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https://www.readbyqxmd.com/read/29339251/quinoxaline-derivatives-as-new-inhibitors-of-coxsackievirus-b5
#1
Antonio Carta, Giuseppina Sanna, Irene Briguglio, Silvia Madeddu, Gabriella Vitale, Sandra Piras, Paola Corona, Alessandra Tiziana Peana, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl, Alessandra Serra, Elisa Carta, Roberta Loddo, Gabriele Giliberti
Enteroviruses are among the most common and important human pathogens for which there are no specific antiviral agents approved by the US Food and Drug Administration so far. Particularly, coxsackievirus infections have a worldwide distribution and can cause many important diseases. We here report the synthesis of new 14 quinoxaline derivatives and the evaluation of their cytotoxicity and antiviral activity against representatives of ssRNA, dsRNA and dsDNA viruses. Promisingly, three compounds showed a very potent and selective antiviral activity against coxsackievirus B5, with EC50 in the sub-micromolar range (0...
December 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29336038/a-single-nucleotide-polymorphism-in-the-canine-cytochrome-b5-reductase-cyb5r3-gene-is-associated-with-sulfonamide-hypersensitivity-and-is-overrepresented-in-doberman-pinschers
#2
J M Reinhart, J Ekena, A C Cioffi, L A Trepanier
Canine sulfonamide hypersensitivity (HS) has been associated with a variant in the cytochrome b5 reductase gene (CYB5R3 729A>G), which encodes a drug-detoxifying enzyme. Study objectives were to determine variant allele frequency in Doberman Pinschers (DOBE), a breed which may be predisposed to sulfonamide HS, and to characterize the effects of CYB5R3 729G on gene expression and function. CYB5R3 729A>G allele frequencies were compared between DOBE (n = 24) vs. non-Doberman (non-DOBE; n = 60) dogs...
January 15, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29329608/polyphenols-isolated-from-acacia-mearnsii-bark-with-anti-inflammatory-and-carbolytic-enzyme-inhibitory-activities
#3
Jia Xiong, Mary H Grace, Debora Esposito, Slavko Komarnytsky, Fei Wang, Mary Ann Lila
The present study was designed to characterize the polyphenols isolated from Acacia mearnsii bark crude extract (B) and fractions (B1-B7) obtained by high-speed counter-current chromatography (HSCCC) and evaluate their anti-inflammatory and carbolytic enzymes (α-glucosidase and α-amylase) inhibitory activities. Fractions B4, B5, B6, B7 (total phenolics 850.3, 983.0, 843.9, and 572.5 mg·g-1, respectively; proanthocyanidins 75.7, 90.5, 95.0, and 44.8 mg·g-1, respectively) showed significant activities against reactive oxygen species (ROS), nitric oxide (NO) production, and expression of pro-inflammatory genes interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) in a lipopolysaccharide (LPS)-stimulated mouse macrophage cell line RAW 264...
November 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/29324679/antibacterial-evaluation-and-virtual-screening-of-new-thiazolyl-triazole-schiff-bases-as-potential-dna-gyrase-inhibitors
#4
Cristina Nastasă, Dan C Vodnar, Ioana Ionuţ, Anca Stana, Daniela Benedec, Radu Tamaian, Ovidiu Oniga, Brînduşa Tiperciuc
The global spread of bacterial resistance to drugs used in therapy requires new potent and safe antimicrobial agents. DNA gyrases represent important targets in drug discovery. Schiff bases, thiazole, and triazole derivatives are considered key scaffolds in medicinal chemistry. Fifteen thiazolyl-triazole Schiff bases were evaluated for their antibacterial activity, measuring the growth inhibition zone diameter, the minimum inhibitory concentration (MIC), and the minimum bactericidal concentration (MBC), against Gram-positive (Staphylococcus aureus, Listeria monocytogenes) and Gram-negative (Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa) bacteria...
January 11, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29323107/serological-survey-of-neutralizing-antibodies-to-eight-major-enteroviruses-among-healthy-population
#5
Rui Zhu, Tong Cheng, Zhichao Yin, Dongxiao Liu, Longfa Xu, Yongchao Li, Wei Wang, Jian Liu, Yuqiong Que, Xiangzhong Ye, Qiyi Tang, Qinjian Zhao, Shengxiang Ge, Shuizhen He, Ningshao Xia
Human enteroviruses (EVs) are the most common causative agents infecting human, causing many harmful diseases, such as hand, foot, and mouth disease (HFMD), herpangina (HA), myocarditis, encephalitis, and aseptic meningitis. EV-related diseases pose a serious worldwide threat to public health. To gain comprehensive insight into the seroepidemiology of major prevalent EVs in humans, we firstly performed a serological survey for neutralizing antibodies (nAbs) against Enterovirus A71 (EV-A71), Coxsackie virus A16 (CV-A16), Coxsackie virus A6 (CV-A6), Coxsackie virus A10 (CV-A10), Coxsackie virus B3 (CV-B3), Coxsackie virus B5 (CV-B5), Echovirus 25 (ECHO25), and Echovirus 30 (ECHO30) among the healthy population in Xiamen City in 2016, using micro-neutralization assay...
January 10, 2018: Emerging Microbes & Infections
https://www.readbyqxmd.com/read/29305326/neonatal-exposure-to-bisphenol-a-alters-the-hypothalamic-pituitary-thyroid-axis-in-female-rats
#6
Marina O Fernandez, Nadia S Bourguignon, Paula Arocena, Matías Rosa, Carlos Libertun, Victoria Lux-Lantos
Bisphenol A (BPA) is a component of polycarbonate plastics, epoxy resins and polystyrene found in many common products. Several reports revealed potent in vivo and in vitro effects. In this study we analyzed the effects of the exposure to BPA in the hypothalamic-pituitary-thyroid axis in female rats, both in vivo and in vitro. Female Sprague-Dawley rats were injected sc from postnatal day 1 (PND1) to PND10 with BPA: 500 μg 50 μl-1 oil (B500), or 50 μg 50 μl-1 (B50), or 5 μg 50 μl-1 (B5). Controls were injected with 50 μl vehicle during the same period...
January 2, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29300748/functional-interrogation-of-plasmodium-genus-metabolism-identifies-species-and-stage-specific-differences-in-nutrient-essentiality-and-drug-targeting
#7
Alyaa M Abdel-Haleem, Hooman Hefzi, Katsuhiko Mineta, Xin Gao, Takashi Gojobori, Bernhard O Palsson, Nathan E Lewis, Neema Jamshidi
Several antimalarial drugs exist, but differences between life cycle stages among malaria species pose challenges for developing more effective therapies. To understand the diversity among stages and species, we reconstructed genome-scale models (GEMs) of metabolism for five life cycle stages and five species of Plasmodium spanning the blood, transmission, and mosquito stages. The stage-specific models of Plasmodium falciparum uncovered stage-dependent changes in central carbon metabolism and predicted potential targets that could affect several life cycle stages...
January 4, 2018: PLoS Computational Biology
https://www.readbyqxmd.com/read/29300297/e3l-and-f1l-gene-functions-modulate-the-protective-capacity-of-modified-vaccinia-virus-ankara-immunization-in-murine-model-of-human-smallpox
#8
Asisa Volz, Sylvia Jany, Astrid Freudenstein, Markus Lantermann, Holger Ludwig, Gerd Sutter
The highly attenuated Modified Vaccinia virus Ankara (MVA) lacks most of the known vaccinia virus (VACV) virulence and immune evasion genes. Today MVA can serve as a safety-tested next-generation smallpox vaccine. Yet, we still need to learn about regulatory gene functions preserved in the MVA genome, such as the apoptosis inhibitor genes F1L and E3L. Here, we tested MVA vaccine preparations on the basis of the deletion mutant viruses MVA-ΔF1L and MVA-ΔE3L for efficacy against ectromelia virus (ECTV) challenge infections in mice...
January 4, 2018: Viruses
https://www.readbyqxmd.com/read/29298649/an-inflammation-related-nutrient-pattern-is-associated-with-both-brain-and-cognitive-measures-in-a-multiethnic-elderly-population
#9
Yian Gu, Jennifer J Manly, Richard P Mayeux, Adam M Brickman
BACKGROUND: Accumulating evidence suggest that dietary factors are associated with Alzheimer's disease, and brain and cognitive health. It is unclear whether inflammation explains this association. OBJECTIVE: To examine whether an inflammation-related nutrient pattern (INP) was associated with neuroimaging and cognitive measures of brain health. METHOD: The current cross-sectional study included 330 non-demented elderly (mean age 79 years at MRI scan) participants in a multi-ethnic, community-based cohort study who had information on nutritional intakes (estimated from food frequency questionnaire), circulating C-reactive protein and interleukin-6 (measured by ELISA), MRI scans, and cognition...
January 1, 2018: Current Alzheimer Research
https://www.readbyqxmd.com/read/29288354/functional-characterization-and-substrate-specificity-analysis-of-%C3%AE-6-desaturase-from-marine-microalga-isochrysis-sp
#10
S Thiyagarajan, M Arumugam, N Senthil, S Vellaikumar, S Kathiresan
OBJECTIVES: To express a Δ6-desaturase gene and produce gamma-linolenic acid (GLA) and stearidonic acid (SDA) in prokaryotic expression system (Escherichia coli), and analyze its substrate specificity in the omega-3 fatty acid biosynthetic pathway. RESULTS: Full-length ORF (1448 bp) of Δ6Des-Iso was isolated from Isochrysis sp. and characterized using multiple sequence alignment, phylogenetic analysis, transmembrane domain, and protein tertiary structure. Δ6Des-Iso is a front-end desaturase consisting of three conserved histidine domains and a cytochrome b5 domain...
December 29, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/29237573/identification-of-cytochrome-b5-cytb-5-1-and-cytb-5-2-in-c-elegans-evidence-for-differential-regulation-of-scd
#11
Baoshen He, Jingjing Zhang, Yanli Wang, Yamei Li, Xiaoju Zou, Bin Liang
Unsaturated fatty acids (UFAs) play crucial roles in living organisms regarding development, energy metabolism, stress resistance, etc. The biosynthesis of UFAs starts from the introduction of the first double bond by stearoyl-CoA desaturase (SCD), converting saturated fatty acids (SFAs) to monounsaturated fatty acids (MUFAs). This desaturation is considered to be an aerobic process that requires cytochrome b5 reductase, cytochrome b5 and SCD. However, this enzyme system remains elusive in Caenorhabditis elegans...
December 10, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29233590/structure-activity-analysis-of-cj-15-801-analogues-that-interact-with-plasmodium-falciparum-pantothenate-kinase-and-inhibit-parasite-proliferation
#12
Christina Spry, Alan L Sewell, Yuliya Hering, Mathew V J Villa, Jonas Weber, Stephen J Hobson, Suzannah J Harnor, Sheraz Gul, Rodolfo Marquez, Kevin J Saliba
Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferation in vitro by targeting pantothenate utilization. To inform the design of next generation analogues, we set out to synthesize and test a series of synthetic enamide-bearing pantothenate analogues...
August 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29232844/protection-of-mice-from-lethal-vaccinia-virus-infection-by-vaccinia-virus-protein-subunits-with-a-cpg-adjuvant
#13
Sarah Reeman, Amanda J Gates, David J Pulford, Art Krieg, David O Ulaeto
Smallpox vaccination carries a high risk of adverse events in recipients with a variety of contra-indications for live vaccines. Although alternative non-replicating vaccines have been described in the form of replication-deficient vaccine viruses, DNA vaccines, and subunit vaccines, these are less efficacious than replicating vaccines in animal models. DNA and subunit vaccines in particular have not been shown to give equivalent protection to the traditional replicating smallpox vaccine. We show here that combinations of the orthopoxvirus A27, A33, B5 and L1 proteins give differing levels of protection when administered in different combinations with different adjuvants...
December 9, 2017: Viruses
https://www.readbyqxmd.com/read/29227865/cytochrome-b5-reductase-is-the-component-from-neuronal-synaptic-plasma-membrane-vesicles-that-generates-superoxide-anion-upon-stimulation-by-cytochrome-c
#14
Alejandro K Samhan-Arias, Sofia Fortalezas, Cristina M Cordas, Isabel Moura, José J G Moura, Carlos Gutierrez-Merino
In this work, we measured the effect of cytochrome c on the NADH-dependent superoxide anion production by synaptic plasma membrane vesicles from rat brain. In these membranes, the cytochrome c stimulated NADH-dependent superoxide anion production was inhibited by antibodies against cytochrome b5 reductase linking the production to this enzyme. Measurement of the superoxide anion radical generated by purified recombinant soluble and membrane cytochrome b5 reductase corroborates the production of the radical by different enzyme isoforms...
November 27, 2017: Redox Biology
https://www.readbyqxmd.com/read/29223806/preventing-the-n-terminal-processing-of-human-interferon-%C3%AE-2b-and-its-chimeric-derivatives-expressed-in-escherichia-coli
#15
Fatima Ahsan, Qurratulann Afza Gardner, Naeem Rashid, Greg J Towers, Muhammad Akhtar
We have previously shown that human interferon α-2b (IFN) produced in Escherichia coli (E. coli) is heterogeneous at the N-terminal, with three major species (Ahsan et al., 2014). These are: (a) the direct translation product of the gene retaining the N-terminal methionine, (b) a species from which the methionyl residue has been removed by E. coli methionyl aminopeptidase to give the native interferon α-2b and (c) in which the N-terminal Cys residue of the latter contains an acetyl group. In this paper we overcome this heterogeneity, using engineered interferon derivatives with phenylalanine residue directly downstream of the N-terminal methionine (Met-Phe-IFN)...
November 23, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29214051/cytochrome-b5-protects-photoreceptors-from-light-stress-induced-lipid-peroxidation-and-retinal-degeneration
#16
Xinping Chen, Hana Hall, Jeffrey P Simpson, Walter D Leon-Salas, Donald F Ready, Vikki M Weake
Lipid peroxides are generated by oxidative stress in cells, and contribute to ageing and neurodegenerative disease. The eye is at special risk for lipid peroxidation because photoreceptors possess amplified sensory membranes rich in peroxidation-susceptible polyunsaturated fatty acids. Light-induced lipid peroxidation in the retina contributes to retinal degeneration, and lipid peroxidation has been implicated in the progression of age-associated ocular diseases such as age-related macular degeneration (AMD)...
2017: NPJ Aging and Mechanisms of Disease
https://www.readbyqxmd.com/read/29201218/svp-b5-peptide-from-buthus-martensii-karsch-scorpion-venom-exerts-hyperproliferative-effects-on-irradiated-hematopoietic-cells
#17
Yan Wang, Baiqian Xing, Ting Li, Caixia Wang, Meixun Zhou, Yamin Liu, Lingjie Fan, Lili Hu, Xiang Peng, Yongxin Xiang, Han Wang, Tianhan Kong, Weihua Dong, Qifeng Guo
Previous studies have demonstrated the radioprotective efficacy of scorpion venom peptide, fraction II (SVPII) from the venom of Buthus martensii Karsch. In the present study, the SVP-B5 polypeptide, which is one of the active components of SVPII, was purified using a two-step chromatographic process. SVP-B5 significantly promoted the proliferation of irradiated M-NFS-60 mouse-derived myelocytic leukemia cells. In addition, SVP-B5 effectively and persistently promoted hematopoietic recovery and expansion of hematopoietic cells after irradiation as demonstrated by cobblestone area forming cell and long-term bone marrow culture assays...
November 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29182907/evaluation-of-the-suitability-of-a-plant-virus-pepper-mild-mottle-virus-as-a-surrogate-of-human-enteric-viruses-for-assessment-of-the-efficacy-of-coagulation-rapid-sand-filtration-to-remove-those-viruses
#18
N Shirasaki, T Matsushita, Y Matsui, R Yamashita
Here, we evaluated the removal of three representative human enteric viruses - adenovirus (AdV) type 40, coxsackievirus (CV) B5, and hepatitis A virus (HAV) IB - and one surrogate of human caliciviruses - murine norovirus (MNV) type 1 - by coagulation-rapid sand filtration, using water samples from eight water sources for drinking water treatment plants in Japan. The removal ratios of a plant virus (pepper mild mottle virus; PMMoV) and two bacteriophages (MS2 and φX174) were compared with the removal ratios of human enteric viruses to assess the suitability of PMMoV, MS2, and φX174 as surrogates for human enteric viruses...
November 21, 2017: Water Research
https://www.readbyqxmd.com/read/29174007/-acute-hemorrhagic-edema-of-infancy-associated-with-coxsackie-virus-infection
#19
A Debray, V Ollier, A Coutard, F Arditty, S Bekkar, C Bodemer, M Leruez-Ville, A Mirand, F Lesage, P Foucaud
Acute hemorrhagic edema of infancy is a rare but benign vasculitis occurring in infants aged from 4 to 24 months. Skin lesions can take various forms, including extensive hemorrhagic purpura, and can therefore be mistaken for purpura fulminans if associated with fever, which leads to initiating broad-spectrum antibiotic treatment. In the present case, we describe a 7-month-old boy with acute hemorrhagic edema of infancy and rapidly extensive purpura lesions that led to intravenous cefotaxime and amikacin treatment...
November 21, 2017: Archives de Pédiatrie: Organe Officiel de la Sociéte Française de Pédiatrie
https://www.readbyqxmd.com/read/29165844/oral-microbiomes-from-hunter-gatherers-and-traditional-farmers-reveal-shifts-in-commensal-balance-and-pathogen-load-linked-to-diet
#20
Florent Lassalle, Matteo Spagnoletti, Matteo Fumagalli, Liam Shaw, Mark Dyble, Catherine Walker, Mark G Thomas, Andrea Bamberg Migliano, Francois Balloux
Maladaptation to modern diets has been implicated in several chronic disorders. Given the higher prevalence of disease such as dental caries and chronic gum diseases in industrialized societies, we sought to investigate the impact of different subsistence strategies on oral health and physiology, as documented by the oral microbiome. To control for confounding variables such as environment and host genetics, we sampled saliva from three pairs of populations of hunter-gatherers and traditional farmers living in close proximity in the Philippines...
November 22, 2017: Molecular Ecology
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