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https://www.readbyqxmd.com/read/29767512/azide-and-dye-conjugated-coelenterazine-analogues-for-a-multiplex-molecular-imaging-platform
#1
Ryo Nishihara, Emi Hoshino, Yoshiki Kakudate, Satoshi Kishigami, Naoko Iwasawa, Shin-Ichi Sasaki, Takahiro Nakajima, Moritoshi Sato, Shigeru Nishiyama, Daniel Citterio, Koji Suzuki, Sung Bae Kim
Native coelenterazine (nCTZ) is a common substrate to most marine luciferases and photoproteins. In this study, nine novel dye- and azide-conjugated CTZ analogues were synthesized by conjugating a series of fluorescent dyes or an azide group to the C-2 or C-6 position of the nCTZ backbone to obtain bulkiness-driven substrate specificity and potential chemiluminescence/bioluminescence resonance energy transfer (C/BRET). The investigation on the optical properties revealed that azide-conjugated CTZs emit greatly biased bioluminescence to ALucs and ca...
May 16, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29763829/silver-loaded-graphene-as-an-effective-sers-substrate-for-clotrimazole-detection-dft-and-spectroscopic-studies
#2
Abdulmujeeb T Onawole, Saheed A Popoola, Tawfik A Saleh, Abdulaziz A Al-Saadi
Vibrational infrared, Raman and surface-enhanced Raman scattering (SERS) spectra of clotrimazole (CTZ) were documented and evaluated. Density-functional theory, B3LYP/6-311++G(d,p), approach was implemented to identify the possible conformations, develop the electrostatic potential map, evaluate frontier molecular orbitals and calculate the vibrational spectra of the target compound. The silver-loaded graphene was shown to be an effective SERS substrate for CTZ trace detection. The SERS spectrum showed two enhanced bands at 670 cm-1 and 700 cm-1 which confirmed the absorption of the silver substrate through chlorine and nitrogen atoms...
May 7, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29689297/clotrimazole-is-effective-for-the-regression-of-endometriotic-implants-in-a-wistar-rat-experimental-model-of-endometriosis
#3
Daniel Escorsim Machado, Jamila Alessandra Perini, Erika Menezes de Mendonça, Jessica Ristow Branco, Karina Cristina Rodrigues-Baptista, Jessica Alessandra-Perini, Jair Machado Espíndola-Neto, Thiago Alves Dos Santos, Wagner Santos Coelho, Luiz Eurico Nasciutti, Mauro Sola-Penna, Patricia Zancan
The present work aimed to evaluate molecular, angiogenic and inflammatory changes induced by clotrimazole (CTZ) on endometriosis lesions. For this, thirty female Wistar rats with surgically implanted autologous endometrium were treated with CTZ or vehicle (200 mg/kg) via esophageal gavage for 15 consecutive days. CTZ treatment significantly decreased the growth and the size of the implants, and histological examination indicated regression and atrophy, with no toxicity to the animals. The levels of the angiogenic markers VEGF and VEGFR-2 were significantly decreased in CTZ group...
April 21, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29689061/the-role-of-sedem-for-characterizing-the-active-substance-and-polyvinyilpyrrolidone-eliminating-metastable-forms-in-an-oral-lyophilizate-a-preformulation-study
#4
Paloma Flórez Borges, Encarna García-Montoya, Pilar Pérez-Lozano, Enric Jo, Montserrat Miñarro, Albert Manich, Josep Maria Suñé-Negre
A preformulation study of an oral lyophilisate with cetirizine dihydrochloride (CTZ) as active ingredient, mannitol and PVP K30 as bulking agents is presented. CTZ shown a humidity content of 0.150% and a spontaneous hygroscopicity of 0.200% (both determined by SeDeM diagram), demonstrating an adequate stability behavior in solid form. A design of experiments (DoE) performed with both mannitol and PVP K30, followed by a simple factorial design (32) has determined the optimum combination of excipients and CTZ, and showed that a higher proportion of PVP K30 was able to prevent metastable forms generated by mannitol...
2018: PloS One
https://www.readbyqxmd.com/read/29688172/comparative-effect-of-beclomethasone-dipropionate-and-cetirizine-on-acoustic-rhinometry-parameters-in-children-with-perennial-allergic-rhinitis-a-randomized-controlled-trial
#5
V Malizia, S Fasola, G Ferrante, G Cilluffo, R Gagliardo, M Landi, L Montalbano, D Marchese, S La Grutta
BACKGROUND AND OBJECTIVE: The effect of intranasal corticosteroids and oral antihistamines on acoustic rhinometry parameters was not directly compared in previous studies. Objectives: The primary aim was to compare the effect of 21-day treatment with nasal beclomethasone dipropionate (nBDP) versus cetirizine (CTZ) on nasal patency measured by acoustic rhinometry in children with PAR. Comparing their effect on nasal cytology, symptom severity, sleep quality and quality of life was the secondary aim...
April 24, 2018: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/29676342/audit-of-prevention-of-mother-to-child-transmission-programme-interventions-in-hiv-exposed-children-at-national-hospital-abuja-nigeria
#6
Mariya Mukhtar-Yola, Adekunle Tolulope Otuneye, Amsa Baba Mairami, Yewande Wey, Vincent Nwatah, Lamidi Isah Audu
Background: Ninety percentage of children acquire human immunodeficiency virus (HIV) infection in the form of Mother-to-child Transmission (MTCT). In the absence of interventions, transmission rates range from 15% to 45%. This can be reduced to below 5% with effective interventions. The last published national guideline (NG) on prevention of MTCT (PMTCT) was in 2010. Clinical audits are essential in improving the quality of care delivered to patients. Objectives: The study objectives were to determine the rate of MTCT of HIV in exposed infants at a follow-up clinic between 2011 and 2014 and to determine the level of adherence to 2010 NG on the use of highly active antiretroviral therapy (HAART), polymerase chain reaction (PCR) testing, feeding options, antiretroviral (ARV) prophylaxis and the use of co-trimoxazole (CTZ)...
January 2018: Nigerian Postgraduate Medical Journal
https://www.readbyqxmd.com/read/29577367/bioluminescence-driven-optogenetic-activation-of-transplanted-neural-precursor-cells-improves-motor-deficits-in-a-parkinson-s-disease-mouse-model
#7
Jessica R Zenchak, Brandon Palmateer, Nicolai Dorka, Tariq M Brown, Lina-Marie Wagner, William E Medendorp, Eric D Petersen, Mansi Prakash, Ute Hochgeschwender
The need to develop efficient therapies for neurodegenerative diseases is urgent, especially given the increasing percentages of the population living longer, with increasing chances of being afflicted with conditions like Parkinson's disease (PD). A promising curative approach toward PD and other neurodegenerative diseases is the transplantation of stem cells to halt and potentially reverse neuronal degeneration. However, stem cell therapy does not consistently lead to improvement for patients. Using remote stimulation to optogenetically activate transplanted cells, we attempted to improve behavioral outcomes of stem cell transplantation...
March 25, 2018: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/29565188/safety-of-cetirizine-in-pregnancy
#8
Amanda Golembesky, Maureen Cooney, Rossen Boev, Anne-Françoise Schlit, Jürgen W G Bentz
Managing symptoms of allergic rhinitis (AR) and urticaria in pregnant women is important to reduce complications and negative outcomes. The objective of this study was to provide information on the pregnancy outcomes of women exposed to the antihistamine cetirizine (CTZ). The UCB Pharma Patient Safety Database was searched for pregnancies up to 28 February 2015. Maternal CTZ exposure reports were extracted, and pregnancy outcomes were examined, including exposure, comorbidities and infant events. 228 of 522 pregnancies with maternal CTZ exposure had available outcomes; 49 were prospective...
March 22, 2018: Journal of Obstetrics and Gynaecology: the Journal of the Institute of Obstetrics and Gynaecology
https://www.readbyqxmd.com/read/29502174/baricitinib-for-previously-treated-moderate-or-severe-rheumatoid-arthritis-an-evidence-review-group-perspective-of-a-nice-single-technology-appraisal
#9
REVIEW
Shijie Ren, Iñigo Bermejo, Emma Simpson, Ruth Wong, David L Scott, Adam Young, Matt Stevenson
As part of its single technology appraisal process, the National Institute for Health and Care Excellence invited the manufacturer (Eli Lilly) of baricitinib (BARI; Olumiant® ; a Janus kinase inhibitor that is taken orally) to submit evidence of its clinical and cost effectiveness for the treatment of moderate to severe rheumatoid arthritis (RA) after the failure of disease-modifying antirheumatic drugs (DMARDs). The School of Health and Related Research Technology Appraisal Group at the University of Sheffield was commissioned to act as the independent Evidence Review Group (ERG)...
March 3, 2018: PharmacoEconomics
https://www.readbyqxmd.com/read/29494826/effects-of-single-and-combined-exposure-of-pharmaceutical-drugs-carbamazepine-and-cetirizine-and-a-metal-cadmium-on-the-biochemical-responses-of-r-philippinarum
#10
Ângela Almeida, Vânia Calisto, Valdemar I Esteves, Rudolf J Schneider, Amadeu M V M Soares, Etelvina Figueira, Rosa Freitas
In the aquatic environment, organisms are exposed to complex mixtures of contaminants which may alter the toxicity profile of each compound, compared to its toxicity alone. Pharmaceutical drugs (e.g. carbamazepine (CBZ) and cetirizine (CTZ)) and metals (e.g. cadmium (Cd)) are among those contaminants that co-occur in the environment. However, most studies concerning their toxicity towards aquatic species are based on single exposure experiments. Thus, the present study aimed to evaluate single and combined effects of Cd and CBZ or CTZ (single conditions: Cd, CTZ, CBZ; combined conditions: CTZ + Cd, CBZ + Cd) on biomarkers related to oxidative stress and energy metabolism in the edible clam Ruditapes philippinarum, by exposing the organisms for 28 days to environmentally relevant concentrations of these contaminants...
May 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29353802/effects-of-carbamazepine-and-cetirizine-under-an-ocean-acidification-scenario-on-the-biochemical-and-transcriptome-responses-of-the-clam-ruditapes-philippinarum
#11
Ângela Almeida, Rosa Freitas, Vânia Calisto, Valdemar I Esteves, Rudolf J Schneider, Amadeu M V M Soares, Etelvina Figueira, Bruno Campos, Carlos Barata
Several works evaluated the toxicity of pharmaceutical drugs and climate related changes in invertebrates but few explored the combined effects of both stressors, namely considering their mode of action (MoA). Carbamazepine (CBZ) and cetirizine (CTZ) are pharmaceutical drugs detected in the environment and the toxicity derived from the combined effects of these drugs with ocean acidification (OA) is poorly explored. Thus, the present study investigated the biochemical parameters related to an oxidative stress response and the transcription of genes related to the MoA of CBZ (1...
April 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29330065/stargazin-differentially-modulates-ampakine-gating-kinetics-and-pharmacology
#12
Daniel P Radin, Yong-Xin Li, Gary Rogers, Richard Purcell, Arnold Lippa
It was previously reported that Stargazin (STG) enhances the surface expression of AMPA receptors, controls receptor gating and slows channel desensitization as an auxiliary subunit of the receptors. Ampakines are a class of AMPA receptor positive allosteric modulators that modify rates of transmitter binding, channel activity and desensitization parameters. As such, they have shown efficacy in animal models of neurodegenerative diseases, where excitatory synaptic transmission is compromised. Given the functional similarities between STG and ampakines, the current study sought to probe interactions between STG and ampakine gating properties...
February 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28863863/unitary-properties-of-ampa-receptors-with-reduced-desensitization
#13
Wei Zhang, Clarissa Eibl, Autumn M Weeks, Irene Riva, Yan-Jun Li, Andrew J R Plested, James R Howe
Wild-type AMPA receptors display a characteristic rapidly desensitizing phenotype. Many studies point to the dimer interface between pairs of extracellular ligand binding domains as the key region controlling the rate at which the receptors desensitize. However, mutations at the extracellular end of the pore-forming regions (near the putative ion channel gate) have also been shown to alter desensitization. Here we report the behavior of single GluA4 receptors carrying one of two mutations that greatly reduce desensitization at the level of ensemble currents: the dimer interface mutation L484Y and the Lurcher mutation (A623T, GluA4-Lc) in the extracellular end of M3 (the second true transmembrane helix)...
November 21, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28836273/clotrimazole-microemulsion-and-microemulsion-based-gel-evaluation-of-buccal-drug-delivery-and-irritancy-using-chick-chorioallantoic-membrane-as-the-model
#14
Jarika Kaewbanjong, Paul Wan Sia Heng, Prapaporn Boonme
OBJECTIVES: To investigate the efficacy of clotrimazole microemulsion (CTZ-ME) and its gel form, clotrimazole microemulsion-based gel (CTZ-MBG), for the treatment of oral candidiasis. METHODS: CTZ-ME and CTZ-MBG were characterized for droplet size and texture, respectively. The ex-vivo permeation study and irritancy assessment of CTZ-ME and CTZ-MBG were performed using chick chorioallantoic membrane (CAM) as the model. Antifungal activity against Candida albicans ATCC 10 231 of CTZ-ME and CTZ-MBG was determined by agar diffusion method compared to the blank counterparts...
December 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28827351/mechanisms-of-synaptic-depression-at-the-hair-cell-ribbon-synapse-that-support-auditory-nerve-function
#15
Juan D Goutman
Inner hair cells (IHCs) in the cochlea are the mammalian phono-receptors, transducing sound energy into graded changes in membrane potentials, the so called "receptor potentials." Ribbon synapses between IHCs and auditory nerve neurons are responsible for converting receptor potentials into spike rates. The characteristics of auditory nerve responses to sound have been described extensively. For instance, persistent acoustic stimulation produces sensory adaptation, which is revealed as a reduction in neuronal spike rate with time constants in the range of milliseconds to seconds...
September 5, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28799218/synergy-and-mechanism-of-action-of-%C3%AE-mangostin-and-ceftazidime-against-ceftazidime-resistant-acinetobacter-baumannii
#16
T Pimchan, D Maensiri, G Eumkeb
To address the resistance of Acinetobacter baumannii to β-lactam antibiotics, combination therapy between different antibiotic classes is increasingly used. The antibacterial activity of α-mangostin (AMT) alone or in combination with ceftazidime (CTZ) was investigated against ceftazidime-resistant A. baumannii DMST 45378 (CRAB). Initial screening showed that A. baumannii strains possessed AmpC β-lactamase (AmpC), extended-spectrum beta-lactamase (ESBL) and metallo-β-lactamases (MBL). Minimum inhibitory concentrations (MICs) of all test agents were >800 μg ml-1 against CRAB...
October 2017: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/28771790/motoneuron-activity-is-required-for-enhancements-in-functional-recovery-after-peripheral-nerve-injury-in-exercised-female-mice
#17
Poonam B Jaiswal, Jack K Tung, Robert E Gross, Arthur W English
Inhibitory luminopsins (iLMO2) integrate opto- and chemo-genetic approaches and allow for cell-type specific inhibition of neuronal activity. When exposed to a Renilla luciferase substrate, Coelenterazine (CTZ), iLMO2 generates bioluminescence-mediated activation of its amino-terminal halorhodopsin, resulting in neuronal inhibition. Moderate daily exercise in the form of interval treadmill-training (IT) applied following a peripheral nerve injury results in enhanced motor axon regeneration and muscle fiber reinnervation in female mice...
August 3, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28732904/preparation-and-characterization-of-mucosal-adhesive-and-two-step-drug-releasing-cetirizine-chitosan-nanoparticle
#18
Xiaoping Yu, Yuzhi Mu, Mengxue Xu, Guixue Xia, Juan Wang, Ya Liu, Xiguang Chen
To develop a functional nanosized mucosal drug delivery system, a series of amphiphilic cetirizine-chitosan polymer (CTZ-CSs) were constructed. CTZ-CSs could self-assemble into nanoparticles (NPs) which gradually evolved from irregular aggregates to spherical particles with an increasing substitution degree (DS) in CTZ group. The average particle size of CTZ-CSs-NPs with nano ZS90 Zetasizer varied from 153.92nm to 184.48nm and their zeta potential varied between +19.14mV and +22.93mV. Biocompatibility assay exhibited CTZ-CS-NPs had few adverse effects within a certain concentration range...
October 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28623690/candidate-cytochrome-p450-genes-for-ethoxyresorufin-o-deethylase-activity-in-oyster-crassostrea-gigas
#19
Marília Nardelli Siebert, Jacó Joaquim Mattos, Guilherme Toledo-Silva, Guilherme Razzera, Afonso Celso Dias Bainy
Vertebrate cytochrome P450 1 (CYP1) enzymes metabolize endogenous and xenobiotic compounds and usually demonstrate a substrate-inducible response. Ethoxyresorufin O-deethylase activity (EROD) is a common method to quantify CYP1 enzymes activity in these organisms. Despite the absence of this gene family in protostomes, CYP1-like genes were identified in several species, even though no evolutionary relationship has been established with the vertebrate CYP1 family. In the present study, EROD activity was evaluated in microsomal fraction of gills, digestive gland and mantle of Crassostrea gigas...
August 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28601791/effect-of-operational-and-water-quality-parameters-on-conventional-ozonation-and-the-advanced-oxidation-process-o-3-h-2-o-2-kinetics-of-micropollutant-abatement-transformation-product-and-bromate-formation-in-a-surface-water
#20
Marc Bourgin, Ewa Borowska, Jakob Helbing, Juliane Hollender, Hans-Peter Kaiser, Cornelia Kienle, Christa S McArdell, Eszter Simon, Urs von Gunten
The efficiency of ozone-based processes under various conditions was studied for the treatment of a surface water (Lake Zürich water, Switzerland) spiked with 19 micropollutants (pharmaceuticals, pesticides, industrial chemical, X-ray contrast medium, sweetener) each at 1 μg L-1 . Two pilot-scale ozonation reactors (4-5 m3  h-1 ), a 4-chamber reactor and a tubular reactor, were investigated by either conventional ozonation and/or the advanced oxidation process (AOP) O3 /H2 O2 . The effects of selected operational parameters, such as ozone dose (0...
October 1, 2017: Water Research
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