM) integrity. Feasibility, medication compliance and tolerability were evaluated. DESIGN: Two-arm double-blind randomized controlled proof-of-concept pilot trial of PIO or placebo (PLC). SETTING: Single-site out-patient treatment research clinic in Houston, TX, USA...
May 12, 2017: Addiction
https://www.readbyqxmd.com/read/28449155/mitochondrial-dysfunction-in-diabetic-cardiomyopathy-effect-of-mesenchymal-stem-cell-with-ppar-%C3%AE-agonist-or-exendin-4
#8
Mohamed Abd Elaziz Wassef, Ola M Tork, Laila A Rashed, Walaa Ibrahim, Heba Morsi, Dina Mohamed Mekawy Rabie
Therapy targeting mitochondria may provide novel ways to treat diabetes and its complications. Bone marrow-derived mesenchymal stem cells (MSCs), the peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists and exendin-4; an analog of glucagon-like peptide-1 have shown cardioprotective properties in many cardiac injury models. So, we evaluated their effects in diabetic cardiomyopathy (DCM) in relation to mitochondrial dysfunction. This work included seven groups of adult male albino rats: the control group, the non-treated diabetic group, and the treated diabetic groups: one group was treated with MSCs only, the second with pioglitazone only, the third with MSCs and pioglitazone, the forth with exendin-4 only and the fifth with MSCs and exendin-4...
April 27, 2017: Experimental and Clinical Endocrinology & Diabetes
https://www.readbyqxmd.com/read/28397719/toll-like-receptor-4-signaling-pathway-in-the-protective-effect-of-pioglitazone-on-experimental-immunoglobulin-a-nephropathy
#9
Jia-Nan Zou, Jing Xiao, Sha-Sha Hu, Chen-Sheng Fu, Xiao-Li Zhang, Zhen-Xing Zhang, Yi-Jun Lu, Wei-Jun Chen, Zhi-Bin Ye
BACKGROUND: In vitro experiments have revealed that toll-like receptor 4 (TLR4) pathway is involved in the progression of immunoglobulin A nephropathy (IgAN) by induction of proinflammatory cytokines. Evidence showed that, in other disease models, peroxisome proliferator-activated receptor-γ (PPAR-γ) agonists have been shown to exert anti-inflammatory effects through suppression of the expression and activity of TLR4. However, the interaction between PPAR-γ and TLR4 in IgAN has not been fully studied both in vitro and in vivo...
April 20, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28254448/effects-of-pioglitazone-on-the-incidence-of-dementia-in-patients-with-diabetes
#10
Ping-Song Chou, Bo-Lin Ho, Yuan-Han Yang
AIMS: Peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists exert neuroprotective effects in the brain. Therefore, in this population-based cohort study, we investigated the effects of pioglitazone, a PPAR-γ agonist, on the risk of dementia. METHODS: By using claims data from Taiwan's National Health Insurance Research Database, we included 6401 patients with diabetes who were treated with pioglitazone and 12,802 age- and sex-matched patients with diabetes who were never treated with pioglitazone from 2004 to 2009 and who were free of dementia at baseline...
June 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28219679/thiazolidinediones-abrogate-cervical-cancer-growth
#11
Beverly R Wuertz, Lindsay Darrah, Justin Wudel, Frank G Ondrey
Peroxisome proliferator-activated receptor gamma (PPAR γ) is activated by thiazolidinedione drugs (TZDs) and can promote anti-cancer properties. We used three TZDs (pioglitazone, rosiglitazone, and ciglitazone) to target cervical cancer cell lines and a nude mouse animal model. Each agent increased activation of PPAR γ, as judged by a luciferase reporter gene assay in three HPV-associated cell lines (CaSki, SiHa, and HeLa cells) while decreasing cellular proliferation in a dose-dependent manner. They also promoted Oil Red O accumulation in treated cell lines and upregulated the lipid differentiation marker adipsin...
April 15, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28031713/pioglitazone-could-induce-remission-in-major-depression-a-meta-analysis
#12
Romain Colle, Delphine de Larminat, Samuel Rotenberg, Franz Hozer, Patrick Hardy, Céline Verstuyft, Bruno Fève, Emmanuelle Corruble
BACKGROUND: Pioglitazone, a selective agonist of the nuclear transcription factor peroxisome proliferator-activated receptor-gamma (PPAR-γ), prescribed for the treatment of type 2 diabetes, could have antidepressant properties. However, its potential to induce remission of major depressive episodes, the optimal clinical target for an antidepressant drug, is a matter of concern. Indeed, only one out of four double-blind randomized controlled trials show higher remission rates with pioglitazone than with control treatments...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/27978584/ppar-%C3%AE-agonists-for-the-treatment-of-major-depression-a-review
#13
REVIEW
R Colle, D de Larminat, S Rotenberg, F Hozer, P Hardy, C Verstuyft, B Fève, E Corruble
Introduction: Selective agonists of the nuclear transcription factor peroxisome proliferator-activated receptor-gamma (PPAR-γ) are used for the treatment of type 2 diabetes. We reviewed their efficacy and safety for the treatment of major depression and the association of their potential antidepressant effects with changes in biomarkers of metabolism and inflammation. Methods: From 8 studies, 4 open-label trials, and 4 randomized controlled trials (RCT) (3 vs. placebo and 1 vs. metformin), 448 patients with major depression were included, of which 209 patients received PPAR-γ agonists (pioglitazone or rosiglitazone) for 6-12 weeks, either alone or in add-on therapy to conventional treatments...
March 2017: Pharmacopsychiatry
https://www.readbyqxmd.com/read/27930978/mechanism-of-action-and-effect-of-immune-modulating-agents-in-the-treatment-of-psoriasis
#14
Rehab M El-Gharabawy, Amira S Ahmed, Amal H Al-Najjar
OBJECTIVES: The aim of this work is to study the possible mechanisms through which different immune-modulating agents can produce their beneficial effects on treatment of psoriasis and to determine whether the supplementation of these agents for psoriasis patients induces regression of psoriasis. SUBJECTS AND METHODS: One hundred fifty participants were included in this study. The participants were divided into five groups: 1. Normal control group, 2. Psoriasis patients not taking any treatment, 3...
January 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27792919/ppar-%C3%AE-agonist-pioglitazone-regulates-dendritic-cells-immunogenicity-mediated-by-dc-sign-via-the-mapk-and-nf-%C3%AE%C2%BAb-pathways
#15
Weiguo Zhu, Hui Yan, Shan Li, Wencheng Nie, Fangyan Fan, Jianhua Zhu
Dendritic cell-specific ICAM-3 grabbing non-integrin (DC-SIGN) is a dendritic cell-specific lectin which participates in dendritic cell (DC) trafficking, antigen uptake and DC-T cell interactions at the initiation of immune responses. This study investigated whether peroxisome proliferator-activated receptor-gamma (PPAR-γ) activation in human DCs regulates the immunogenicity of DCs mediated by DC-SIGN and exploited the possible molecular mechanisms, especially focused on the signaling pathways of mitogen-activated protein kinases (MAPK) and nuclear factor-κB (NF-κB)...
December 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27698768/effect-of-pioglitazone-on-neuropathic-pain-and-spinal-expression-of-tlr-4-and-cytokines
#16
Hongbin Jia, Shuangshuang Xu, Qingzhen Liu, Jian Liu, Jianguo Xu, Weiyan Li, Yi Jin, Qing Ji
The molecular mechanisms underlying neuropathic pain have yet to be elucidated. The present study aimed to examine the modulation of neuroimmune activation in the spinal cord by the synthetic peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist, pioglitazone (Pio), in a rat model of neuropathic pain induced by chronic constriction injury (CCI). Rats were randomly assigned into four groups: Sham surgery with vehicle, chronic constriction injury with vehicle or Pio (10 mg/kg), and chronic constriction injury with Pio and a PPAR-γ antagonist GW9662 (2 mg/kg)...
October 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27560168/evaluation-of-the-ppar-%C3%AE-agonist-pioglitazone-in-mild-asthma-a-double-blind-randomized-controlled-trial
#17
RANDOMIZED CONTROLLED TRIAL
J R Anderson, K Mortimer, L Pang, K M Smith, H Bailey, D B Hodgson, D E Shaw, A J Knox, T W Harrison
BACKGROUND: Peroxisome proliferator-activated receptor gamma (PPAR-γ) is a nuclear receptor that modulates inflammation in models of asthma. To determine whether pioglitazone improves measures of asthma control and airway inflammation, we performed a single-center randomized, double-blind, placebo-controlled, parallel-group trial. METHODS: Sixty-eight participants with mild asthma were randomized to 12 weeks pioglitazone (30 mg for 4 weeks, then 45 mg for 8 weeks) or placebo...
2016: PloS One
https://www.readbyqxmd.com/read/27175924/peroxisome-proliferator-activated-receptor-gamma-dependent-pathway-reduces-the-phosphorylation-of-dynamin-related-protein-1-and-ameliorates-hippocampal-injury-induced-by-global-ischemia-in-rats
#18
Yao-Chung Chuang, Tsu-Kung Lin, Ding-I Yang, Jenq-Lin Yang, Chia-Wei Liou, Shang-Der Chen
BACKGROUND: Dynamin-related protein 1 (Drp1) is a mitochondrial fission protein that, upon phosphorylation at serine 616 (p-Drp1(Ser616)), plays a pivotal role in neuronal death after ischemia. In the present study, we hypothesized that peroxisome proliferator-activated receptor-gamma (PPARγ)-dependent pathway can reduce the expression of p-Drp1(Ser616) and ameliorate hippocampal injury induced by global ischemia in rats. RESULTS: We found that pretreatment of the rats with Mdivi-1, a selective Drp1 inhibitor, decreased the level of transient global ischemia (TGI)-induced p-Drp1(Ser616) and reduced cellular contents of oxidized proteins, activated caspase-3 expression as well as the extent of DNA fragmentation...
May 12, 2016: Journal of Biomedical Science
https://www.readbyqxmd.com/read/27150869/treatment-of-mitochondrial-diabetes-with-a-peroxisome-proliferator-activated-receptor-ppar-gamma-agonist
#19
Hiroyo Ninomiya, Ayumu Hirata, Junji Kozawa, Shinsuke Nakata, Takekazu Kimura, Tetsuhiro Kitamura, Tetsuyuki Yasuda, Michio Otsuki, Akihisa Imagawa, Hideaki Kaneto, Tohru Funahashi, Iichiro Shimomura
The 3243 A>G mutation in mitochondrial DNA is the most common cause of monogenic diabetes mellitus in Japan. A 45-year-old woman with mitochondrial diabetes and significant insulin resistance presented with hypoadiponectinemia despite a normal amount of visceral fat. Three months of treatment with pioglitazone (PIO) improved her blood glucose profile and response to the 75-g oral glucose tolerance test. These changes were accompanied by the amelioration of her insulin resistance and the impairment of early-phase insulin secretion...
2016: Internal Medicine
https://www.readbyqxmd.com/read/27149161/effects-of-a-ppar-gamma-receptor-agonist-and-an-angiotensin-receptor-antagonist-on-aortic-contractile-responses-to-alpha-receptor-agonists-in-diabetic-and-or-hypertensive-rats
#20
Ibrahim Tugrul, Turhan Dost, Omer Demir, Filiz Gokalp, Ozlem Oz, Necip Girit, Mustafa Birincioglu
AIM: The aim of this study was to investigate the effects of pioglitazone and losartan pre-treatment on the aortic contractile response to the alpha-1 agonist, phenylephrine, and the alpha-2 agonist, clonidine, in L-NAME-induced hypertensive, STZ-induced diabetic, and hypertensive diabetic rats. METHODS: Male Wistar rats were randomly allocated to four groups: control, diabetic (DM), hypertensive (HT) and hypertensive diabetic (HT + DM) groups. Three weeks after drug application, in vitro dose-response curves to phenylephrine (Phe) (10(-9)-10(-5) M) and clonidine (Clo) (10(-9)-10(-5) M) were recorded in aortic rings in the absence (control) and presence of pioglitazone (10 µM) and/or losartan (10 µM)...
May 2016: Cardiovascular Journal of Africa
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