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Yosefifard Masoomeh - - 2014
BackgroundIn this study, neostigmine-loaded electrospun nanofibers were prepared and then their efficacy and duration of analgesic action were studied after epidural administration in rats by repeated tail flick and formalin tests.MethodsThe neostigmine poly vinyl alcohol (PVA) nanofibers were fabricated by electrospinning methods. The nanofibers (1 mg) were injected into the lumbar ...
Li Xiangqian X *Department of Orthopaedic Surgery, Zhongshan Hospital †State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Advanced Materials Laboratory, Fudan University, Shanghai, - - 2014
Experimental animal study. The authors conducted a study to determine the efficacy and safety of the PLGA-PEG-PLGA thermogel to prevent peridural fibrosis in an adult rat laminectomy model. Peridural fibrosis often occurs after spinal laminectomy. It might cause persistent back and/or leg pain postoperatively and make a reoperation more difficult ...
Chen Feng - - 2014
Epidural fibrosis (EF) is a common complication after laminectomy. Salvianolic acid B (Sal B) is a major bioactive component of a traditional Chinese medical agent, Salvia miltiorrhiza, which has shown anti-inflammatory, anti-fibrotic and anti-proliferative properties. The object of this study was to investigate the effect of Sal B on the ...
Al-Olama Mohamed M Institute of Biomedicine, Sahlgrenska Academy, University of Gothenburg, P.O.B. 440, 405 30, Göteborg, - - 2014
AF-16 is a 16-amino-acid-long peptide derived from the amino-terminal part of the endogenous protein, antisecretory factor (AF). AF-16 in vivo has been shown to regulate dysfunctions in the water and ion transport system under various pathological conditions and also to counteract experimentally increased tissue pressure. Rats were subjected to a ...
Mezzapesa Anna - - 2014
BackgroundPlasminogen activation is a ubiquitous source of fibrinolytic and proteolytic activity. Besides its role in prevention of thrombosis, plasminogen is involved in inflammatory reactions in the central nervous system. Plasminogen has been detected in the cerebrospinal fluid (CSF) of patients with inflammatory diseases; however, its origin remains controversial, as the ...
Zhang Kun K Department of Orthopedic Trauma and Hand Surgery, The First Affiliated Hospital of Guangxi Medical University, Nanning, 530021, Guangxi Zhuang Autonomous Region, - - 2014
The object of this study was to investigate the effects of licofelone on the prevention of epidural fibrosis (EF) formation in post-laminectomy rat models. A controlled double-blinded study was conducted in sixty, healthy adult Wistar rats that underwent laminectomy at the L1-L2 vertebrae levels. All the rats were divided randomly ...
Maerckx Cédric C Cédric Maerckx, Tatiana Tondreau, Silvia Berardis, Mustapha Najimi, Etienne Sokal, Laboratory of Pediatric Hepatology and Cell Therapy, Université Catholique de Louvain - Institut de Recherche Expérimentale et Clinique (IRCE), 1200 Brussels, - - 2014
To test the ability of adult-derived human liver stem/progenitor cells (ADHLSC) from large scale cultures to conjugate bilirubin in vitro and in bilirubin conjugation deficient rat. ADHLSC from large scale cultures were tested for their phenotype and for their capacity to conjugate bilirubin in vitro after hepatogenic differentiation. In vivo, ...
Moss Lee L Department of Preclinical Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park , NC , USA - - 2014
Abstract 1.  Plasma clearance of dolutegravir, an unboosted HIV-1 integrase inhibitor, was low in rat and monkey (0.23 and 2.12 mL/min/kg, respectively) as was the volume of distribution (0.1 and 0.28 L/kg, respectively) with terminal elimination half-life approximately 6 h. Dolutegravir was rapidly absorbed from oral solution with a high bioavailability in rat ...
Hubbard Dallin D Utah Center for Nanomedicine, Nano Institute of Utah, ‡Department of Bioengineering, and §Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah , 36 S. Wasatch Blvd., Salt Lake City, Utah 84112, United - - 2014
Oral delivery remains a challenge for poorly permeable hydrophilic macromolecules. Poly(amido amine) (PAMAM) dendrimers have shown potential for their possible oral delivery. Transepithelial transport of carboxyl-terminated G3.5 and amine-terminated G4 PAMAM dendrimers was assessed using isolated rat jejunal mucosae mounted in Ussing chambers. The 1 mM FITC-labeled dendrimers were added ...
Takubo Hiroaki H Drug Metabolism and Pharmacokinetics Research Laboratories, Central Pharmaceutical Research Institute, Japan Tobacco Inc. , Osaka , Japan - - 2014
Abstract 1. The pharmacokinetics and metabolism of dalcetrapib (JTT-705/RO4607381), a novel cholesteryl ester transfer protein inhibitor, were investigated in rats and monkeys. 2. In in vitro stability studies, dalcetrapib was extremely unstable in plasma, liver S9 and small intestinal mucosa, and the pharmacologically active form (dalcetrapib thiol) was detected as major component. ...
Lu Yang Y Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, Jiangsu, China; Division of Pharmacotherapy and Experimental Therapeutics, Eshelman School of Pharmacy, the University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, - - 2014
Liquorice is a commonly prescribed herb in traditional Chinese medicine with the primary constituent, glycyrrhetinic acid (GA) responsible for the toxic effects arising from its chronic consumption. Hepatic transformation and biliary excretion of GA are significant and well-documented pharmacokinetic pathways in humans, while glucuronide conjugates are the major identified metabolites. ...
Wu Wenjin W State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Av. Padre Tomás Pereira Taipa, Macao, - - 2014
Anthraquinones naturally distribute in many plants including rhubarb and have widespread applications throughout industry and medicine. Recent studies provided new insights in potential applications of these traditional laxative constituents. Glucuronidation was the main metabolic pathway of rhubarb anthraquinones in vivo. This study examined the activity and regioselectivity of glucuronidation of ...
Zielińska-Dawidziak Magdalena M Department of Food Biochemistry and Analysis, Poznań University of Life Sciences, Mazowiecka 48, 60-623, Poznań, Poland, - - 2014
An isolate of lead-ferritin obtained from soybean seeds sprouted in 25 mM of PbNO3 was introduced into the diet of both iron-deficient and iron non-deficient male rats. After a 21-day administration period, statistical differences in the lead accumulation in the femurs of the rats were noted. Iron-deficient rats accumulated more than ...
Dinan Nahid Mobarghei NM Department of Pharmaceutics, Faculty of Pharmacy, Teheran University of Medical Sciences, Teheran, - - 2014
The objective of this study was to use the functionalized multi-wall carbon nanotubes (CNTs) for the delivery of doxorubicin (DOX). Polyethylene glycol (PEG) chains are attached to CNTs then folate-conjugation of PEGylated CNTs was prepared. The amount of drug loading was calculated by the Multivariate Calibration Method for simultaneous quantification ...
Sadhukhan Sushabhan S Department of Chemistry, Case Western Reserve University, 10900 Euclid Avenue, Cleveland, OH 44106, United - - 2014
The major route for elimination of 4-hydroxy-2-(E)-nonenal (4-HNE) has long been considered to be through glutathionylation and eventual excretion as a mercapturic acid conjugate. To better quantitate the glutathionylation process, we developed a sensitive LC-MS/MS method for the detection of glutathione (GSH) conjugates of 4-hydroxy-2-(E)-alkenal enantiomers having carbon skeleton of ...
Wang Chun-Li CL School of Pharmacy, College of Pharmacy, Taipei Medical University, No. 250, Wu-Hsing Street, Taipei 110, - - 2014
TW01003, a piperazinedione derivative designed as an antimitotic agent, exhibited potent anticancer and antiangiogenesis activities in mice. However, oral administration of this compound in rats led to poor systemic bioavailability which suggested that in vivo efficacy might come from its metabolites. This report describes the identification of TW01003 metabolites in ...
Omar Khaled - - 2013
Abstract 1. The metabolism of ferulic acid (FA) has been studied in a number of different systems and several metabolites of FA have been characterised. No previous work has been carried out using hepatocytes to characterise the metabolism of FA. 2. A metabolomics approach in combination with high resolution mass spectrometry was ...
Cona Marlein Miranda - - 2013
We sought to reduce the radioactive intestinal waste after intravenous injection of necrosis avid iodine-131-labeled hypericin in dual-targeting anticancer radiotherapy and to study its pharmacokinetics in rats using a newly designed catheter. Iodine-123-labeled hypericin was prepared with iodogen as oxidant and characterized by high-performance liquid chromatography and mass spectrometry. After ...
Land Michael F - - 2013
A recent study using two head-mounted cameras has found that, in freely moving rats, eye movements are usually not conjugate, precluding stereopsis, but they maintain a wide region of binocular overlap above the head, presumably to detect flying predators.
Tomiya Noboru - - 2013
We have synthesized poly-γ-glutamic acid (PGA) modified with a synthetic trivalent glyco-ligand (TriGalNAc) for the hepatocyte asialoglycoprotein receptor (ASGP-R). We investigated in vivo distribution of unmodified PGA and TriGalNAc-modified PGA (TriGalNAc-PGA) in mice after intravenous injection. Most of unmodified PGA administered was transported to the bladder over 20-80min, suggesting a ...
Erve John C L - - 2013
Sitaxentan is a selective endothelin-A receptor antagonist that was marketed as Thelin in several European countries and Canada for pulmonary arterial hypertension. Sitaxentan was undergoing further clinical trials in the United States but due to four deaths and one case of liver transplantation from severe liver toxicity that appeared to ...
Kim Juhyun - - 2013
Abstract 1. GTx-024, a novel selective androgen receptor modulator, is currently being investigated as an oral treatment for muscle wasting disorders associated with cancer and other chronic conditions. 2. Absorption of GTx-024 was rapid and complete, with high oral bioavailability. A wide tissue distribution of [(14)C]GTx-024 derived radioactivity was observed. ...
Yang Xiaoxia - - 2013
Bisphenol A (BPA) has received considerable attention throughout the last decade due to its widespread use in consumer products. For the first time a physiologically based pharmacokinetic (PBPK) model was developed in neonatal and adult rats to quantitatively evaluate age-dependent pharmacokinetics of BPA and its phase II metabolites. The PBPK ...
Fonseca Nayanna Brunna da Silva - - 2013
Gossypol is a highly reactive compound present in cotton (Gossypium spp.). The aim of this work was to determine whether the administration of gossypol conjugated to albumin can immunize rats and thereby prevent the acute hepatotoxicity associated with gossypol. The first experiment consisted of administering the immunogen gossypol-BSA, with or ...
Révész Katalin - - 2012
Morphine is converted to morphine 3-β-D-glucuronide (M3G) by the UDP-glucuronosyltransferase Ugt2b1 in the endoplasmic reticulum (ER) of rat liver. Because of its luminal localization, UGT activity requires UDP-glucuronate import and glucuronide export across the ER membrane. The former transport is generally considered to be rate limiting and to explain the ...
Tozlovanu Mariana - - 2012
Abstract In the present study the photoreactivity of the fungal carcinogen ochratoxin A (OTA) has been utilised to generate authentic samples of reduced glutathione (GSH) and N-acetylcysteine (NAC) conjugates of the parent toxin. These conjugates, along with the nontoxic OTα, which is generated through hydrolysis of the amide bond of ...
Elfarra Adnan A AA Department of Comparative Biosciences and the Molecular and Environmental Toxicology Center, University of Wisconsin-Madison, Madison, WI 53706, USA. - - 2012
1,3-Butadiene (BD) is an air pollutant whose toxicity and carcinogenicity have been considered primarily mediated by its reactive metabolites, 3,4-epoxy-1-butene and 1,2,3,4-diepoxybutane, formed in liver and extrahepatic tissues by cytochromes P450s. A possible alternative metabolic pathway in bone marrow and immune cells is the conversion of BD to the chlorinated ...
Rosales Ruben - - 2012
Small organic molecules are believed to freely diffuse across nuclear pores but this may not be so if this route is blocked during protein and nucleic acid transfer. Here we have investigated the existence of transport mechanisms across the nuclear envelope (NE) of hepatocytes. Using nuclei isolated from rat liver ...
Jia Z Q - - 2012
Several studies have documented cardiovascular effects of apelin, including enhanced inotropy and vasodilation. However, these cardiovascular effects are short lived due to the predicted short circulating half-life of the apelin peptide. To address this limitation of apelin, we pursued N-terminal PEGylation of apelin and examined the cardiovascular effects of the ...
Yuan Jintao - - 2012
The quantitative structure-activity relationship (QSAR) of N-nitroso compounds (NOCs) for rat liver was developed by a topological sub-structural molecular-descriptors (TOPS-MODE) approach to predict non-liver-carcinogenic and liver-carcinogenic N-nitroso compounds based on a data set of 108 NOCs. Three descriptors calculated solely from the molecular structures of the compounds were selected by ...
Acimovic Jure - - 2012
Ubiquinone (Q) is a product in the cholesterol synthesis pathway and is an essential component of the respiratory chain in the mitochondrial membrane. In addition, extra-mitochondrial Q has anti-oxidative properties and this fraction is increased during carcinogenesis. The aim of the present study was to investigate if extra-mitochondrial level of ...
McDaniel L Patrice - - 2012
Aristolochic acid (AA) is a potent human nephrotoxin and carcinogen. We previously reported that AA treatment resulted in DNA damage and mutation in the kidney and liver of rats. In this study, we have determined the DNA adducts and mutations induced by AA in rat spleen. Big Blue® transgenic rats ...
Doktorova Tatyana Y - - 2012
At present, substantial efforts are focused on the development of in vitro assays coupled with "omics" technologies for the identification of carcinogenic substances as an alternative to the classical 2-year rodent carcinogenicity bioassay. A prerequisite for the eventual regulatory acceptance of such assays, however, is the in vivo relevance of ...
Akman Steven A - - 2012
Ochratoxin A (OTA) is a mycotoxin that enhances renal tumor formation in the outer medulla of male rat kidney. Direct DNA damage and subsequent mutagenicity may contribute to these processes. In this study we have determined whether OTA in the absence or presence of activated rat liver microsomes (RLM) or ...
Piccirillo Vincent J - - 2012
Inhalation bioassays in mice and rats exposed to naphthalene (NA) show incidences of lung and nasal cancer, respectively. This paper describes a preliminary mode of action (MOA)/human relevance (HR) framework for NA. Species differences in both carcinogenic and cytotoxic responses between the rodent and human have been noted based on ...
Watanabe Atsushi - - 2012
Teriparatide, a therapeutic agent for osteoporosis, has been reported to increase the incidences of bone neoplasms such as osteosarcoma when administered subcutaneously to Fischer 344 (F344) rats for a long term, but its non-carcinogenic dose level following 2-year daily administration has not been established. Here we report detailed studies on ...
Esteves-Pedro Natália Mencacci - - 2012
Dipteryx alata Vogel popularly known as "baru" is an important commercial leguminous tree species from the Brazilian Cerrado, which possess medicinal properties, besides its fruits consumption by animals and humans. The use of the "naturally occurring plants" as herbal remedies and foods mainly from leaves, seeds, flowers and roots of ...
Punvittayagul Charatda - - 2012
Pinocembrin (5, 7-dihydroxyflavanone) is a flavanone extracted from the rhizome of Boesenbergia pandurata. Our previous studies demonstrated that pinocembrin had no toxicity or mutagenicity in rats. We here evaluated its effects on the initiation and promotion stages in diethylnitrosamine-induced rat hepatocarcinogenesis, using short- and medium-term carcinogenicity tests. Micronucleated hepatocytes and ...
Peartree Natalie A NA Department of Psychology, Arizona State University, P.O. Box 871104, Tempe, AZ 85287-1104, - - 2012
Adolescence is a period of enhanced sensitivity to social influences and vulnerability to drug abuse. Social reward in adolescent rats has been demonstrated with the conditioned place preference (CPP) model, but it is not clear whether limited contact with another rat without play is sufficient to produce reward. We investigated ...
Dutech Alain - - 2011
Goal-directed action involves a representation of action consequences. Adapting to changes in action-outcome contingency requires the prefrontal region. Indeed, rats with lesions of the medial prefrontal cortex do not adapt their free operant response when food delivery becomes unrelated to lever-pressing. The present study explores the bases of this deficit ...
Meerts Sarah H - - 2011
The present study examined the interaction between the regulation of paced mating behavior by the medial preoptic area (mPOA) and by the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) pathway, as modulated by zaprinast, a phosphodiesterase inhibitor. Rats receiving mPOA or sham lesions were tested for paced mating behavior. Subsequently, rats ...
Ahad Abdul - - 2011
Context: The greatest obstacle for transdermal delivery is the barrier property of the stratum corneum. Many approaches have been employed to breach the skin barrier; the most widely used one is that of chemical penetration enhancers. Of the penetration enhancers, terpenes are arguably the most highly advanced and proven category. ...
Minematsu Takeo - - 2011
BACKGROUND: Skin maceration is recognized as a risk factor for the development of certain skin lesions. In health care settings, incontinence-associated skin maceration is highly prevalent in the elderly. However, the effect of senescence on maceration has not been fully elucidated. OBJECTIVE: To reveal the enhancement of the maceration-induced ultrastructural ...
Xu Jiegou - - 2011
Titanium dioxide (TiO(2)) is used in sunscreens and cosmetics as an ultraviolet light screen. TiO(2) has carcinogenic activity in the rat lung, but its effect on the skin has not been reported. We examined the promoting/carcinogenic effect of nano-size TiO(2) particles using a two-stage skin model. c-Ha-ras proto-oncogene transgenic (Hras128) ...
Shinkai Norihiro - - 2011
The study was performed to evaluate percutaneous penetration of ketoprofen after transdermal administration using a microdialysis technique in pigs, in comparison to rats. Ketoprofen release from patches was determined by analysis of the remaining drug content after application to hairless rats and pigs. Skin and knee joint penetration of ketoprofen ...
Ahad Abdul - - 2011
The purpose of this study was to investigate the effectiveness and mechanism(s) of percutaneous absorption of propranolol hydrochloride (PHCL) across rat and human cadaver skin using seven novel terpenes with reference to marker terpene 1,8-cineole. In-vitro skin permeation studies were carried out via rat and human skin models. The mechanism ...
Yan Hui - - 2011
HPLC analysis proved that coptis chinensis polysaccharides contained Ara, Man, and Gal. The monosaccharide constituents of phellodendron amurense polysaccharides were determined by HPLC analysis. HPLC analysis proved that phellodendron amurense polysaccharides contained Ara, Xyl, Glu, and Gal. FT-IR spectrum of coptis chinensis polysaccharides and phellodendron amurense polysaccharides showed the characteristic ...
Ito Yukako - - 2011
Two-layered dissolving microneedles of which acral portion contained leuprolide acetate (LA) as solid dispersion were prepared with sodium chondroitin sulfate as the base and the systemic absorption efficiency of LA was studied in rats after administration to their abdominal skin. A patch contained 100 dissolving microneedles of which length and ...
Kuramoto Takashi T Institute of Laboratory Animals, Graduate School of Medicine, Kyoto University, Sakyo-ku, Kyoto 606-8501, - - 2011
N-ethyl-N-nitrosourea (ENU) mutagenesis is an important tool for studying gene function and establishing human disease models. Here, we report the characterization of a novel hairless mutant rat strain that carries a recessive mutation called Kyoto rhino (krh), which was created by ENU-mutagenesis. We produced a F344-krh strain through inbreeding without ...
Ross John H - - 2011
The objective of this study was to develop an estimate of the percent dermal absorption of permethrin in humans to provide more accurate estimates of potential systemically absorbed dose associated with dermal exposure scenarios. Piperonyl butoxide (PBO) was used as a reference compound. The human percutaneous absorption estimate was based ...
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