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https://www.readbyqxmd.com/read/29125158/photodissociation-of-ethylphenylcobalamin-antivitamin-b12
#1
Piotr Lodowski, Karolina Ciura, Megan J Toda, Maria Jaworska, Pawel M Kozlowski
Biologically active forms of cobalamins are crucial cofactors in biochemical reactions and these metabolites can be inhibited by their structurally similar analogues known as antivitamins B12. Phenylethynylcobalamin (PhEtyCbl) or 4-ethylphenylcobalamin (EtPhCbl) exemplify recently synthesized and structurally characterized antivitamins B12. Herein, DFT and TD-DFT studies of EtPhCbl are provided to explore its photochemical behavior, which may lead to design of arylcobalamins that can be used as therapeutic agents in light activated drug applications...
November 10, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29121962/direct-interaction-with-14-3-3%C3%AE-promotes-surface-expression-of-best1-channel-in-astrocyte
#2
Soo-Jin Oh, Junsung Woo, Young-Sun Lee, Minhee Cho, Eunju Kim, Nam-Chul Cho, Jae-Yong Park, Ae Nim Pae, C Justin Lee, Eun Mi Hwang
BACKGROUND: Bestrophin-1 (Best1) is a calcium-activated anion channel (CAAC) that is expressed broadly in mammalian tissues including the brain. We have previously reported that Best1 is expressed in hippocampal astrocytes at the distal peri-synaptic regions, called microdomains, right next to synaptic junctions, and that it disappears from the microdomains in Alzheimer's disease mouse model. Although Best1 appears to be dynamically regulated, the mechanism of its regulation and modulation is poorly understood...
November 9, 2017: Molecular Brain
https://www.readbyqxmd.com/read/29112887/comparative-performance-analysis-of-human-ipsc-derived-and-primary-neural-progenitor-cells-npc-grown-as-neurospheres-in-vitro
#3
Maxi Hofrichter, Laura Nimtz, Julia Tigges, Yaschar Kabiri, Friederike Schröter, Brigitte Royer-Pokora, Barbara Hildebrandt, Martin Schmuck, Alexey Epanchintsev, Stephan Theiss, James Adjaye, Jean-Marc Egly, Jean Krutmann, Ellen Fritsche
Developmental neurotoxicity (DNT) testing performed in rats is resource-intensive (costs, time, animals) and bears the issue of species extrapolation. Thus, reliable alternative human-based approaches are needed for predicting neurodevelopmental toxicity. Human induced pluripotent stem cells (hiPSCs) represent a basis for an alternative method possibly being part of an alternative DNT testing strategy. Here, we compared two hiPSC neural induction protocols resulting in 3D neurospheres: one using noggin and one cultivating cells in neural induction medium (NIM protocol)...
October 26, 2017: Stem Cell Research
https://www.readbyqxmd.com/read/29111673/nano-into-micro-formulations-of-tobramycin-for-the-treatment-of-pseudomonas-aeruginosa-infections-in-cystic-fibrosis
#4
Barbara Porsio, Maria Grazia Cusimano, Domenico Schillaci, Emanuela Fabiola Craparo, Gaetano Giammona, Gennara Cavallaro
Here, nano into micro formulations (NiMs) of tobramycin for the treatment of Pseudomonas aeruginosa airway infections in cystic fibrosis (CF) are described. NiMs were produced by spray drying a solution containing polymers or sugars and a nanometric Polyanion-Tobramcyin Complex (PTC), able to achieve a prolonged antibiotic release. NiMs properties were compared to TOBI®Podhaler®(Novartis), the only one commercially available dry powder inhalatory formulation based on porous microparticles. Produced NiMs showed adequate characteristics for pulmonary administration, as spherical shape, micrometric size and high cytocompatibility towards human bronchial epithelial cells...
November 7, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/29111370/synthesis-and-optical-properties-of-pyrrolidinyl-peptide-nucleic-acid-bearing-a-base-discriminating-fluorescence-nucleobase-8-pyrene-1-yl-ethynyladenine
#5
Duangrat Nim-Anussornkul, Tirayut Vilaivan
A combination of fluorophore and nucleobase through a π-conjugated rigid linker integrates the base pairing and the fluorescence change into a single event. Such base discriminating fluorophore can change its fluorescence as a direct response to the base pairing event and therefore have advantages over tethered labels or base surrogates lacking the hydrogen-bonding ability. 8-(Pyrene-1-yl)ethynyl-adenine (A(PyE)) has been extensively used as fluorescence labels in DNA and LNA, but it showed little discrimination between different nucleobases...
October 13, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29107425/novel-lck-fms-inhibitors-based-on-phenoxypyrimidine-scaffold-as-potential-treatment-for-inflammatory-disorders
#6
Ahmed Karam Farag, Ahmed Elkamhawy, Ashwini M Londhe, Kyung-Tae Lee, Ae Nim Pae, Eun Joo Roh
Tyrosine kinases including LCK and FMS are involved in inflammatory disorders as well as many types of cancer. Our team has designed and synthesized thirty novel pyrimidine based inhibitors targeting LCK, classified into four different series (amides, ureas, imines (Schiff base) and benzylamines). Twelve of them showed nanomolar IC50 values. Compound 7g showed excellent selectivity profile and was selectively potent over FMS kinase (IC50 value of 4.6 nM). Molecular docking study was performed to help us rationalize the obtained results and predict the possible binding mode for our compounds in both LCK and FMS...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29101081/molecular-characterization-of-multidrug-resistant-bacteroides-isolates-from-hungarian-clinical-samples
#7
Károly Péter Sárvári, József Sóki, Katalin Kristóf, Emese Juhász, Cecilia Miszti, Szilvia Zsóka Melegh, Krisztina Latkóczy, Edit Urbán
INTRODUCTION: Members of the Bacteroides fragilis group are the most important components of the normal human gut microbiota, but these bacteria can cause severe infections as well. Due to the frequent usage of antibiotics, the spreading of the MDR strains is a real threat worldwide. MATERIALS AND METHODS: In a multicentre study 400 Bacteroides isolates from five Hungarian microbiological laboratories were cultured and identified by MALDI TOF-MS. The MIC values of ten antibiotics were determined by the agar dilution method and evaluated by the breakpoints of EUCAST or CLSI...
October 31, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29100907/feasibility-and-safety-of-nerve-stimulator-attachment-to-energy-based-devices-a-porcine-model-study
#8
Sung-Chan Shin, Eui-Suk Sung, Sung-Won Choi, Sung-Dong Kim, Da-Woon Jung, Seok-Hyun Kim, Jung Hoon Ro, Jin-Choon Lee, Byung-Joo Lee
BACKGROUND: Recently, several energy-based devices (EBDs) have been developed and applied in the context of thyroid surgery. EBDs can reduce operation time, blood loss, and postoperative pain. Compared to conventional electrocautery, EBDs operate at a relatively lower temperature and produce minimal lateral tissue damage. Yet, during device operation, the tip of the EBD is hot enough to cause thermal nerve damage, increasing the need for surgeons to be cautious about EBD application. To increase the safety of EBDs, we attached nerve stimulators to the tips of two EBDs and compared them to conventional monopolar nerve stimulation using a porcine model...
October 31, 2017: International Journal of Surgery
https://www.readbyqxmd.com/read/29091347/thickness-mapping-of-individual-retinal-layers-and-sectors-by-spectralis-sd-oct-in-autosomal-dominant-optic-atrophy
#9
Nihada Corajevic, Michael Larsen, Cecilia Rönnbäck
PURPOSE: To assess layer- and location-specific retinal thickness deficits in autosomal dominant optic atrophy (ADOA) using Spectralis SD-OCT. METHODS: This cross-sectional study included 41 ADOA patients with OPA1 exon 28 (2826delT) mutation [age, 8.6-83.5 years; best-corrected visual acuity (BCVA), 8-89 Early Treatment Diabetic Retinopathy Study (ETDRS) letters] and 55 mutation-free first-degree relatives as healthy controls (age, 8.9-68.7; BCVA, 80-99). Participants underwent routine examination and optical coherence tomography (OCT) with segmentation of the whole retina, inner retinal layers (IRL) and outer retinal layers (ORL)...
November 1, 2017: Acta Ophthalmologica
https://www.readbyqxmd.com/read/29068693/in-vivo-pulmonary-delivery-and-magnetic-targeting-of-dry-powder-nano-in-microparticles
#10
Dominique N Price, Loreen R Stromberg, Nitesh K Kunda, Pavan Muttil
This brief communication evaluates the cytotoxicity and targeting capability of a dry powder chemotherapeutic. Nano-in-microparticles (NIMs) are a dry powder drug delivery vehicle containing superparamagnetic iron oxide nanoparticles (SPIONs) and either doxorubicin (w/w solids) or fluorescent nanospheres (w/v during formulation; as a drug surrogate) in a lactose matrix. In vitro cytotoxicity was evaluated in A549 adenocarcinoma cells using MTS and LDH assays to assess viability and toxicity after 48 hours of NIMs exposure...
October 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29061436/pattern-and-prevalence-of-psychiatric-disorders-among-patients-attending-dermatology-opd
#11
Sasha Raikhy, Shiv Gautam, Sanjay Kanodia
BACKGROUND: Consideration of psychiatric and psychosocial factors is important for the management and prevention of dermatologic disorders. Dermatology patients suffer commonly from psychiatric comorbidity. AIM: To study pattern and prevalence of psychiatric disorders among patient attending dermatology OPD. METHODS: The study was carried out in Psychiatry department of NIMS Medical College, Jaipur, Rajasthan, a north State of India. The sample was taken from Dermatology department of Medical College...
October 2017: Asian Journal of Psychiatry
https://www.readbyqxmd.com/read/29059091/contact-allergy-to-neem-oil
#12
Anton de Groot, Berend A Jagtman, Marjolijn Woutersen
A case of allergic contact dermatitis from neem oil is presented. Neem oil (synonyms: Melia azadirachta seed oil [INCI name], nim oil, margosa oil) is a vegetable (fixed) oil obtained from the seed of the neem tree Azadirachta indica by cold pressing. Contact allergy to neem oil has been described previously in only 3 patients. The allergen(s) is/are unknown.
November 2017: Dermatitis
https://www.readbyqxmd.com/read/29056763/a-boltzmann-constant-determination-based-on-johnson-noise-thermometry
#13
N E Flowers-Jacobs, A Pollarolo, K J Coakley, A E Fox, H Rogalla, W L Tew, S P Benz
A value for the Boltzmann constant was measured electronically using an improved version of the Johnson Noise Thermometry (JNT) system at the National Institute of Standards and Technology (NIST), USA. This system is different from prior ones, including those from the 2011 determination at NIST and both 2015 and 2017 determinations at the National Institute of Metrology (NIM), China. As in all three previous determinations, the main contribution to the combined uncertainty is the statistical uncertainty in the noise measurement, which is mitigated by accumulating and integrating many weeks of cross-correlated measured data...
October 2017: Metrologia
https://www.readbyqxmd.com/read/29047354/using-risk-tracing-snowball-approach-to-increase-hiv-case-detection-among-high-risk-populations-in-cambodia-an-intervention-study
#14
Srean Chhim, John Macom, Chettana Pav, Nirada Nim, Phearun Yun, Sopheap Seng, Kolab Chhim, Sovannary Tuot, Siyan Yi
BACKGROUND: Early HIV diagnosis and initiation onto antiretroviral therapy may prevent ongoing spread of HIV. Risk Tracing Snowball Approach (RTSA) has been shown to be effective in detecting new HIV cases in other settings. The main objective of this study is to evaluate the effectiveness of RTSA in increasing the rate of newly identified HIV cases among high-risk populations. Our second objective was to evaluate the effectiveness of RTSA, as compared to the walk-in group, in increasing the number of HIV tests and early case detection...
October 18, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/29039561/hovenia-dulcis-thunb-and-its-active-compound-ampelopsin-inhibit-angiogenesis-through-suppression-of-vegfr2-signaling-and-hif-1%C3%AE-expression
#15
Jang Mi Han, Haet Nim Lim, Hye Jin Jung
Specific inhibition of angiogenesis has been considered a powerful strategy for the treatment of cancer and other angiogenesis-related human diseases. Hovenia dulcis Thunb., Japanese raisin tree or Oriental raisin tree, is a hardy tree found in Asia, Eastern China and Korea and has been known to possess various biological activities, including antifatigue, antidiabetic, neuroprotective and hepatoprotective activity. In the present study, for the first time, we evaluated whether a 100% ethanol extract of Hovenia dulcis Thunb...
October 11, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29031076/synthesis-and-evaluation-of-new-pyridyl-pyrazinyl-thiourea-derivatives-neuroprotection-against-amyloid-%C3%AE-induced-toxicity
#16
Jung-Eun Park, Ahmed Elkamhawy, Ahmed H E Hassan, Ae Nim Pae, Jiyoun Lee, Sora Paik, Beoung-Geon Park, Eun Joo Roh
Herein, we report synthesis and evaluation of new twenty six small molecules against β amyloid (Aβ)-induced opening of mitochondrial permeability transition pore (mPTP) using JC-1 assay which measures the change of mitochondrial membrane potential (ΔΨm). The neuroprotective effect of seventeen compounds against Aβ-induced mPTP opening was superior to that of the standard Cyclosporin A (CsA). Fifteen derivatives eliciting increased green to red fluorescence percentage less than 40.0% were evaluated for their impact on ATP production, cell viability and neuroprotection against Aβ-induced neuronal cell death...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031071/discovery-of-thienopyrrolotriazine-derivatives-to-protect-mitochondrial-function-against-a%C3%AE-induced-neurotoxicity
#17
TaeHun Kim, Woo Seung Son, Mohammad Neaz Morshed, Ashwini M Londhe, Seo Yun Jung, Jong-Hyun Park, Woo-Kyu Park, Sang Min Lim, Ki Duk Park, Sung Jin Cho, Kyu-Sung Jeong, Jiyoun Lee, Ae Nim Pae
Recovery of mitochondrial dysfunction has gained increasing attention as an alternative therapeutic strategy for Alzheimer's disease (AD). Recent studies suggested that the 18 kDa mitochondrial translocator protein (TSPO) has the potential to serve as a drug target for the treatment of AD. In this study, we generated a structure-based pharmacophore model and virtually screened a commercial library, identifying SVH07 as a virtual hit, which contained a tricyclic core structure, thieno[2',3':4,5]pyrrolo[1,2-d][1,2,4]triazine group...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28993819/vigilance-the-amygdala-and-anxiety-in-youths-with-a-history-of-institutional-care
#18
Jennifer A Silvers, Bonnie Goff, Laurel J Gabard-Durnam, Dylan G Gee, Dominic S Fareri, Christina Caldera, Nim Tottenham
BACKGROUND: Early adversity is commonly associated with alterations of amygdala circuitry and increased anxiety. While many theoretical and clinical accounts of early adversity suggest that it increases vigilance to threatening stimuli, the present study tested whether heightened anxiety and amygdala reactivity associated with early adversity enhanced goal-directed attention for threatening stimuli. Showing this association would provide support that these adversity-induced alterations are developmental adaptations of the individual...
September 2017: Biological Psychiatry: Cognitive Neuroscience and Neuroimaging
https://www.readbyqxmd.com/read/28989571/black-soybean-anthocyanins-attenuate-inflammatory-responses-by-suppressing-reactive-oxygen-species-production-and-mitogen-activated-protein-kinases-signaling-in-lipopolysaccharide-stimulated-macrophages
#19
Jin Nam Kim, Sung Nim Han, Tae Joung Ha, Hye-Kyeong Kim
BACKGROUND/OBJECTIVES: Oxidative stress is closely related with inflammation and development of many diseases. Black soybean seed coat contains high amount of anthocyanins, which are well-known for free radical scavenging activities. This study investigated inflammatory response and action mechanism of black soybean anthocyanins with regard to antioxidant activity in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. MATERIALS/METHODS: RAW 264.7 cells were treated with anthocyanins extracted from black soybean seed coats in a concentration range of 12...
October 2017: Nutrition Research and Practice
https://www.readbyqxmd.com/read/28963808/injury-mechanisms-and-electromyographic-changes-after-injury-of-the-recurrent-laryngeal-nerve-experiments-in-a-porcine-model
#20
Katrin Brauckhoff, Øyvind S Svendsen, Lodve Stangeland, Martin Biermann, Turid Aas, Paul J A Husby
BACKGROUND: Recurrent laryngeal nerve (RLN) injury during surgery may reveal differences in electromyographic (EMG) changes after sustained compression or traction. METHODS: In 20 pigs with the NIM-FLEX EMG-endotracheal tube, EMG was recorded at baseline, during sustained RLN compression, or traction until 70% amplitude decrease and during 30 minutes of recovery. RESULTS: Seventy percent amplitude decrease from baseline was reached after 110 ± 98 seconds (compression group) and 2034 ± 2108 seconds (traction group)...
September 30, 2017: Head & Neck
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