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Simone Cristoni, Guglielmo Dusi, Paolo Brambilla, Adriana Albini, Matteo Conti, Maura Brambilla, Antonino Bruno, Francesca Digaudio, Luca Ferlin, Valeria Tazzari, Silvia Mengozzi, Simone Barera, Carlos Salier, Tommaso Trenti, Marco Cantu, Luigi Rossi Bernardi, Douglas M Noonan
Electrospray Ionization (EI) and Collision Induced Dissociation tandem mass spectrometry (CID-MS/MS) are usually employed to obtain compound identification through a mass spectra match. Different algorithms have been developed for this purpose (for example the NIST match algorithm). These approaches compare the tandem mass spectra (MS/MS) of the unknown analyte with the MS/MS spectra of known compounds inserted in a database. The compounds are usually identified on the basis of spectral match value associated with a probability of recognition...
October 24, 2016: Journal of Mass Spectrometry: JMS
M Mezzelani, S Gorbi, D Fattorini, G d'Errico, M Benedetti, M Milan, L Bargelloni, F Regoli
The aim of the present investigation was to provide new insights on accumulation and possible adverse effects of various non-steroidal anti-inflammatory drugs (NSAIDs) in mussels, Mytilus galloprovincialis, exposed to an environmentally realistic concentration (0.5μg/L) of individual compounds, Acetaminophen (AMP), Diclofenac (DIC), Ibuprofen (IBU), Ketoprofen (KET) or Nimesulide (NIM). The measurement of drugs in mussel tissues was integrated with both functional alterations at cellular level and transcriptomic responses...
October 11, 2016: Aquatic Toxicology
E Sawicki, J H M Schellens, J H Beijnen, B Nuijen
Dissolution from the pharmaceutical formulation is a prerequisite for complete and consistent absorption of any orally administered drug, including anticancer agents (oncolytics). Poor dissolution of an oncolytic can result in low oral bioavailability, high variability in blood concentrations and with that suboptimal or even failing therapy. This review discusses pharmaceutical formulation aspects and absorption pharmacokinetics of currently licensed orally administered oncolytics. In nearly half of orally dosed oncolytics poor dissolution is likely to play a major role in low and unpredictable absorption...
September 20, 2016: Cancer Treatment Reviews
Ingo Hoffmann, Miriam Simon, Anja Hörmann, Thorsten Gravert, Peggy Heunemann, Sarah E Rogers, Michael Gradzielski
Nanoemulsions are metastable emulsions with droplet sizes between 20 and 100 nm with a wide range of applications e.g. in polymerization, in pharmaceutical and cos- metic formulations and as drug delivery systems. Even though they are not in ther- modynamic equilibrium, they can be metastable over relatively long times and have the advantage that they can be formed easily by low energy input methods. In par- ticular, the phase inversion concentration method (PIC) allows to form nanoemulsions simply by diluting a suitable mixture of oil and surfactants with water...
October 24, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Fang Miao, Ying Shi, Zhi-Feng Fan, Shan Jiang, Shi-Zheng Xu, Tie-Chi Lei
Safe and effective ingredients capable of removing undesired hyperpigmentation from facial skin are urgently needed for both pharmaceutical and cosmetic purposes. Deoxyarbutin (4-[(tetrahydro-2H-pyran-2-yl) oxy] phenol, D-Arb) is a glucoside derivative of hydroquinone. Here, we investigated the toxicity and efficacy of D-Arb at the sub-cellular level (directly on melanosomes) and skin pigmentation using in vivo and in vitro models to compare with its parent compound hydroquinone (1,4-benzenediol, HQ). At first, we examined the ultrastructural changes of melanosomes in hyperpigmented guinea pig skin induced by 308-nm monochromatic excimer lightand/or treated with HQ and D-Arb using transmission electron microscopy...
2016: PloS One
B C C Khoo, J K Brown, R L Prince
OBJECTIVES: In recent years quantitative computed tomography (QCT) has allowed precise non-invasive, three dimensional, in vivo measurement of hip structure in large numbers of individuals. The effects of ageing on proximal femur structure are reported and implications for the prevention of hip prosthesis loosening and hip fracture considered. DESIGN, SETTING AND PARTICIPANTS: An observational cross-sectional study of proximal femur QCT in 719 unselected female European descent aged 20 to 89 years recruited from US and Australian populations...
2016: PloS One
Meghan L M Fuzzen, Leslie M Bragg, Gerald R Tetreault, Paulina A Bahamonde, Rajiv N Tanna, Charles J Bennett, Mark E McMaster, Mark R Servos
Municipal wastewater effluent (MWWE) and its constituents, such as chemicals of emerging concern, pose a potential threat to the sustainability of fish populations by disrupting key endocrine functions in aquatic organisms. While studies have demonstrated changes in biological markers of exposure of aquatic organisms to groups of chemicals of emerging concern, the variability of these markers over time has not been sufficiently described in wild fish species. The aim of this study was to assess the spatial and temporal variability of biological markers in response to MWWE exposure and to test the consistency of these responses between seasons and among years...
2016: PloS One
Julia Reinfelder, Torsten Kuwert, Michael Beck, James C Sanders, Philipp Ritt, Christian Schmidkonz, Peter Hennig, Olaf Prante, Michael Uder, Bernd Wullich, Peter Goebell
AIM: Prostate-specific membrane antigen (PSMA) is overexpressed in most prostate cancers (PCs). Here, we report our first experience using the Tc-labeled PSMA inhibitor MIP-1404 (Progenics Pharmaceuticals, Inc, Tarrytown, NY) in 60 patients with biochemically recurrent PC. METHODS: Whole-body planar scintigraphy and SPECT/CT of the lower abdominal pelvic region of 60 patients with biochemical relapse of PC were analyzed retrospectively. In these subjects, an average dose of 733...
October 21, 2016: Clinical Nuclear Medicine
Peter M Fischer
Kinase inhibitor research is a comparatively recent branch of medicinal chemistry and pharmacology and the first small-molecule kinase inhibitor, imatinib, was approved for clinical use only 15 years ago. Since then, 33 more kinase inhibitor drugs have received regulatory approval for the treatment of a variety of cancers and the volume of reports on the discovery and development of kinase inhibitors has increased to an extent where it is now difficult-even for those working in the field-easily to keep an overview of the compounds that are being developed, as currently there are 231 such compounds, targeting 38 different protein and lipid kinases (not counting isoforms), in clinical use or under clinical investigation...
October 24, 2016: Medicinal Research Reviews
Agnes Vitry
No abstract text is available yet for this article.
August 2016: Australian Prescriber
A Sangion, P Gramatica
Pharmaceutical and Personal Care Products (PPCPs) became a class of contaminants of emerging concern because are ubiquitously detected in surface water and soil, where they can affect wildlife. Ecotoxicological data are only available for a few PPCPs, thus modelling approaches are essential tools to maximize the information contained in the existing data. In silico methods may be helpful in filling data gaps for the toxicity of PPCPs towards various ecological indicator organisms. The good correlation between toxicity toward Daphnia magna and those on two fish species (Pimephales promelas and Oncorhynchus mykiss), improved by the addition of one theoretical molecular descriptor, allowed us to develop predictive models to investigate the relationship between toxicities in different species...
October 2016: SAR and QSAR in Environmental Research
Maria Inês Dias, Lillian Barros, Patricia Morales, Montaña Cámara, Maria José Alves, M Beatriz P P Oliveira, Celestino Santos-Buelga, Isabel C F R Ferreira
Wild Fragaria vesca L. fruits were studied regarding nutritional and phytochemical compounds, and also antioxidant, antibacterial and biofilm formation inhibition activities. The fruits are good sources of carbohydrates (e.g., sucrose), soluble dietary fiber and polyunsaturated fatty acids, mainly linoleic and linolenic acids, as well as other components such as citric and succinic acids, and vitamins B9 and E (mainly γ-tocopherol). Significant amounts of soluble sugars, citric acid and some amounts of ascorbic acid, vitamins B9 and E (only α-tocopherol) were found also in the infusions...
October 24, 2016: Food & Function
Alessandra Imbrogno, Jennifer Biscarat, Andrea Iris Schäfer
BACKGROUND: Estrogens and their synthetic analogues are widely used as pharmaceuticals. Upon oral administration these drugs are eventually excreted via urine. The persistence of these pharmaceuticals and inefficient removal by water treatment lead to accumulation in surface water and effluents with negative effects for aquatic life and human health. METHODS: In this study, the uptake of estradiol by a combined magnetic ion exchange resin - ultrafiltration process (MIEX-UF) was investigated...
October 21, 2016: Current Pharmaceutical Design
Thao Td Tran, Phuong Hl Tran
Poorly water-soluble drugs, which commonly face the issue of poor absorption and low bioavailability, have been under ongoing research of many formulation scientists for the past few decades. Solid dispersion is one of the most effective strategies in concerns for improving bioavailability of poorly water-soluble drugs. Either application of solid dispersions in dissolution enhancement of poorly water-soluble drugs or the use of swellable polymers in controlled drug release has been reported in pharmaceutical designs widely...
October 21, 2016: Current Pharmaceutical Design
Hojjat Rouhi-Boroujeni, Esfandiar Heidarian, Hamid Rouhi-Boroujeni, Fatemeh Deris, Mahmoud Rafieian-Kopaei
INTRODUCTION: Hyperlipidemia, obesity, hypertension, and diabetes are the most important risk factors for cardiovascular diseases. The aim of this systematic review article is to introduce the medicinal plants that exert significant clinical effects on hypertension, hyperlipidemia, obesity, and diabetes. METHODS: In this review article, the international research databases including MEDLINE, Google scholar, EBSCO, Academic Search, Web of Science, SciVerse, Scopus (SCOPUS), EBSCO, Academic Search, Cochrane, Central Register of Controlled Trials (CENTRAL) and a Chinese database (China Network Knowledge Infrastructure [CNKI]) were searched using the key words hyperlipidemia, hypertension, diabetes, herbal, obesity, and phytomedicine, matched by MESH, from their respective inceptions up to March, 2016...
October 21, 2016: Current Pharmaceutical Design
Marcello Locatelli, Gokhan Zengin, Ahmet Uysal, Simone Carradori, Elisa De Luca, Giuseppe Bellagamba, Abdurrahman Aktumsek, Irina Lazarova
The current study was carried out to evaluate multicomponent pattern, biological and enzymatic activities of seven Asphodeline taxa root extracts as useful ingredients, due to the fact that these plants are commonly used as traditional food supplements in Turkish regions. The extracts were characterized for free anthraquinones and phenolics to obtain a specific chemical fingerprint useful for quality control. These analyzes were coupled to biological and enzymatic activities in order to obtain comprehensive information of the natural product...
October 24, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Fei Yan, Bin Su
Antioxidants are widely found or used in food, pharmaceutical and cosmetics industries, thus rapid and sensitive detection of antioxidants is of great interest. The present work reports a simple and fast electrochemical method for direct analysis of antioxidants in fruit juices by modulating the permeability of mesochannels on the electrode surface. This goal was achieved by growing vertical silica mesochannel array (SMA) with a channel diameter of 2 ∼ 3 nm on the indium tin oxide (ITO) electrode surface using the cylindrical micelles (CMs) as the template...
October 24, 2016: Analytical Chemistry
Nghi C Nguyen, Muhammad Shah, Leonard J Appleman, Rahul Parikh, James M Mountz
Background and Purpose. Radium-223 dichloride (Xofigo®, Bayer HealthCare Pharmaceuticals Inc.) is the first α-particle emitter therapeutic agent approved by the FDA, with benefits in overall survival and delay in symptomatic skeletal event for patients with metastatic castrate-resistant prostate cancer (CRPC). Recent post hoc analyses of the phase III ALSYMPCA trial support the previously established safety profile as well as therapeutic effect and clinical outcome of Radium-223. Currently, Radium-223 is approved as a single agent therapy for metastatic CRPC...
2016: International Journal of Molecular Imaging
Naren P Tallapragada
In August 2015, Turing Pharmaceuticals acquired the marketing rights to Daraprim (pyrimethamine), a drug used to treat parasitic infections like malaria and toxoplasmosis. Soon after, Turing caused an uproar when it announced that it would raise the price per tablet of Daraprim from [Formula: see text], a 5500% price hike for a drug that has been on the market for over 60 years and off patent since the 1970s. Old, off-patent drugs are becoming increasingly expensive; Daraprim is the archetypal example. Turing had the power to set a high price for Daraprim because the drug's limited patient population, the absence of competing manufacturers, and a lack of therapeutic alternatives all created an effective monopoly...
April 2016: Journal of Law and the Biosciences
Andrew K Cordova, Robin Feldman
Research universities have made enormous contributions to the field of medicine and the treatment of human disease. Alone or in collaboration with pharmaceutical companies, academic researchers have added to the store of knowledge that has led to numerous life science breakthroughs. A new chapter may be opening for academic researchers, however, that could lead to a darker tale. 'The mouse that trolled: the long and tortuous history of a gene mutation patent that became an expensive impediment to Alzheimer's research, by Bubela et al...
November 2015: Journal of Law and the Biosciences
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