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Pettit Marie W MW Faculty of Engineering and Science, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, - - 2014
An increasing human population requires a secure food supply and a cost effective, oral vaccine delivery system for livestock would help facilitate this end. Recombinant antigen adsorbed onto silica beads and coated with myristic acid, was released (∼15% (w/v)) over 24h at pH 8.8. At pH 2, the myristic acid ...
Tang Yan-Bo YB Beijing Key Laboratory of Active Substance Discovery & Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 1 Xiannongtan Street, Beijing 100050 - - 2014
Protein tyrosine phosphatase 1B (PTP1B) is a promising therapeutic target for type 2 diabetes. Herein, we report the evolution of a previously identified 3-phenylpropanoic acid-based PTP1B inhibitor to an orally active lead compound. A series of 3-phenylpropanoic acid-based PTP1B inhibitors were synthesized, and three of them, 3-(4-(9H-carbazol-9-yl)phenyl)-5-(3,5-di-tert-butyl-4-methoxyphenyl)-5-oxopentanoic acid (9), 3-(4-(9H-carbazol-9-yl)phenyl)-5-(4'-bromo-[1,1'-biphenyl]-4-yl)-5-oxopentanoic acid (10) ...
Morabito Rossana R Department of Human and Social Sciences, Via T. Cannizzaro 278, Messina, Italy. Electronic address: - - 2014
Nematocyst discharge and concomitant delivery of toxins is triggered to perform both defence and predation strategies in Cnidarians, and may lead to serious local and systemic reactions in humans. Pelagia noctiluca (Cnidaria, Scyphozoa) is a jellyfish particularly abundant in the Strait of Messina (Italy). After accidental contact with this jellyfish, ...
de Ferrars R M RM Department of Nutrition, Norwich Medical School, University of East Anglia, Norwich, NR4 7TJ, United - - 2014
Anthocyanins are phytochemicals with reported vasoactive bioactivity. However, given their instability at neutral pH, they are presumed to undergo significant degradation and subsequent biotransformation. The aim of the present study was to establish the pharmacokinetics of the metabolites of cyanidin-3-glucoside (C3G), a widely consumed dietary phytochemical with potential cardio-protective properties. ...
Nøhr Martha Kampp MK Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2100 Copenhagen, - - 2014
The anti-epileptic drug substance vigabatrin is used against infantile spasms. In vitro evidence suggests that vigabatrin is transported via the proton coupled amino acid transporter (PAT1). The aim of the present study was to investigate whether the intestinal absorption of vigabatrin in vivo was mediated via PAT1 in non-rodents. This ...
Stine Cynthia B CB Center for Veterinary Medicine, US Food and Drug Administration, 8401 Muirkirk Rd, Laurel, MD 20708, USA. Electronic address: - - 2014
The industrial chemical melamine was used in 2007 and 2008 to raise the apparent protein content in pet feed and watered down milk, respectively. Because humans may be exposed to melamine via several different routes into the human diet as well as deliberate contamination, this study was designed to characterize ...
Pitt William C WC Hawaii Field Station, National Wildlife Research Center, Wildlife Services, Animal and Plant Health Inspection Service, U.S. Department of Agriculture, P.O. Box 10880, Hilo, HI, 96721, USA, - - 2014
We examined potential exposure of Hawaiian hoary bats (Lasiurus cinereus semotus) to citric acid, a minimum risk pesticide registered for control of invasive Eleutherodactylus frog populations. Hoary bats are nocturnal insectivores that roost solitarily in foliage, federally listed as endangered, and are endemic to Hawaii. Oral ingestion during grooming of ...
Chevrot Michael M From Physiologie de la Nutrition et Toxicologie (MC, PP-D, DA, AB, MG, and PB) and Physiopathologie des Dyslipidémies (IR and BV), Unité Mixte de Recherche (UMR) U866, Institut National de la Santé et de Recherche Médicale (INSERM), Université de Bourgogne/AgroSup Dijon, Dijon, France; the Centre National de la Recherche Scientifique, UMR6265 (GE, MG, SI, and SN) and the Institut National de la Recherche Agronomique, UMR1324 Centre des Sciences du Goût et de l'Alimentation, Dijon, France (GE, MG, SI, and SN); and the Université de Bourgogne, UMR Centre des Sciences du Goût et de l'Alimentation, Dijon, France (GE, MG, SI, and - - 2014
The association between the orosensory detection of lipids, preference for fatty foods, and body mass index (BMI; in kg/m(2)) is controversial in humans. We explored the oral lipid-sensing system and the orosensory-induced autonomic reflex system in lean and obese subjects. Lean (BMI: 19 to <25; n = 30) and obese ...
Yu Xiaolan X Department of Biological Sciences, School of Dental Medicine, Case Western Reserve University, 10900 Euclid Avenue, Cleveland, Ohio 44106. - - 2014
Periodontal pathogens such as Porphyromonas gingivalis (Pg) and Fusobacterium nucleatum (Fn) produce five different short chain fatty acids (SCFAs) as metabolic by-products. We detect significantly higher levels of SCFAs in the saliva of patients with severe periodontal disease. The different SCFAs stimulate lytic gene expression of Kaposi's sarcoma-associated herpesvirus (KSHV) ...
Yun Dae-Woong DW Oral Biology Research Institute, Chosun University School of Dentistry, - - 2014
Compared to most normal cells that express L-type amino acid transporter 2, L-type amino acid transporter 1 is highly expressed in cancer cells and presumed to support their elevated growth and proliferation. This study examined JPH203, a potent and selective L-type amino acid transporter 1 inhibitor, and its ability to ...
Fazio Alejandra T - - 2014
A strain of the lichen mycobiont of Ramalina celastri, isolated from ascospores, was cultured axenically on two solid media containing high amounts of the carbon source: sucrose in MY10 and mannitol in BMRM. Usnic acid, the major cortical lichen metabolite, was produced by the colonies grown on MY10, with a ...
Khatun Zehedina Z Department of Green Bioengineering, Korea National University of Transportation, Chungju, 380-702 Republic of - - 2014
Oral delivery is the preferred route to deliver therapeutics via nanoparticles due to ease of administration and patient acceptance. Here, we report on the findings of the absorption pathway of taurocholic acid (TCA)-linked heparin and docetaxel (DTX) conjugate, which we refer to as HDTA. We studied the oral absorption of ...
Zhou Wei W College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, PR China; Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, PR - - 2014
The current study aims to investigate the pharmacokinetic study of eight caffeic acid derivatives (forsythoside A, isoforsythoside, forsythoside B, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, 3,5-dicaffeoylquinic acid and 3,4-dicaffeoylquinic acid) following oral administration of Flos Lonicerae-Fructus Forsythiae herb combination in rats. A rapid and sensitive ultra performance liquid chromatography-tandem mass ...
Chagas Pietro Maria PM Laboratório de Síntese, Reatividade e Avaliação Farmacológica e Toxicológica de Organocalcogênios, Universidade Federal de Santa Maria, CEP 97105-900, Santa Maria, RS, - - 2014
The present study evaluated the antinociceptive and anti-inflammatory effects of per oral (p.o.) administration of salicylic acid-derivative organoselenium compounds in chemical models of nociception in mice. The compounds (50mg/kg; p.o.) were administered 30 and 60min before the nociceptive behaviour and compared to the positive-control, acetylsalicylic acid (ASA; 200mg/kg; p.o.). In ...
Gama Ricardo Ribeiro RR Postgraduate Programme in Oncology, Universidade de São Paulo, São Paulo, SP, Brazil and Operative Technique and Experimental Surgery Laboratory, Faculdade Evangélica do Paraná, Alameda Augusto Stelfeld, 2134 Curitiba, PR 80730-150, - - 2014
To study the potential chemopreventive effects of polyunsaturated fatty acids omega-3 in Swiss mice submitted to oral and oesophageal carcinogenesis induction by 4-nitroquinoline-1-oxide (4-NQO). The animals underwent carcinogenesis induction with 50 µg/mL 4-NQO for eight weeks. The animals were divided into groups: Group I-4-NQO induction without chemoprevention, Group II-chemoprevention with ...
Büsing Kirsten K University of Rostock, Faculty of Agricultural and Environmental Sciences, Chair for Nutritional Physiology and Animal Nutrition, Justus-von-Liebig-Weg 8, 18059 Rostock, Germany. Electronic address: - - 2013
Humic acids are used to prophylactically treat intestinal diseases in a wide number of species, yet the mechanism of action remains unknown. The general assumption has been that humic acids act locally; however studies using young piglets show orally supplemented humic acids can penetrate the intestinal wall, and thus potentially ...
Yang Shyh-Ming SM Cardiovascular and Metabolism Research, Janssen Research and Development, LLC, Welsh & McKean Roads, Spring House, PA 19477, USA. Electronic address: - - 2013
Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1) inhibitors are described. In a chronic study of selected analog (3e) in Zucker fa/fa (ZF) rat, dose-dependent decrease of body weight gain and plasma fatty acid desaturation index (DI) in both C16 and C18 are ...
Kono Mitsunori M Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, 26-1, Muraokahigashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan. Electronic address: - - 2013
A series of piperazine ureas were designed, synthesized, and evaluated for their potential as novel orally efficacious fatty acid amide hydrolase (FAAH) inhibitors for the treatment of neuropathic and inflammatory pain. We carried out an optimization study of compound 5 to improve its in vitro FAAH inhibitory activity, and identified ...
Tsume Yasuhiro Y Department of Pharmaceutical Science, University of Michigan, Ann Arbor, Michigan 48109, - - 2013
Gemcitabine prodrugs with D- and L-configuration amino acids were synthesized and their chemical stability in buffers, resistance to glycosidic bond metabolism, enzymatic activation, permeability in Caco-2 cells and mouse intestinal membrane, anti-proliferation activity in cancer cell were determined and compared to that of parent drug, gemcitabine. Prodrugs containing D-configuration amino ...
Hsieh Chien-Ming - - 2013
A series of adipic acid dihydrazide (ADH)-modified hyaluronic acid (HA-ADH) compounds were synthesized and conjugated with QDots (QDots-HA conjugates) to assess the effects of the molecular weight (MW) and extent of chemical modification of HA on its biodistribution. Their physicochemical structures were confirmed by complementary application of GPC, H(1) NMR, ...
Agrawal Ashish Kumar - - 2013
The present study reports the folic acid (FA) functionalized insulin loaded stable liposomes with improved bioavailability following oral administration. Liposomes were stabilized by alternating coating of negatively charged polyacrylic acid (PAA) and positively charged poly (allyl amine) hydrochloride (PAH) over liposomes. Furthermore, folic acid was appended as targeting ligand by ...
Park Jin Woo - - 2013
Risedronate is widely used clinically to treat osteoporosis, Paget's disease, hypercalcemia, bone metastasis, and multiple myeloma. However, its oral efficacy is restricted due to its low bioavailability and severe gastrointestinal adverse effects. This study was designed to evaluate the effect of deoxycholic acid derivatives on the permeability and oral bioavailability ...
Fujii Yoshimine - - 2013
Poor oral absorption of a factor Xa inhibitor, DX-9065, is partly due to the interaction with bile acids in the gastrointestinal tract. The aim of this study is to improve the oral bioavailability of DX-9065 by cyclodextrins (CyDs) capable of interfering with such interaction. The abilities of the CyDs to ...
Wang Qian - - 2013
Boswellic acid is a plant-derived molecule with putative anti-inflammatory effects. This study was performed to determine whether oral or topical administration of boswellic acid can attenuate joint damage in a mouse model of osteoarthritis (OA). Levels of boswellic acid were measured in the blood and synovium of mice treated with ...
Marmet Cynthia - - 2013
Chlorogenic acids and derivatives like phenolic acids are potentially bioactive phenolics, which are commonly found in many foods. Once absorbed, chlorogenic and phenolic acids are highly metabolized by the intestine and the liver, producing glucuronidated and/or sulphated compounds. These metabolites were analyzed in human plasma using a validated liquid chromatography-electrospray ...
Leuratti Chiara - - 2013
Background/Aims: Absorption, biotransformation and elimination of safinamide, an enantiomeric α-aminoamide derivative developed as an add-on therapy for Parkinson's disease patients, were studied in healthy volunteers administered a single oral dose of 400 mg (14)C safinamide methanesulphonate, labelled in metabolically stable positions. Methods: Pharmacokinetics of the parent compound were investigated up ...
Loniewski Igor - - 2013
Kidney injury in chronic kidney disease (CKD) is likely multifactorial, but recent data support that a component is mediated by mechanisms used by the kidney to increase acidification in response to an acid challenge to systemic acid-base status. If so, systemic alkalization might attenuate this acid-induced component of kidney injury. ...
Gonzales Gustavo F - - 2013
Summary Context: Sacha Inchi (Plukenetia volubilis L.) is a potential oilseed crop because is rich in α-linolenic acid (ALA) (omega-3 fatty acid). Objective: To evaluate the exposure of fatty acids after a single oral administration of sacha inchi or sunflower oil in healthy volunteers. Material and Methods: Plasma fatty acids ...
Rozendaal Anna M - - 2013
Periconceptional folic acid has been associated with a reduced risk of neural tube defects, but findings on its effect in oral clefts are largely inconclusive. This case-control study assesses the effects of periconceptional folic acid on cleft risk, using complementary data from the Dutch Oral Cleft Registry and a population-based ...
Kawashima Junko - - 2013
Actinomyces are predominant oral bacteria; however, its cariogenic potential, such as acid production and fluoride sensitivity, has not been elucidated in details and compared with the other caries-associated oral bacteria, such as Streptococcus. Therefore, this study aimed to elucidate and compare the acid production and growth of Actinomyces and Streptococcus, ...
Zhou Wei - - 2013
Phenolic acids, the main active ingredients in Flos Lonicerae extract possess strong antibacterial, antioxidant and antiviral effects, and their contents was higher largely than that of other ingredients such as flavones, but the absolute bioavailability orally was significantly low, which is significant low influencing clinical efficacies of its oral preparations. ...
Saito T - - 2013
This study examined the negative effects of zoledronic acid on the re-epithelialization of oral mucosa in a three-dimensional in vitro oral mucosa wound healing model. A living oral mucosa equivalent was constructed by seeding a mixture of primary human oral keratinocytes and fibroblasts, at a cell density of 1.5×10(5)cm(2) each, ...
Lee Kyung Eun - - 2013
This study aims to investigate the feasibility of Levodopa transdermal delivery systems (TDSs). Levodopa TDSs were formulated using various vehicles and permeation enhancers, and in vitro permeation and in vivo pharmacokinetic studies were carried out. In the in vitro study, ester-type vehicles showed relatively high enhancing effects; propylene glycol monocaprylate ...
Gadaria-Rathod Neha - - 2013
Abstract Purpose: To evaluate pill counts and red blood cell (RBC) membrane fatty acid profiles as measures of compliance with oral omega3 polyunsaturated fatty acids (ω3 PUFAs) and to compare the two techniques. Methods: Sixteen dry eye disease subjects were given oral ω3 PUFA or placebo for 3 months. Compliance ...
Zhao Yanli - - 2013
Abstract The aim of the study is to synthesize a thiolated Pluronic copolymer, Pluronic-poly (acrylic acid)-cysteine copolymer, to construct a mixed micelle system with the Pluronic-poly (acrylic acid)-cysteine copolymer and Pluronic L121 (PL121) and to evaluate the potential of these mixed micelles as an oral drug delivery system for paclitaxel. ...
Hong Yong Rae - - 2013
A new series of PHD (HIF prolyl 4-hydroxylase) inhibitors was designed based on the X-ray co-crystal structure of FG-2216. Using a lead generation process, a series of [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives was developed as potent PHD2 inhibitors. This class of compounds also showed the ability to stabilize HIF-α, to stimulate EPO ...
Zhou Wei - - 2013
The current study aims to investigate the pharmacokinetic study of five phenolic acids (neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, 3,5-dicaffeoylquinic acid and 3,4-dicaffeoylquinic acid) following oral administration of Flos Lonicerae preparations in rats. A rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed to simultaneously determine ...
Wang Xiang-Yang - - 2013
A simple, sensitive and selective high-performance liquid chromatography electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method was developed for simultaneous determination and pharmacokinetic study of six active components, protocatechuic acid, chlorogenic acid, caffeic acid, ferulic acid rosmarinic acid and paeoniflorin in rat plasma after oral administration of Cerebralcare granule(®) for the ...
Reich Marco - - 2013
The first step of bioadhesion on dental surfaces is the formation of the acquired pellicle. This mainly acellular layer is formed instantaneously on all solid surfaces exposed to oral fluids. It is composed of proteins, glycoproteins and lipids. However, information on the lipid composition is sparse. The aim of the ...
Gao Li-Mei - - 2013
A series of novel N-substituted sophocarpinic acid derivatives was designed, synthesized, and evaluated for their anti-enteroviral activities against coxsackievirus type B3 (CVB3) and coxsackievirus type B6 (CVB6) in Vero cells. Structure-activity relationship analysis revealed that the introduction of a benzenesulfonyl moiety on the 12-nitrogen atom in (E)-β,γ-sophocarpinic acid might significantly enhance anti-CVB3 ...
Fischer Carol L CL Dows Institute for Dental Research, College of Dentistry, The University of Iowa, Iowa City, - - 2013
Oral mucosal and salivary lipids exhibit potent antimicrobial activity for a variety of Gram-positive and Gram-negative bacteria; however, little is known about their spectrum of antimicrobial activity or mechanisms of action against oral bacteria. In this study, we examine the activity of two fatty acids and three sphingoid bases against ...
Choi Jae-Suk - - 2013
The antibacterial activity of various saturated fatty acids (SFA) and unsaturated fatty acids (USFA) against different oral pathogens which are implicated in the cause of dental caries, stomatitis, gingivitis, and periodontitis was examined. The saturated fatty acids Pa, StA and ArA, and the unsaturated omega-7 fatty acids PLA and omega-9 ...
Kurniyati Kurni - - 2013
Neuraminidases (sialidases) catalyze the removal of terminal sialic acid from glycoconjugates. Bacterial pathogens often utilize neuraminidases to scavenge host sialic acid, which can be utilized either as a nutrient or as a decorating molecule to disguise themselves from host immune attacks. Herein, a putative neuraminidase (TDE0471) was identified in Treponema ...
Dehmlow Henrietta - - 2013
A series of non-steroidal GPBAR1 (TGR5) agonists was developed from a hit in a high-throughput screening campaign. Lead identification efforts produced biphenyl-4-carboxylic acid derivative (R)-22, which displayed a robust secretion of PYY after oral administration in a degree that can be correlated with the unbound plasma concentration. Further optimisation work ...
Fretz Heinz - - 2013
Herein we describe the discovery of the novel CRTh2 antagonist 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid 28 (setipiprant/ACT-129968), a clinical development candidate for the treatment of asthma and seasonal allergic rhinitis. A lead optimization program was started based on the discovery of the recently disclosed CRTh2 antagonist 2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid 5. An already favorable and ...
Gorovoy Ian - - 2013
PURPOSE:: To determine whether oral folic acid can ameliorate an iatrogenic, visually significant corneal epitheliopathy, which commonly occurs with intravitreal injections of methotrexate for the treatment of intraocular lymphoma. METHODS:: We report 2 cases of visually significant corneal epitheliopathy occurring after intravitreal injections of methotrexate for intraocular lymphoma. The first ...
Khatun Zehedina - - 2013
We have synthesized taurocholic acid (TCA) linked heparin-docetaxel (DTX) conjugates for oral delivery of anticancer drug. The ternary biomolecular conjugates formed self-assembly nanoparticles where docetaxel was located inside the core and taurocholic acid was located on the surface of the nanoparticles. The coupled taurocholic acid in the nanoparticles had enhanced ...
Appel Klaus E - - 2013
In order to quantify the relative bioavailability of glycidol from glycidyl fatty acid esters in vivo, glycidyl palmitoyl ester and glycidol were orally applied to rats in equimolar doses. The time courses of the amounts of glycidol binding to hemoglobin as well as the excretion of 2,3-dihydroxypropyl mercapturic acids were ...
Katsnelson Boris A - - 2013
Inhalation exposure of outbred female white rats (initial age about 4 months) to formaldehyde vapours (12.8±0.69mg/m(3)) 4hrs per day, 5 days per week during 10 weeks induced statistically significant changes in some indices characterizing differential WBC count, functional status of the central nervous system and liver, redox and porphyrin metabolisms, ...
Arulmozhi V - - 2013
Ellagic acid (EA), a naturally occurring polyphenolic compound is well documented for its anticancer property in numerous pre-clinical models. The properties like poor water solubility and limited oral bio-availability of ellagic acid has hampered its clinical applications. The present study, reports the preparation of ellagic acid encapsulated chitosan nanoparticles (EA@CS-NP) ...
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