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Mazhar Hussian, Abdul Qudoos Arain, Sadia Chiragh
OBJECTIVE: To evaluate the anti-dyslipidaemic effects of pioglitazone in diet-induced non-diabetic hyperlipidaemic rats and to compare them with gemfibrozil. METHODS: This comparative animal study was conducted at the Postgraduate Medical Institute, Lahore, Pakistan, from July to September 2011, and comprised Sprague Dawley albino rats divided into three equal groups. Initially all three groups were given high-lipid diet containing cholesterol 1.5g, coconut oil 8ml and sodium cholate 1...
October 2016: JPMA. the Journal of the Pakistan Medical Association
Mutsuko Hirata-Koizumi, Ryota Ise, Hirohito Kato, Takashi Matsuyama, Tomoko Nishimaki-Mogami, Mika Takahashi, Atsushi Ono, Makoto Ema, Akihiko Hirose
2-(2'-Hydroxy-3',5'-di-tert-butylphenyl)benzotriazole (HDBB), the Benzotriazole UV-stabilizer (BUVSs) known as UV-320, is widely used in plastic materials for protection against UV-irradiation. Previously, we reported that oral ingestion of HDBB induce hepatotoxicity including hepatocyte hypertrophy and necrosis in rats and, males was more susceptible compared with females in young rats while no sex-related difference was observed in preweaning rats. Phenotypes observed in our previous study imply involvement of peroxisome proliferator-activated receptor (PPAR) α in HDBB hepatotoxicity, however, direct evidence that HDBB can activate PPARα has not been provided and the mechanism which underlying the gender difference of HDBB hepatotoxicity was not clearly elucidated...
2016: Journal of Toxicological Sciences
M V Varma, E Kimoto, R Scialis, Y Bi, J Lin, H Eng, A S Kalgutkar, A F El-Kattan, A D Rodrigues, L M Tremaine
Montelukast, a leukotriene receptor antagonist commonly prescribed for treatment of asthma, is primarily metabolized by Cytochrome P450 (CYP)2C8, and has been suggested as a probe substrate for investigating CYP2C8 activity in vivo. We evaluated the quantitative role of hepatic uptake transport in its pharmacokinetics and drug-drug interactions (DDIs). Montelukast was characterized with significant active uptake in human hepatocytes, and showed affinity towards organic anion transporting polypeptides (OATPs) in transfected cell systems...
September 20, 2016: Clinical Pharmacology and Therapeutics
I E Templeton, Y Chen, J Mao, J Lin, H Yu, S Peters, M Shebley, M V Varma
This subteam under the Drug Metabolism Leadership Group (Innovation and Quality Consortium) investigated the quantitative role of circulating inhibitory metabolites in drug-drug interactions using physiologically based pharmacokinetic (PBPK) modeling. Three drugs with major circulating inhibitory metabolites (amiodarone, gemfibrozil, and sertraline) were systematically evaluated in addition to the literature review of recent examples. The application of PBPK modeling in drug interactions by inhibitory parent-metabolite pairs is described and guidance on strategic application is provided...
September 19, 2016: CPT: Pharmacometrics & Systems Pharmacology
Nan Shu, Mengyue Hu, Zhaoli Ling, Peihua Liu, Fan Wang, Ping Xu, Zeyu Zhong, Binbin Sun, Mian Zhang, Feng Li, Qiushi Xie, Xiaodong Liu, Li Liu
Liver injury is a common adverse effect of atorvastatin. This study aimed to investigate atorvastatin-induced hepatotoxicity in diabetic rats induced by high-fat diet combined with streptozotocin. The results showed that 40 mg/kg atorvastatin was lethal to diabetic rats, whose mean survival time was 6.2 days. Severe liver injury also occurred in diabetic rats treated with 10 mg/kg and 20 mg/kg atorvastatin. The in vitro results indicated that atorvastatin cytotoxicity in hepatocytes of diabetic rats was more severe than normal and high-fat diet feeding rats...
2016: Scientific Reports
Ma Rosa Pino, Selene Muñiz, Jonatan Val, Enrique Navarro
Pharmaceuticals reach terrestrial environments through the application of treated wastewaters and biosolids to agricultural soils. We have investigated the toxicity of 15 common pharmaceuticals, classified as nonsteroidal anti-inflammatory drugs (NSAIDs), blood lipid-lowering agents, β-blockers and antibiotics, in two photosynthetic organisms. Twelve pharmaceuticals caused inhibitory effects on the radicle and hypocotyl elongation of Lactuca sativa seeds. The EC50 values obtained were in the range of 170-5656 mg L(-1) in the case of the radicle and 188-4558 mg L(-1) for the hypocotyl...
August 24, 2016: Environmental Science and Pollution Research International
Aleksi Tornio, Pertti J Neuvonen, Mikko Niemi, Janne T Backman
INTRODUCTION: Cytochrome P450 (CYP) 2C8 is a drug metabolizing enzyme of major importance. The lipid-lowering drug gemfibrozil has been identified as a strong inhibitor of CYP2C8 in vivo. This effect is due to mechanism-based inhibition of CYP2C8 by gemfibrozil 1-O-β-glucuronide. In vivo, gemfibrozil is a fairly selective CYP2C8 inhibitor, which lacks significant inhibitory effect on other CYP enzymes. Gemfibrozil can, however, have a smaller but clinically meaningful inhibitory effect on membrane transporters, such as organic anion transporting polypeptide 1B1 and organic anion transporter 3...
August 22, 2016: Expert Opinion on Drug Metabolism & Toxicology
Monika Wieczerzak, Błażej Kudłak, Galina Yotova, Miroslava Nedyalkova, Stefan Tsakovski, Vasil Simeonov, Jacek Namieśnik
The present study deals with assessment of ecotoxicological parameters of 9 drugs (diclofenac (sodium salt), oxytetracycline hydrochloride, fluoxetine hydrochloride, chloramphenicol, ketoprofen, progesterone, estrone, androstenedione and gemfibrozil), present in the environmental compartments at specific concentration levels, and their mutual combinations by couples against Microtox® and XenoScreen YES/YAS® bioassays. As the quantitative assessment of ecotoxicity of drug mixtures is an complex and sophisticated topic in the present study we have used two major approaches to gain specific information on the mutual impact of two separate drugs present in a mixture...
November 15, 2016: Science of the Total Environment
Renata Francik, Jadwiga Kryczyk, Sławomir Francik
Clofibric acid derivatives called fibrates, are quite commonly used lipid-lowering drugs, so it is necessary to know beneficial and adverse effects of these compounds on the body. The European Medicines Agency's Committee for Medicinal Products for Human Use (CHMP) has concluded that benefits of four fibrates such as: bezafibrate, ciprofibrate, fenofibrate and gemfibrozil continue outweigh their risk in treatment of people with blood lipid disorders. According to recommendations of the CHMP fibrates should not be used as first-line drugs, except in patients with severe hypertriglyceridemia and patients who cannot use statins...
May 2016: Acta Poloniae Pharmaceutica
M Teles, C Fierro-Castro, P Na-Phatthalung, A Tvarijonaviciute, A M V M Soares, L Tort, M Oliveira
The information on the potential hazardous effects of gemfibrozil (GEM) on marine fish is extremely scarce. In the current study, molecular, endocrine and biochemical parameters were assessed in Sparus aurata after 96h waterborne exposure to a GEM concentration range. Hepatic mRNA levels of target genes known to be regulated via peroxisome proliferator-activated receptor α (pparα) in mammals, such as apolipoprotein AI (apoa1) and lipoprotein (lpl) were significantly increased, without a concomitant activation of the ppar pathways...
November 15, 2016: Journal of Hazardous Materials
Yoshifumi Ashikawa, Yuhei Nishimura, Shiko Okabe, Shota Sasagawa, Soichiro Murakami, Mizuki Yuge, Koki Kawaguchi, Reiko Kawase, Toshio Tanaka
Oligodendrocytes are major myelin-producing cells and play essential roles in the function of a healthy nervous system. However, they are also one of the most vulnerable neural cell types in the central nervous system (CNS), and myelin abnormalities in the CNS are found in a wide variety of neurological disorders, including multiple sclerosis, adrenoleukodystrophy, and schizophrenia. There is an urgent need to identify small molecular weight compounds that can stimulate myelination. In this study, we performed comparative transcriptome analysis to identify pharmacodynamic effects common to miconazole and clobetasol, which have been shown to stimulate myelination by mouse oligodendrocyte progenitor cells (OPCs)...
2016: Frontiers in Pharmacology
Jose R Alvarez-Corena, John A Bergendahl, Fred L Hart
The extent and kinetics of degradation of 1,4 dioxane, n-nitrosodimethylamine (NDMA), tris-2-chloroethyl phosphate (TCEP), gemfibrozil, and 17β estradiol in a prepared aqueous matrix by means of UV/TiO2 (ultraviolet light/titanium dioxide) oxidation was evaluated. Degussa P25 TiO2 was employed as a photocatalyst excited by UV light in a 1 L water-jacketed batch photoreactor. The rate of degradation was modeled using a pseudo-first order rate model and the Langmuir-Hinshelwood rate model with a high correlation...
October 1, 2016: Journal of Environmental Management
Itamar A Shabtai, Yael G Mishael
Hybrid polycation-clay composites, based on methylated poly vinylpyridinium, were optimized as sorbents for secondary effluent organic matter (EfOM) including emerging micropollutants. Composite structure was tuned by solution ionic strength and characterized by zeta potential, FTIR, X-ray diffraction, and thermal gravimetric analyses. An increase in ionic strength induced a transition from a train to a loops and tails configuration, accompanied by greater polycation adsorption. Composite charge reversal (zeta potential -18 to 45 mV) increased the adsorption of EfOM and humic acid (HA), moderately and sharply, respectively, suggesting electrostatic and also nonspecific interactions with EfOM...
August 2, 2016: Environmental Science & Technology
Richard Bade, Ana Causanilles, Erik Emke, Lubertus Bijlsma, Juan V Sancho, Felix Hernandez, Pim de Voogt
A screening approach was applied to influent and effluent wastewater samples. After injection in a LC-LTQ-Orbitrap, data analysis was performed using two deconvolution tools, MsXelerator (modules MPeaks and MS Compare) and Sieve 2.1. The outputs were searched incorporating an in-house database of >200 pharmaceuticals and illicit drugs or ChemSpider. This hidden target screening approach led to the detection of numerous compounds including the illicit drug cocaine and its metabolite benzoylecgonine and the pharmaceuticals carbamazepine, gemfibrozil and losartan...
November 1, 2016: Science of the Total Environment
A V Dordio, S Miranda, J P Prates Ramalho, A J Palace Carvalho
Pharmaceutical residues presence in the environment is among nowadays top emergent environmental issues. For removal of such pollutants, adsorption is a generally efficient process that can be complementary to conventional treatment. Research of cheap, widely available adsorbents may make this process economically attractive. The aim of the present work was to evaluate the capacity of two clay materials (exfoliated vermiculite, LECA) to adsorb gemfibrozil, mefenamic acid and naproxen in lab-scale batch assays...
June 1, 2016: Journal of Hazardous Materials
Shubha Ananthakrishnan, George A Kaysen
Lipoprotein abnormalities such as low levels of high-density lipoprotein (HDL) and high triglycerides (TGs), associated with the metabolic syndrome, are also associated with subsequent decline in kidney function. Patients with end-stage kidney disease also exhibit low HDL and high TGs and a modest reduction in low-density lipoprotein (LDL), although the mechanisms responsible for these changes differ when patients with end-stage kidney disease are compared with those having metabolic syndrome with normal kidney function, as do lipoprotein structures...
July 2016: Advances in Chronic Kidney Disease
Amirhossein Sahebkar, Renato Giua, Claudio Pedone, Kausik K Ray, Antonio J Vallejo-Vaz, Luisa Costanzo
Flow-mediated dilation (FMD) of the brachial artery reflects endothelium-dependent vasodilator function; since it correlates with coronary endothelial function, its reduction could predict cardiovascular events. Several studies have investigated the potential impact of fibrates therapy on endothelial function, but clinical findings have not been fully consistent. We aimed to conduct a meta-analysis of randomized placebo-controlled trials in order to clarify whether fibrate therapy could improve endothelial function...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Mandu Inyang, Riley Flowers, Drew McAvoy, Eric Dickenson
The removal of trace organic compounds (TOrCs) and their biotransformation rates, kb (LgSS(-)(1)h(-)(1)) was investigated across different redox zones in a biological nutrient removal (BNR) system using an OECD batch test. Biodegradation kinetics of fourteen TOrCs with initial concentration of 1-36μgL(-)(1) in activated sludge were monitored over the course of 24h. Degradation kinetic behavior for the TOrCs fell into four groupings: Group 1 (atenolol) was biotransformed (0.018-0.22LgSS(-)(1)h(-)(1)) under anaerobic, anoxic, and aerobic conditions...
September 2016: Bioresource Technology
Yunting Xu, Dandan Zhou, Yedong Wang, Jiajun Li, Meiyu Wang, Jia Lu, Hongjian Zhang
CYP2C8 is involved in the metabolic clearance of several important drugs and recent reports have shown that acyl glucuronides of gemfibrozil and clopidogrel are potent time-dependent inhibitors of CYP2C8 activity. In the present study, the inhibitory effect of steviol acyl glucuronide (SVAG), a circulating metabolite formed after the ingestion of rebaudioside A, was investigated using in vitro and in vivo systems. Results indicated that SVAG was a reversible but not a time-dependent inhibitor of CYP2C8-mediated paclitaxel 6α-hydroxylation...
August 2016: Food and Chemical Toxicology
Massimiliano Sgroi, Paolo Roccaro, Gregory V Korshin, Valentina Greco, Sebastiano Sciuto, Tarun Anumol, Shane A Snyder, Federico G A Vagliasindi
This study investigated the applicability of different techniques for fluorescence excitation/emission matrices data interpretations, including peak-picking method, fluorescence regional integration and PARAFAC modelling, to act as surrogates in predicting emerging trace organic compounds (ETOrCs) removal during conventional wastewater treatments that usually comprise primary and secondary treatments. Results showed that fluorescence indexes developed using alternative methodologies but indicative of a same dissolved organic matter component resulted in similar predictions of the removal of the target compounds...
May 11, 2016: Journal of Hazardous Materials
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