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Fenofibrate

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https://www.readbyqxmd.com/read/29446047/epigallocatechin-gallate-suppresses-hepatic-cholesterol-synthesis-by-targeting-srebp-2-through-sirt1-foxo1-signaling-pathway
#1
Yongnan Li, Shuodong Wu
This study aims to explore the effect of epigallocatechin gallate (EGCG) on blood lipids, liver lipids, and cholesterol synthesis in hyperlipidemic rats. SREBP-2 transgenic rats were used to investigate the transcriptional level of SREBP-2 regulated by SIRT-1/FOXO1 and the molecular mechanism of rate-limiting enzyme HMGCR that affects cholesterol synthesis. Rat models of hyperlipidemia were established and administered EGCG. Cholesterol synthesis was observed. Enzyme linked immunosorbent assay was used to determine serum triglyceride (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), free fatty acid (FFA), superoxide dismutase (SOD), malondialdehyde (MDA), and T-AOC contents...
February 14, 2018: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29441882/dissolution-permeation-the-importance-of-the-experimental-setup-for-the-prediction-of-formulation-effects-on-fenofibrate-in-vivo-performance
#2
K Forner, I Hidalgo, J Lin, M Ackermann, P Langguth
The evaluation of formulation strategies in early drug development requires in vitro methods that correctly predict oral drug absorption. The present study aimed to define key parameters for the predictability of dissolution/permeation experiments. Dissolution/permeation experiments were performed in various setups. The IDAS1 chamber, Ussing chamber, and transwells were used as Caco-2 cell based dissolution/permeation models to study the impact of chamber volumes and vertical or horizontal membrane orientation...
October 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29438297/fenofibrate-nanocrystals-embedded-in-oral-strip-films-for-bioavailability-enhancement
#3
Bhavesh D Kevadiya, Manish Barvaliya, Lu Zhang, Ashish Anovadiya, Harshad Brahmbhatt, Parimal Paul, Chandrabhanu Tripathi
The aim of the present study was to make a fenofibrate (FNB) nanocrystal (NC) by wet media milling, characterizations and formulates into oral strip-films (OSFs). Mechanical properties, redispersion study, and solid-state characterizations results suggested that reduction of drug crystal size at nanoscale and incorporation into OSFs does not affect the solid-state properties of the drug. In vitro dissolution kinetics showed enhanced dissolution rate was easily manipulated by changing the thickness of the OSF...
February 13, 2018: Bioengineering
https://www.readbyqxmd.com/read/29436756/alirocumab-versus-usual-lipid-lowering-care-as-add-on-to-statin-therapy-in-individuals-with-type-2-diabetes-and-mixed-dyslipidaemia-the-odyssey-dm-dyslipidemia-randomized-trial
#4
Kausik K Ray, Lawrence A Leiter, Dirk Müller-Wieland, Bertrand Cariou, Helen M Colhoun, Robert R Henry, Francisco J Tinahones, Maja Bujas-Bobanovic, Catherine Domenger, Alexia Letierce, Rita Samuel, Stefano Del Prato
AIMS: Individuals with type 2 diabetes (T2DM) and mixed dyslipidaemia represent a high-risk and difficult-to-treat population. ODYSSEY DM-DYSLIPIDEMIA (NCT02642159) compared alirocumab, a proprotein convertase subtilisin-kexin type 9 inhibitor, with usual care (UC) in individuals with T2DM and mixed dyslipidaemia not optimally managed by maximally-tolerated statins. MATERIALS AND METHODS: UC options (no additional lipid-lowering therapy; fenofibrate; ezetimibe; omega-3 fatty acid; nicotinic acid) were selected prior to stratified randomization to open-label alirocumab 75 mg every 2 weeks (Q2W; with increase to 150 mg Q2W at Week [W]12 if W8 non-high-density lipoprotein cholesterol [non-HDL-C] was ≥2...
February 13, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29433142/ppar-%C3%AE-agonist-improves-hyperglycemia-induced-oxidative-stress-in-pancreatic-cells-by-potentiating-antioxidant-defense-system
#5
Habib Yaribeygi, Mohammad Taghi Mohammadi, Amirhossein Sahebkar
BACKGROUND: Diabetes-induced oxidative stress has an essential role in pancreatic cells dysfunction. The present study aimed to evaluate whether peroxisome proliferator activated receptor- alpha (PPAR-α) induction by fenofibrate counterbalances oxidative stress in pancreatic cells. METHODS: In this in vivo study, male Wistar rats were randomly divided into four groups as normal, normal treated, diabetic and diabetic treated groups (n=6 in each group). Diabetes was induced by a single intravenous injection of streptozotocin (45 mg/kg)...
February 12, 2018: Drug Research
https://www.readbyqxmd.com/read/29412757/effects-of-triptolide-on-pharmacokinetics-of-fenofibrate-in-rats-and-its-potential-mechanism
#6
Tonghui Li, Jijun Liu, Yingying Zheng, Shengchang Yang, Xun Liu, Xuejing Li
1. Triptolide and fenofibrate are often used together for the treatment of nephrotic syndrome in Chinese clinics. 2. This study investigates the effects of triptolide on the pharmacokinetics of fenofibrate in rats and it potential mechanism. 3. The pharmacokinetics of fenofibrate (20 mg/kg) with or without triptolide pretreatment (2 mg/kg/day for 7 days) were investigated. Additionally, the inhibitory effects of triptolide on the metabolic stability of fenofibrate were investigated using rat liver microsome incubation systems...
February 7, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29398675/the-novel-apolipoprotein-e-mutation-apoe-chengdu-c-518t%C3%AF-c-p-l173p-in-a-chinese-patient-with-lipoprotein-glomerulopathy
#7
Hongyan Wu, Yuan Yang, Zhangxue Hu
AIMS: Lipoprotein glomerulopathy (LPG) is a rare inherited renal disease. Several apolipoprotein E (apoE) mutations have been reported to be related to LPG. Herein, we report a case of a LPG patient with a novel apoE mutation. METHODS: A 45-year-old Chinese female was diagnosed as LPG by renal biopsy. APOE gene was sequenced. Clinical and genetic studies were conducted. RESULTS: The patient presented with nephrotic syndrome and hypertension...
February 2, 2018: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/29370865/a-mechanism-based-pharmacokinetic-model-of-fenofibrate-for-explaining-increased-drug-absorption-after-food-consumption
#8
Hyun-Moon Back, Byungjeong Song, Sudeep Pradhan, Jung-Woo Chae, Nayoung Han, Wonku Kang, Min Jung Chang, Jiao Zheng, Kwang-Il Kwon, Mats O Karlsson, Hwi-Yeol Yun
BACKGROUND: Oral administration of drugs is convenient and shows good compliance but it can be affected by many factors in the gastrointestinal (GI) system. Consumption of food is one of the major factors affecting the GI system and consequently the absorption of drugs. The aim of this study was to develop a mechanistic GI absorption model for explaining the effect of food on fenofibrate pharmacokinetics (PK), focusing on the food type and calorie content. METHODS: Clinical data from a fenofibrate PK study involving three different conditions (fasting, standard meals and high-fat meals) were used...
January 25, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29365992/effects-of-free-omega-3-carboxylic-acids-and-fenofibrate-on-liver-steatosis-and-serum-lipoproteins-in-overweight-patients-with-hypertriglyceridemia-and-non-alcoholic-fatty-liver-disease-nafld
#9
Lars Lind, Kristina Önnerhag, Ulf Riserus, Mats Kvarnström, Lars Johansson, Per-Anders Jansson, Linda Moris, Peter Nilsson, Jan W Eriksson, Jan Oscarsson
No abstract text is available yet for this article.
August 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29365930/effect-of-fenofibrate-on-renal-function-related-parameters-and-reversibility
#10
Chee Jeong Kim, Myung-A Kim
No abstract text is available yet for this article.
August 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29345261/an-inert-3d-emulsification-device-for-individual-precipitation-and-concentration-of-amorphous-drug-nanoparticles
#11
T Lorenz, S Bojko, H Bunjes, A Dietzel
Nanosizing increases the specific surface of drug particles, leading to faster dissolution inside the organism and improving the bioavailability of poorly water-soluble drugs. A novel approach for the preparation of drug nanoparticles in water using chemically inert microfluidic emulsification devices is presented in this paper. A lithographic fabrication sequence was established, allowing fabrication of intersecting and coaxial channels of different depths in glass as is required for 3D flow-focusing. Fenofibrate was used as a model for active pharmaceutical ingredients with very low water solubility in the experiments...
January 18, 2018: Lab on a Chip
https://www.readbyqxmd.com/read/29321376/retinal-de-novo-lipogenesis-coordinates-neurotrophic-signaling-to-maintain-vision
#12
Rithwick Rajagopal, Sheng Zhang, Xiaochao Wei, Teresa Doggett, Sangeeta Adak, Jennifer Enright, Vaishali Shah, Guoyu Ling, Shiming Chen, Jun Yoshino, Fong-Fu Hsu, Clay F Semenkovich
Membrane lipid composition is central to the highly specialized functions of neurological tissues. In the retina, abnormal lipid metabolism causes severe forms of blindness, often through poorly understood neuronal cell death. Here, we demonstrate that deleting the de novo lipogenic enzyme fatty acid synthase (FAS) from the neural retina, but not the vascular retina, results in progressive neurodegeneration and blindness with a temporal pattern resembling rodent models of retinitis pigmentosa. Blindness was not rescued by protection from light-evoked activity; by eating a diet enriched in palmitate, the product of the FAS reaction; or by treatment with the PPARα agonist fenofibrate...
January 11, 2018: JCI Insight
https://www.readbyqxmd.com/read/29313565/utilization-of-the-lipid-lowering-therapies-in-outpatient-settings-in-poland-epidemiological-survey-economedica-dyslipidemia-2015
#13
Filip M Szymański, Anna E Płatek, Anna Ryś, Karolina Semczuk-Kaczmarek, Bartosz Krzowski, Katarzyna Wróbel, Krzysztof J Filipiak
BACKGROUND: Dyslipidemia, especially elevated low-density lipoprotein (LDL) cholesterol is one of the most important cardiovascular risk factors. Treatment of dyslipidemia and prevention of cardiovascular disease with lipid-lowering drugs is one of the key issues in reducing cardiovascular mortality. Nevertheless, underutilization of statins and lipid-lowering drugs is still a problem globally. AIM: The present study aimed to describe the utilization of lipid-lowering drugs in groups of patients with indications for statin treatment and elevated LDL cholesterol...
January 9, 2018: Kardiologia Polska
https://www.readbyqxmd.com/read/29311302/fenofibrate-prevents-skeletal-muscle-loss-in-mice-with-lung-cancer
#14
Marcus D Goncalves, Seo-Kyoung Hwang, Chantal Pauli, Charles J Murphy, Zhe Cheng, Benjamin D Hopkins, David Wu, Ryan M Loughran, Brooke M Emerling, Guoan Zhang, Douglas T Fearon, Lewis C Cantley
The cancer anorexia cachexia syndrome is a systemic metabolic disorder characterized by the catabolism of stored nutrients in skeletal muscle and adipose tissue that is particularly prevalent in nonsmall cell lung cancer (NSCLC). Loss of skeletal muscle results in functional impairments and increased mortality. The aim of the present study was to characterize the changes in systemic metabolism in a genetically engineered mouse model of NSCLC. We show that a portion of these animals develop loss of skeletal muscle, loss of adipose tissue, and increased inflammatory markers mirroring the human cachexia syndrome...
January 8, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29305864/fenofibrate-inhibits-mtor-p70s6k-signaling-and-simultaneously-induces-cell-death-in-human-prostate-cancer-cells
#15
Xin Lian, Junlian Gu, Baoshan Gao, Yan Li, Chendil Damodaran, Wei Wei, Yaowen Fu, Lu Cai
Fenofibrate is the most widely used lipid-lowering drug, but it seems to have anti-tumor effects in several tumor cell lines. However, there are only a few reports on its effects on human prostate cancer cells. Thus, we investigated the anti-proliferative effects of fenofibrate on human prostate cancer cells and potential mechanisms. The methods used include cell viability analysis with an MTT assay, as well as apoptosis and related signaling pathway analyses with flow cytometry and Western blotting. Fenofibrate inhibited PC-3 cell growth in dose- and time-dependent manners...
January 3, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29290096/protective-effect-of-fenofibrate-against-ischemia-reperfusion-induced-cardiac-arrhythmias-in-isolated-rat-hearts
#16
Ishfaq A Bukhari, Abdulrahman A Almotrefi, Osama Y Mohamed, Abeer A Al-Masri, Saeed Ahmed Sheikh
Fenofibrate is a peroxisome proliferator-activated receptor (PPAR)-α activator that lowers triglycerides and influences cytochrome P-450 (CYP-450) epoxygenase dependent arachidonic acid (AA) metabolism. CYP-450 epoxygenase metabolizes AA to epoxyeicosatrienoic acids (EETs). EETs have coronary dilating, cardiac and renal protective properties. Fibrates possess similar properties due to their CYP-450 epoxygenase inducing properties that leads to increase in endogenous EETs production. In the current investigations fenofibrate (100 mg/kg, orally) for two weeks decreased ischemia/reperfusion (I/R)-induced premature ventricular contractions (PVCs), ventricular tachycardia (VT) and ventricular fibrillation (VF) in the isolated rat hearts...
December 31, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29288381/modulation-of-the-il-23-il-17-axis-by-fenofibrate-ameliorates-the-ovalbumin-lipopolysaccharide-induced-airway-inflammation-and-bronchial-asthma-in-rats
#17
Samah M Elaidy, Soha S Essawy, Mona A Hussain, Mohamed K El-Kherbetawy, Eman R Hamed
The overlapping between asthmatic subtypes, including both CD4+ T helper (TH)2 and TH17 cells, is found in the natural course of allergic asthma, especially in exacerbations and severe and insensitive forms to steroids, which are in need of new molecular therapies. In the TH2-subset mediated asthma, fenofibrate displays therapeutic promises, besides evidenced therapeutic effects on TH17-mediated colitis and myocarditis. Therefore, the effects of fenofibrate versus dexamethasone on IL-23/IL-17 axis in ovalbumin (OVA)/lipopolysaccharide (LPS)-induced airway inflammation and bronchial asthma in rats were explored...
December 30, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29287198/upregulation-of-peroxisome-proliferator-activated-receptor-alpha-by-fenofibrate-in-induced-testicular-ischemia-reperfusion
#18
Marwa M M Refaie
Torsion of the spermatic cord is a common urological emergency among infants and adolescents that can lead to testicular necrosis and infertility. We investigated the effect of fenofibrate (FEN) on induced testicular ischemia reperfusion (testicular (I-R). FEN (100, 300 mg/kg/day) was administered orally in presence or absence of testicular (I-R). We measured testicular weight changes and serum testosterone level. In addition; Testicular tissue reduced glutathione (GSH), malondialdehyde (MDA), total nitrites (NOx) and superoxide dismutase (SOD) activity were measured...
December 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29284388/fenofibrate-and-telmisartan-in-the-management-of-abdominal-aortic-aneurysm
#19
Sophie E Rowbotham, Smriti M Krishna, Corey S Moran, Jonathan Golledge
Objective This mini-review provides the rationale and updated progress for ongoing randomized controlled trials assessing fenofibrate and telmisartan efficacy to limit abdominal aortic aneurysm (AAA) growth. Methods / Results Data from preclinical and human studies investigating the efficacy of fenofibrate and telmisartan to limit AAA growth is presented and provides the rationale for three current randomized controlled trials assessing these medications as potential interventions to limit aneurysm growth in AAA patients...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29283132/efficiency-of-fenofibrate-in-facilitating-the-reduction-of-central-macular-thickness-in-diabetic-macular-edema
#20
Srilakshmi Srinivasan, Prathibha Hande, Jyoti Shetty, Sindhu Murali
PURPOSE: The purpose of this study is to study the benefit of addition of oral fenofibrate to the current regimen of diabetic macular edema (DME) management and quantify its effect on macular thickness and visual function in DME. METHODS: Fifty-three eyes of 50 patients were randomized into treatment (Group A) (oral fenofibrate 160 mg/day) and control groups (Group B). Both groups underwent treatment of DME as per the standard treatment protocol of our hospital including intravitreal injections (anti-vascular endothelial growth factor/steroid) and grid laser...
January 2018: Indian Journal of Ophthalmology
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