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Bice S Martincigh, Moses A Ollengo
The photostabilizing ability of grape seed extract on three common sunscreen absorbers: 2-ethylhexyl-p-methoxcinnamate (EHMC), benzophenone-3 (BP3) and tert-butylmethoxy dibenzoylmethane (BMDBM), was investigated. Samples were exposed to simulated solar radiation and monitored by spectrophotometric and chromatographic methods. The chemical composition of the grape seed extract was determined by GC-MS and HPLC-MS and the major secondary metabolites were found to be epicatechin and catechin. Exposure of the extract to UV radiation increased the UV absorption capacity of the extract...
October 19, 2016: Photochemistry and Photobiology
Carlos Walter Sobrado, Lucas Faraco Sobrado
Introduction: Acute severe colitis is a potentially lethal medical emergency and, even today, its treatment remains a challenge for clinicians and surgeons. Intravenous corticoid therapy, which was introduced into the therapeutic arsenal in the 1950s, continues to be the first-line treatment and, for patients who are refractory to this, the rescue therapy may consist of clinical measures or emergency colectomy. Objective: To evaluate the indications for and results from drug rescue therapy (cyclosporine, infliximab and tacrolimus), and to suggest a practical guide for clinical approaches...
July 2016: Arquivos Brasileiros de Cirurgia Digestiva: ABCD, Brazilian Archives of Digestive Surgery
Kim Heang Ly, François Dalmay, Guillaume Gondran, Sylvain Palat, Holy Bezanahary, Anne Cypierre, Anne-Laure Fauchais, Eric Liozon
Although a glucocorticoid (GC)-sparing strategy is needed for patients with giant cell arteritis (GCA) suffering from refractory disease or serious treatment-related complications, evidence of efficacy in this setting of immunosuppressive drugs and biotherapies is lacking. Herein, we evaluated the GC-sparing effects and tolerability of addition of dapsone (DDS) to prednisone therapy in patients with GCA. We retrospectively assessed data on 18 GCA patients who received DDS as a first-line treatment (DDS-1 group) and 52 patients who received it as a second- or third-line treatment for refractory GCA, with or without excessive GC-related toxicity (DDS-2 group)...
October 2016: Medicine (Baltimore)
Maneea Eizadi Sharifabad, Tim Mercer, Tapas Sen
Liposome-capped core-shell mesoporous silica-coated superparamagnetic iron oxide nanoparticles called 'magnetic protocells' were prepared as novel nanocomposites and used for loading anticancer drug doxorubicin (DOX) for cellular toxicity study. Cytotoxicity of the magnetic protocells with or without DOX was tested in vitro on commercial MCF7 and U87 cell lines under alternating magnetic field. MCF7 cell line treated with the DOX-loaded nanoparticles under alternating magnetic field exhibited nearly 20% lower survival rate after 24 h compared with cells treated with free DOX and similarly, it was around 24% when applied to U87...
October 19, 2016: Nanomedicine
Nahid Shahabadi, Monireh Falsafi, Maryam Maghsudi
The interaction of anticancer drug cytarabine with calf thymus DNA (CT-DNA) was investigated in vitro under simulated physiological conditions by multispectroscopic techniques and molecular modeling study. The fluorescence spectroscopy and UV absorption spectroscopy indicated drug interacted with CT-DNA in a groove-binding mode, while the binding constant of UV-vis and the number of binding sites were 4.0 ± 0.2 × 10(4) L mol(-1) and 1.39, respectively. The fluorimetric studies showed that the reaction between the drugs with CT-DNA is exothermic...
October 19, 2016: Nucleosides, Nucleotides & Nucleic Acids
Feng Chen, Liping Liu, Zengguo Bai, Tianhua Zhang, Keke Zhao
Here, 3 fluorinated intermediates of drug were synthesized: (M1), (M2), (M3). Three new anticoagulant rodenticides were designed which were based on 4-hydroxycoumarin or 1,3-indandione, added acute toxicity groups containing fluorine. The structures of synthesized compounds were analyzed and proved by FT-IR spectroscopy and (1)H nuclear magnetic resonance ((1)H-NMR). The compounds were also evaluated for their anticoagulant and acute biologic activity. In addition, both the acute orally toxicity and the feeding indexes of R1 and R2 were tested...
October 19, 2016: Bioengineered
Justin C Chia, P Régine Mydlarski
PURPOSE: Omalizumab is a recombinant humanized monoclonal antibody that inhibits the binding of IgE to the high-affinity IgE receptor (FceRI) on the surface of mast cells and basophils. Omalizumab has been approved for use in asthma, and new reports show promise in a variety of dermatologic diseases. Herein, we review the literature on omalizumab in dermatology and discuss the safety, efficacy and mechanisms of action for this emerging therapy. MATERIALS AND METHODS: PubMED, MEDLINE, and Embase databases were searched for the period January 1, 1990, to September 1, 2016...
October 19, 2016: Journal of Dermatological Treatment
Mark Haden, John R H Archer, Paul I Dargan, David M Wood
BACKGROUND: MDMB-CHMICA (methyl 2-[[1-(cyclohexylmethyl)indole-3-carbonyl]amino]-3,3-dimethylbutanoate) is a synthetic cannabinoid receptor agonist that has been detected in several recreational drug products in Europe since August 2014. OBJECTIVES: This article aims to describe the prevalence of use, availability, and desired and adverse effects of MDMB-CHMICA. METHODS: Data were collated from published scientific literature, and systematic searches were conducted of publically available Internet sources (the "gray literature"), including websites offering to sell MDMB-CHMICA and Internet discussion forums featuring user reports...
October 19, 2016: Substance Use & Misuse
Wing-Hin Lee, Ching-Yee Loo, Chean-Ring Leong, Paul M Young, Daniela Traini, Ramin Rohanizadeh
The effectiveness of conventional cancer chemotherapy is hampered by the occurrence of multidrug resistance (MDR) in tumor cells. Although many studies have reported the development of novel MDR chemotherapeutic agents, clinical success is lacking owing to the high associated toxicity. Nanoparticle-based delivery of chemotherapeutic drugs has emerged as alternative approach to treat MDR cancers via exploitation of leaky vasculature in the tumor microenvironment. Accordingly, functionalization of nanoparticles with target specific ligands can be employed to achieve significant improvements in the treatment of MDR cancer...
October 19, 2016: Expert Opinion on Drug Delivery
Cheng Zhang, C James Chou
A novel synthetic approach to amidoquinones by the reaction of naphthoquinones with hydroxamic acids under basic conditions was developed. The reaction is mild and operationally simple, and it affords high yields of amidoquinones. With this new method, a novel, very strong HDAC6 inhibitor, which showed high toxicity to AML cells, was successfully synthesized.
October 19, 2016: Organic Letters
Jing-Min Liu, Yao-Yao Liu, Dong-Dong Zhang, Guozhen Fang, Shuo Wang
The rise of multimodal nanoprobes has promoted the development of new methods to explore multiple molecular targets simultaneously, or to combine various bioimaging tools in one assay to more clearly delineate localization and expression of bio-markers. Persistent luminescence nanophosphors (PLNPs) have been qualified as the promising contrast agent for in vivo imaging. The easy surface modification and proper nanostructure design strategy would favor the fabrication of PLNPs based multi-functional nanoprobes for biological application...
October 19, 2016: ACS Applied Materials & Interfaces
Aleksandar Antanasijevic, Nicholas J Hafeman, Smanla Tundup, Carolyn Kingsley, Rama K Mishra, Lijun Rong, Balaji Manicassamy, Duncan Wardrop, Michael Caffrey
The viral envelope protein hemagglutinin (HA) plays a critical role in influenza entry and thus is an attractive target for novel therapeutics. The small molecule tert-butylhydroquinone (TBHQ) has previously been shown to bind to HA and inhibit HA-mediated entry with low micromolar potency. However, enthusiasm for the use of TBHQ has diminished due to the compound's antioxidant properties. In this work we show that the antioxidant properties of TBHQ are not responsible for the inhibition of HA-mediated entry...
September 9, 2016: ACS Infectious Diseases
Vita Wonoputri, Cindy Gunawan, Sanly Liu, Nicolas Barraud, Lachlan Hartley Yee, May Lim, Rose Amal
In this study, we developed a poly(vinyl chloride) (PVC)-solvent casted mixed metal copper and iron complexes capable of catalytic generation of the antibiofilm nitric oxide (NO) from endogenous nitrite. In the absence of additional reducing agent, we demonstrated that the presence of iron complex facilitates a redox cycling, converting the copper(II) complex to active copper(I) species, which catalyzes the generation of NO from nitrite. Assessed by protein assay and surface coverage analyses, the presence of the mixed metal complexes in systems containing water industry-relevant nitrite-producing nitrifying biofilms was shown to result in a 'non-toxic mode' of biofilm suppression, while confining the bacterial growth to the free-floating planktonic phase...
October 19, 2016: ACS Applied Materials & Interfaces
Musfiqur Rahman, A M Abd El-Aty, Sung-Woo Kim, Sung Chul Shin, Ho-Chul Shin, Jae-Han Shim
In pesticide residue analysis, relatively low-sensitivity traditional detectors, such as UV, diode array, electron-capture, flame photometric, and nitrogen-phosphorus detectors, have been used following classical sample preparation (liquid-liquid extraction and open glass column cleanup); however, the extraction method is laborious, time-consuming, and requires large volumes of toxic organic solvents. A quick, easy, cheap, effective, rugged, and safe method was introduced in 2003 and coupled with selective and sensitive mass detectors to overcome the aforementioned drawbacks...
October 19, 2016: Journal of Separation Science
Marika Rai, David Spratt, Paola R Gomez-Pereira, Jay Patel, Sean P Nair
Oral malodour is a common condition which affects a large proportion of the population, resulting in social, emotional and psychological stress. Certain oral bacteria form a coating called a biofilm on the tongue dorsum and degrade organic compounds releasing volatile sulfur compounds that are malodourous. Current chemical treatments for oral malodour such as mouthwashes containing chlorhexidine or essential oils, are not sufficiently effective at reducing the bacterial load on the tongue. One potential alternative to current chemical treatments for oral malodour is the use of light activated antimicrobial agents (LAAAs), which display no toxicity or antimicrobial activity in the dark, but when exposed to light of a specific wavelength produce reactive oxygen species which induce damage to target cells in a process known as photodynamic inactivation...
October 18, 2016: Journal of Breath Research
James N Ayres, Kenneth B Ling, Louis C Morrill
A one-pot N-cyanation of secondary amines has been developed using trichloroacetonitrile as an inexpensive cyano source. A diverse range of cyclic and acyclic secondary amines can be readily transformed into the corresponding cyanamides in good isolated yields, with the method successfully utilized in the final synthetic step of a biologically active rolipram-derived cyanamide. This approach exhibits distinct selectivity when compared to the use of highly toxic cyanogen bromide.
October 18, 2016: Organic Letters
S S Garcia, Q Du, H Wu
The oral cavity is a dynamic environment characterized by hundreds of bacterial species, saliva, and an influx of nutrients and metal ions such as copper. Although there is a physiologic level of copper in the saliva, the oral cavity is often challenged with an influx of copper ions. At high concentrations copper is toxic and must therefore be strictly regulated by pathogens for them to persist and cause disease. The cariogenic pathogen Streptococcus mutans manages excess copper using the copYAZ operon that encodes a negative DNA-binding repressor (CopY), the P1-ATPase copper exporter (CopA), and the copper chaperone (CopZ)...
December 21, 2015: Molecular Oral Microbiology
Thomas C Sparks, Beth A Lorsbach
Agrochemicals have been critical to the production of food and fiber, as well as the control of vectors of disease. The need for the discovery and development of new agrochemicals continues unabated due to the loss of existing products through the development of resistance, the desire for products with more favorable environmental and toxicological profiles, shifting pest spectrums, and changing agricultural needs and practices. As presented in the associated analysis of the agrochemical industry, the rising costs and complexities of agrochemical discovery has, in part, led to increasing consolidation, especially in the US and Europe...
October 18, 2016: Pest Management Science
Zujun Xu, Mengmeng Pang, Changwang Li, Baocun Zhu
Recently, growing attention has been paid to the detection of hydrazine (NH2 NH2 ) because of its important roles in industrial chemical and high toxicity to human beings. Herein, we have constructed a new colorimetric and far-red fluorescent probe containing a receptor of 4-bromobutanoate to selectively detect hydrazine. The probe could detect hydrazine quantitatively in the range of 40-500 μM with the detection limit of 2.9 μM. In addition, the probe could monitor hydrazine by the ratiometric method with a large (185 nm) red-shifted absorption spectrum, and the color changes from yellow to blue make it as a 'naked-eye' indicator for hydrazine...
October 18, 2016: Luminescence: the Journal of Biological and Chemical Luminescence
Takashi Ishida, Sachie Suzuki, Chen-Yi Lai, Satoshi Yamazaki, Shigeru Kakuta, Yoichiro Iwakura, Masanori Nojima, Yasuo Takeuchi, Masaaki Higashihara, Hiromitsu Nakauchi, Makoto Otsu
Hematopoietic stem cell (HSC) transplantation (HSCT) for malignancy requires toxic pre-conditioning to maximize anti-tumor effects and donor-HSC engraftment. While this induces bone marrow (BM)-localized inflammation, how this BM environmental change affects transplanted HSCs in vivo remains largely unknown. We here report that, depending on interval between irradiation and HSCT, residence within lethally irradiated recipient BM compromises donor-HSC reconstitution ability. Both in vivo and in vitro we demonstrate that, among inflammatory cytokines, TNF-α plays a role in HSC damage: TNF-α stimulation leads to accumulation of reactive oxygen species (ROS) in highly purified hematopoietic stem/progenitor cells (HSCs/HSPCs)...
October 18, 2016: Stem Cells
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