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phr1320
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Amadeu Gavaldà et al.
Pulmonary pharmacology & therapeutics, 28(2), 114-121 (2014-06-15)
This study characterised the in vitro and in vivo profiles of two novel long-acting muscarinic antagonists, aclidinium bromide and glycopyrronium bromide, using tiotropium bromide and ipratropium bromide as comparators. All four antagonists had high affinity for the five muscarinic receptor sub-types (M1-M5);
Christine Cahyadi et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 90, 30-37 (2014-12-03)
The Supercell coater was developed as an in-line small batch tablet coater which uses air-fluidization for tablet coating. Coating time is very much reduced, with improved heat and mass transfer. It was hypothesized that the quasi-continuous Supercell coating process was
Y Mei et al.
Oncogene, 33(29), 3839-3850 (2013-08-27)
Podoplanin is highly expressed in human cancers. However, mechanisms regulating podoplanin expression remain elusive. Here we show that podoplanin promotes tumorigenesis of oral squamous cell carcinoma (OSCC) and precancerous cells both in vitro and in vivo, and the ErbB3-binding protein-1
Basavaraj Siddalingappa et al.
PloS one, 10(3), e0118824-e0118824 (2015-03-24)
Resveratrol is naturally occurring phytochemical with diverse biological activities such as chemoprevention, anti-inflammatory, anti-cancer, anti-oxidant. But undergoes rapid metabolism in the body (half life 0.13h). Hence Polymer conjugation utilizing different chemical linkers and polymer compositions was investigated for enhanced pharmacokinetic
Xuekui Dong et al.
Journal of integrative plant biology, 56(9), 876-886 (2014-04-16)
Flavonoids constitute a major group of plant phenolic compounds. While extensively studied in Arabidopsis, profiling and naturally occurring variation of these compounds in rice (Oryza sativa), the monocot model plant, are less reported. Using a collection of rice germplasm, comprehensive
Neale Harrison et al.
PloS one, 9(11), e113007-e113007 (2014-11-26)
N-acylethanolamines are an important class of lipid signaling molecules found in many species, including the nematode Caenorhabditis elegans (C. elegans) where they are involved in development and adult lifespan. In mammals, the relative activity of the biosynthetic enzyme N-acyl phosphatidylethanolamine-specific
L Fontana et al.
Cancer letters, 359(1), 87-96 (2015-01-13)
MAP/microtubule affinity-regulating kinase 4 (MARK4) is a serine-threonine kinase that phosphorylates microtubule-associated proteins taking part in the regulation of microtubule dynamics. MARK4 is expressed in two spliced isoforms characterized by inclusion (MARK4S) or exclusion (MARK4L) of exon 16. The distinct
Anna W Sromek et al.
Journal of labelled compounds & radiopharmaceuticals, 57(14), 725-729 (2014-11-18)
Aporphines are attractive candidates for imaging D2 receptor function because, as agonists rather than antagonists, they are selective for the receptor in the high affinity state. In contrast, D2 antagonists do not distinguish between the high and low affinity states
Aiming Liu et al.
Pharmacological reports : PR, 67(2), 299-304 (2015-02-26)
The antiepileptic drug carbamazepine (CBZ) is a typical inducer of cytochrome P450 (CYP) 3A and 2C in the clinic. It is considered a strong constitutive androstane receptor activator, however both CBZ and its main metabolite CBZ 10, 11-epoxide have been
Pierre-André Billat et al.
Analytical and bioanalytical chemistry, 407(12), 3449-3456 (2015-02-24)
Ganciclovir (GCV) is prescribed for cytomegalovirus infection which is a major issue in immunodepressed patients. It is however characterized by hematological toxicity. A better understanding of GCV concentration-effects relationships implies the measurement of intracellular forms. The objective of this study
Rodica Mărgăoan et al.
Journal of agricultural and food chemistry, 62(27), 6306-6316 (2014-06-19)
Total and individual carotenoids, fatty acid composition of total lipids, and main lipid classes of 16 fresh bee-collected pollen samples from Romania were determined by high-performance liquid chromatography with photodiode array detection and capillary gas chromatography with mass detection. Analyzed
Dan T Vogl et al.
Autophagy, 10(8), 1380-1390 (2014-07-06)
The efficacy of proteasome inhibition for myeloma is limited by therapeutic resistance, which may be mediated by activation of the autophagy pathway as an alternative mechanism of protein degradation. Preclinical studies demonstrate that autophagy inhibition with hydroxychloroquine augments the antimyeloma
Ravi Bhushan et al.
Journal of chromatography. A, 1379, 43-50 (2015-01-13)
Five d-amino acids have been used for the first time to synthesize chiral derivatizing reagents (as variants of Marfey's reagent) by nucleophilic displacement of one of the fluorine atoms in 1,5-difluoro-2,4-dinitrobenzene as against the literature reports on application of only
Yan Ma et al.
Drug development and industrial pharmacy, 41(2), 177-182 (2014-08-13)
Aim to design an effective breviscapine nanoscale drug delivery system to realize the improvement of its oral bioavailability. Based on the investigations of the stabilities in the gastrointestinal tract (GIT), permeation and efflux across the cell membrane, the breviscapine nanoemulsion
Ashish V Kalra et al.
Cancer research, 74(23), 7003-7013 (2014-10-03)
A major challenge in the clinical use of cytotoxic chemotherapeutics is maximizing efficacy in tumors while sparing normal tissue. Irinotecan is used for colorectal cancer treatment but the extent of its use is limited by toxic side effects. Liposomal delivery
Katya Govender et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 985, 6-13 (2015-02-04)
A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantitation of the antimalarial drug, lumefantrine (LF), in mouse whole blood and plasma. The analyte was extracted using a protein precipitation method followed by chromatographic separation on
Fabrice Gritti et al.
Journal of chromatography. A, 1376, 112-125 (2014-12-30)
We propose an original model of effective diffusion along packed beds of mesoporous particles for HILIC developed by combining Torquatos model for heterogeneous beds (external eluent+particles), Landauers model for porous particles (solid skeleton+internal eluent), and the time-averaged model for the
Teresa W Tam et al.
Journal of ethnopharmacology, 155(1), 841-846 (2014-06-28)
Rhododendron groenlandicum (Bog Labrador tea), Rhododendron tomentosum (Marsh Labrador tea) and Juniperus communis (Juniper) are used in medicinal teas by Canadian aboriginal cultures alone and in combination with conventional drug products. The safety of this combination had not been previously
Qionghua Wei et al.
International journal of pharmaceutics, 482(1-2), 11-20 (2014-12-03)
The CapsMorph(®) technology prepares amorphous drugs for oral delivery by encapsulating them into porous materials. Hesperidin as model compound was loaded onto AEROPERL(®) 300 Pharma using the wetness impregnation method. Hesperidin was dissolved in dimethyl sulfoxide (DMSO) and alternatively in
Mary Wharton et al.
Journal of chromatographic science, 52(3), 187-194 (2013-03-12)
A simple, rapid ultra-performance liquid chromatography (UPLC) method was developed for the analysis of itraconazole and its associated production impurities. The optimum chromatographic conditions were achieved using an Agilent Zorbax Eclipse XDB C18 column, 1.8 µm (4.6 × 50 mm)
João Cleverson Gasparetto et al.
PloS one, 10(3), e0118922-e0118922 (2015-03-11)
For decades guaco species have been empirically used for the treatment of respiratory diseases. However, studies have shown that the toxic and therapeutic effects of the main guaco metabolites are dose-dependent, and none clinical study was done to evaluate the
Ying Liu et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 970, 68-76 (2014-09-23)
A high-throughput method for the simultaneous determination of 26 mycotoxins in sesame butter was developed by coupling the modified Quick Easy Cheap Effective Rugged and Safe (QuEChERS) method with ultra-high performance liquid chromatography triple quadrupole mass spectrometry (UHPLC-MS/MS). The samples
Maria Chiara Mimmi et al.
Journal of proteome research, 14(3), 1465-1471 (2015-01-28)
Fetal endoscopic tracheal occlusion has been proposed as a prenatal intervention to ameliorate congenital diaphragmatic hernia (CDH) prognosis. Tracheal occlusion (TO) prevents pulmonary fluid egress, leading to tissue expansion, reversal of lung hypoplasia, and potential maturation. Fetal lung maturity strongly
Joel Lindgren et al.
Chembiochem : a European journal of chemical biology, 15(14), 2132-2138 (2014-09-11)
Protein-based pharmaceuticals typically display high selectivity and low toxicity, but are also characterized by low oral availability, mainly because of enzymatic degradation in the gastrointestinal tract and poor permeability across the intestinal wall. One way to increase the proteolytic stability
Raquel S Teixeira et al.
International journal of pharmaceutics, 474(1-2), 212-222 (2014-08-12)
The aim of this study is to investigate the efficacy of new, biocompatible, lysine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine hydrochloride, topically administered. Results show that this class of surfactants strongly influences permeation
Sara Triñanes et al.
Talanta, 132, 433-442 (2014-12-06)
A new straightforward and inexpensive sample screening method for both EPA and EU priority polycyclic aromatic hydrocarbons (PAHs) in water has been developed. The method is based on combined direct immersion and headspace (DIHS) sorptive extraction, using low-cost disposable material
Yi Dong et al.
Food chemistry, 168, 538-545 (2014-08-31)
The kinetics of adsorption and desorption behaviours of five macroporous resins for enriching flavonoids from Glycyrrhizaglabra L. leaf were investigated. All five resins showed similar and effective adsorption and desorption properties. A pseudo-second-order kinetics model was suitable for evaluating the
S Huber et al.
Journal of pharmaceutical and biomedical analysis, 104, 137-143 (2014-12-17)
Esters of the cytostatic bendamustine (1), previously demonstrated to be much more potent than the parent compound as antiproliferative agents in vitro, were investigated for stability in buffer and plasma, as well as against porcine liver esterase in the presence
Bjoern Wagner et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 68, 68-77 (2014-12-17)
Here we present a miniaturized assay, referred to as Carrier-Mediated Distribution System (CAMDIS) for fast and reliable measurement of octanol/water distribution coefficients, log D(oct). By introducing a filter support for octanol, phase separation from water is facilitated and the tendency
Sahng-Wook Hahm et al.
Journal of medicinal food, 18(1), 31-44 (2014-11-08)
In this study, we found that the total polyphenol and ascorbic acid levels in the fruit of Opuntia humifusa are higher than those in other parts of the plant. We further hypothesized that antioxidants in O. humifusa might affect the
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