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https://www.readbyqxmd.com/read/29668114/-%C3%AE-2-adrenoceptors-inhibit-neutrophil-extracellular-traps-in-human-polymorphonuclear-leukocytes
#1
Franca Marino, Angela Scanzano, Laura Pulze, Monica Pinoli, Emanuela Rasini, Alessandra Luini, Raffaella Bombelli, Massimiliano Legnaro, Magda de Eguileor, Marco Cosentino
This study tests the hypothesis that in isolated human polymorphonuclear leukocytes (PMN) adrenergic ligands can affect neutrophil extracellular trap (NET) formation. We have previously shown that, in PMN, adrenaline (A), through the activation of adrenergic receptors (AR), reduces stimulus-dependent cell activation; we have, therefore, planned to investigate if AR are involved in NET production. PMN were obtained from venous blood of healthy subject. The ability of adrenergic ligands to affect reactive oxygen species (ROS) production, NET production, and cell migration was investigated in cells cultured under resting conditions or after activation with N-formyl-methionyl-leucyl-phenylalanine (fMLP), LPS, or IL-8...
April 18, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29668107/plant-cuticle-under-global-change-biophysical-implications
#2
José A Heredia-Guerrero, Susana Guzman-Puyol, José J Benítez, Athanassia Athanassiou, Antonio Heredia, Eva Domínguez
The climatic stressors that modify the chemical composition of plant tissues have been recently reviewed by Suseela and Tharayil (2017). In particular, the authors stated that the response of plants to global change effects (viz. increasing temperatures and frequent drought periods) can induce important modifications in plant cuticles such as an increase of the main cuticle components (cutin and polysaccharides), a preponderance of cutan, heavier wax loads, and changes in the chemical composition of waxes, mainly the accumulation of longer aliphatic compounds...
April 18, 2018: Global Change Biology
https://www.readbyqxmd.com/read/29668081/lipocalin-type-prostaglandin-d-synthase-is-a-novel-phytocannabinoid-binding-protein
#3
Matthew W Elmes, Anthony D Volpe, Simon d'Oelsnitz, Joseph M Sweeney, Martin Kaczocha
Lipocalin-type prostaglandin D synthase (L-PGDS; EC:5.3.99.2) is an enzyme with dual functional roles as a prostaglandin D2 -synthesizing enzyme and as an extracellular transporter for diverse lipophilic compounds in the cerebrospinal fluid (CSF). Transport of hydrophobic endocannabinoids is mediated by serum albumin in the blood and intracellularly by the fatty acid binding proteins, but no analogous transport mechanism has yet been described in CSF. L-PGDS has been reported to promiscuously bind a wide variety of lipophilic ligands and is among the most abundant proteins found in the CSF...
April 18, 2018: Lipids
https://www.readbyqxmd.com/read/29668069/the-direct-synthesis-of-imines-benzimidazoles-and-quinoxalines-from-nitroarenes-and-carbonyl-compounds-via-selective-nitroarene-hydrogenation-employing-a-reusable-iron-catalyst
#4
Rhett Kempe, Christoph Bäumler
The "replacement" of noble metals by earth abundant metals is a desirable aim in catalysis and a possible way of conserving rare elements. The "replacement" is especially attractive if novel selectivity patterns are observed permitting the development of novel coupling reactions. Herein, we report on a novel, robust and reusable iron catalyst, which permits the selective hydrogenation of nitroarenes in the presence of hydrogenation-sensitive functional groups. Based on the selectivity pattern observed, the direct iron catalyzed synthesis of imines and benzimidazoles from nitroarenes and aldehydes becomes feasible...
April 18, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29668064/assessment-of-a-panel-of-cellular-biomarkers-and-the-kinetics-of-their-induction-in-comparing-genotoxic-modes-of-action-in-hepg2-cells
#5
Benjamin Kopp, Morgane Dario, Daniel Zalko, Marc Audebert
One major challenge for in vitro genotoxicology is the determination of the genotoxic mode of action of tested compounds. The quantification of the phosphorylation of the histones H3 (pH3) and H2AX (γH2AX) allows an efficient discrimination between aneugenic and clastogenic compounds. However, these two biomarkers do not permit to deduct the specific mechanisms involved in the action of clastogenic compounds. The aim of this study was to investigate other possible cellular biomarkers allowing differentiating clastogenic properties...
April 18, 2018: Environmental and Molecular Mutagenesis
https://www.readbyqxmd.com/read/29668047/miniaturization-of-the-microsuspension-salmonella-microsome-assay-in-agar-microplates
#6
José Ricardo R M Zwarg, Daniel A Morales, Bianca S Maselli, Werner Brack, Gisela A Umbuzeiro
The Salmonella/microsome assay (Ames test) is the most widely used mutagenicity test for the evaluation of pure chemicals and environmental samples. There are several versions of protocols available in the literature, including those that reduce the amount of sample needed for testing with liquid and agar media. The microsuspension version of the Salmonella/microsome assay is more sensitive than the standard protocol. It is performed using 5-times concentrated bacteria and less sample and S9 mixture, but still uses conventional Petri dishes (90 × 15 mm)...
April 18, 2018: Environmental and Molecular Mutagenesis
https://www.readbyqxmd.com/read/29667993/transition-metal-complexes-of-a-versatile-polyalkoxy-oxazolidine-based-ligand-derived-from-in-situ-cyclization
#7
Ayaan Saleem, Paulina A Kobielska, Klaus Harms, Maria G Katsikogianni, Richard Telford, Ghenadie Novitchi, Sanjit Nayak
One-pot reaction between 8-hydroxyquinoline-2-carboxaldehyde (HQC) and tris(hydroxymethyl)aminomethane (TRIS) followed by in situ cyclization yielded an oxazolidine based ligand which produced four mononuclear complexes of MnII(1), CoII(2), NiII(3), ZnII(4), a tetranuclear iron (FeIII4) complex (5) and a trinuclear cobalt (CoIICoIII2) complex (6). Magnetic studies show dominant antiferromagnetic interaction in tetranuclear iron (FeIII4) complex 5 and presence of the slow relaxation of magnetisation in 6. The compounds were also studied for their antibacterial properties...
April 18, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29667991/estimating-system-parameters-for-solvent-water-and-plant-cuticle-water-using-quantum-chemically-estimated-abraham-solute-parameters
#8
Yuzhen Liang, Tifany L Torralba-Sanchez, Dominic M Di Toro
Polyparameter Linear Free Energy Relationships (pp-LFERs) using Abraham system parameters have many useful applications. However, developing the Abraham system parameters depends on the availability and quality of the Abraham solute parameters. Using Quantum Chemically estimated Abraham solute Parameters (QCAP) is shown to produce pp-LFERs that have lower root mean square errors (RMSEs) of predictions for solvent-water partition coefficients than parameters that are estimated using other presently available methods...
April 18, 2018: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/29667925/massive-over-representation-of-solute-binding-proteins-sbps-from-the-tripartite-tricarboxylate-transporter-ttt-family-in-the-genome-of-the-%C3%AE-proteobacterium-rhodoplanes-sp-z2-yc6860
#9
Leonardo T Rosa, Vicki Springthorpe, Matheus E Bianconi, Gavin H Thomas, David J Kelly
Lineage-specific expansion (LSE) of protein families is a widespread phenomenon in many eukaryotic genomes, but is generally more limited in bacterial genomes. Here, we report the presence of 434 genes encoding solute-binding proteins (SBPs) from the tripartite tricarboxylate transporter (TTT) family, within the 8.2 Mb genome of the α-proteobacterium Rhodoplanes sp. Z2-YC6860, a gene family over-representation of unprecedented abundance in prokaryotes. Representing over 6 % of the total number of coding sequences, the SBP genes are distributed across the whole genome but are found rarely in low-GC islands, where the gene density for this family is much lower...
April 18, 2018: Microbial Genomics
https://www.readbyqxmd.com/read/29667825/structure-based-design-of-inhibitors-targeting-prfa-the-master-virulence-regulator-of-listeria-monocytogenes
#10
Martina Kulén, Marie Lindgren, Sabine Hansen, Andrew Gerard Cairns, Christin Grundström, Afshan Begum, Ingeborg van der Lingen, Kristoffer Brännström, Michael Hall, Uwe H Sauer, Jörgen Johansson, A Elisabeth Sauer-Eriksson, Fredrik Almqvist
Listeria monocytogenes is a bacterial pathogen that controls much of its virulence through the transcriptional regulator PrfA. In this study, we describe structure-guided design and synthesis of a set of PrfA inhibitors based on ring-fused 2-pyridone heterocycles. Our most effective compound decreased virulence factor expression, reduced bacterial uptake into eukaryotic cells, and improved survival of chicken embryos infected with L. monocytogenes compared to previously identified compounds. Crystal structures identified an intra-protein "tunnel" as the main inhibitor binding site (AI), where the compounds participate in an extensive hydrophobic network that restricts the protein's ability to form functional DNA-binding helix-turn-helix (HTH) motifs...
April 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29667823/luciferase-advisor-high-accuracy-model-to-flag-false-positive-hits-in-luciferase-hts-assays
#11
Dipan Ghosh, Uwe Koch, Kamyar Hadian, Michael Sattler, Igor V Tetko
Firefly luciferase is an enzyme that has found ubiquitous use in biological assays in high-throughput screening (HTS) campaigns. The inhibition of luciferase in such assays could lead to a false positive result. This issue has been known for a long time, and there have been significant efforts to identify luciferase inhibitors in order to enhance recognition of false positives in screening assays. However, although a large amount of publicly accessible luciferase counterscreen data is available, to date little effort has been devoted to building a chemoinformatic model that can identify such molecules in a given data set...
April 18, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29667821/antibacterial-dimeric-acylphloroglucinols-from-hypericum-japonicum
#12
Yan-Ping Li, Kun Hu, Xing-Wei Yang, Gang Xu
Nine dimeric acylphloroglucinols, including the new hyperjaponicols A-D (1-4), were isolated from the whole plant of Hypericum japonicum. The new structures were determined by the interpretation of NMR and MS data, and the relative configuration of the known compound, sarothralen C (5), was reassigned via NMR spectroscopic analysis and single-crystal X-ray diffraction data. The inhibitory activities of the isolates against four bacterial strains were evaluated, and compounds 1-4, 6, and 7 exhibited significant antibacterial activity with MIC values of 0...
April 18, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29667820/identification-of-ingol-and-rhamnofolane-diterpenoids-from-euphorbia-resinifera-and-their-abilities-to-induce-lysosomal-biosynthesis
#13
Ning-Dong Zhao, Xiao Ding, Yu Song, Dong-Qiong Yang, Hai-Li Yu, Tiwalade Adegoke Adelakun, Wen-Dan Qian, Yu Zhang, Ying-Tong Di, Fang Gao, Xiao-Jiang Hao, Shun-Lin Li
The phytochemical study of Euphorbia resinifera afforded 18 structurally diverse diterpenoids, including 14 new ingol-type diterpenoids, euphorblins A-N (1-14), a new rhamnofolane diterpenoid, euphorblin O (15), and three known analogues (16-18). The structures of these compounds were deduced using 2D NMR spectroscopy and NOE experiments. The structure of compound 1 was confirmed by single-crystal X-ray crystallography. The abilities of the compounds to enhance lysosomal biosynthesis were evaluated through LysoTracker Red staining...
April 18, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29667815/theranostic-pt-iv-conjugate-with-target-selectivity-for-androgen-receptor
#14
Xiaodong Qin, Lei Fang, Jian Zhao, Shaohua Gou
It is difficult to diagnose and treat castration-resistant prostate cancer (CRPC) which occurs due to the overexpression of androgen receptor (AR). Because there is a high level of AR in CRPC, we designed and prepared three Pt(IV)-based prodrugs targeting AR. Among them, compound 3, a three-in-one hybrid (an AR binding ligand, a cisplatin unit, and a coumarin moiety), was found to display satisfactory AR binding affinity and antagonist activity against androgen receptor, which could also be effectively internalized and visualized in LNCaP (AR+) cells...
April 18, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29667811/in-vitro-and-in-vivo-studies-of-the-electrophilicity-of-physcion-and-its-oxidative-metabolites
#15
Xiaotong Qin, Ying Peng, Jiang Zheng
Physcion (1,8-dihydroxy-3-methoxy-6-methyl-9,10-anthracenedione) is a bioactive component found in Polygoni Multiflori Radix (PMR) which has been widely used as traditional Chinese medicine. Unfortunately, studies showed hepatotoxicity of PMR during its clinical use. The mechanisms of its toxic action remain unknown. The major objectives of this study were to characterize oxidative metabolites of physcion in vitro and in vivo and to determine the electrophilicity of the parent compound and its oxidative metabolites...
April 18, 2018: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/29667782/hypofolins-a-l-ent-labdane-diterpenoids-from-the-roots-of-hypoestes-phyllostachya-pink-splash
#16
Bin Cheng, Lin-Fen Ding, Tong Yan, Zhang-Qiao Xie, Zhi-Jun Zhang, Liu-Dong Song, Xing-De Wu, Qin-Shi Zhao
Twelve new ent-labdane diterpenoids, hypofolins A-F (1-6) and hypofolins G-L (7a/7b, 8a/8b, and 9a/9b), were isolated from the roots of Hypoestes phyllostachya "Pink Splash". Their structures were elucidated by extensive 1D and 2D NMR spectroscopic and HRMS data. The absolute configurations of 1, 2, 5, and 7a/7b were determined by single crystal X-ray diffraction and ECD analysis, as well as chemical transformations. Compounds 7a/7b, 8a/8b, and 9a/9b were isolated as three pairs of interconverting mixture of two isomers between ketone and hemiketal types...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667768/quinazoline-based-hydroxamic-acids-design-synthesis-and-evaluation-of-histone-deacetylase-inhibitory-effects-and-cytotoxicity
#17
Doan Thanh Hieu, Duong Tien Anh, Hai Pham-The, Le-Thi-Thu Huong, Eun Jae Park, Jeong Eun Choi, Jong Soon Kang, Sang-Bae Han, Phan Thi Phuong Dung, Nguyen-Hai Nam
In our search for novel histone deacetylases inhibitors, we have designed and synthesized a series of novel hydroxamic acids and N-hydroxybenzamides incorporating quinazoline heterocycles (4a-i, 6a-i). Bioevaluation showed that these quinazoline-based hydroxamic acids and N-hydroxybenzamides were potently cytotoxic against three human cancer cell lines (SW620, colon; PC-3, prostate; NCI-H23, lung). In term of cytotoxicity, several compounds, e.g. 4g, 4c, 4g-i, 6c, and 6h, displayed from 5- up to 10-fold higher potency than SAHA (suberoylanilidehydroxamic acid, vorinostat)...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667758/synthesis-of-enantiomerically-enriched-drug-precursors-by-lactobacillus-paracasei-bd87e6-as-a-biocatalyst
#18
Selda Öksüz, Engin Şahin, Enes Dertli
Global sales of single enantiomeric drug products are growing at an alarming rate every year. A total of 7 bacterial strains were screened for their ability to reduce acetophenones to its corresponding alcohol. Among these strain Lactobacillus paracasei BD87E6 was found to be the most successful biocatalyst to reduce the ketones to the corresponding alcohols. The reaction conditions were systematically optimized for the reducing agent Lactobacillus paracasei BD87E6, which showed high enantioselectivity and conversion for the bioreduction...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667756/pharmacokinetic-profiling-of-anticancer-phytocompounds-using-computational-approach
#19
Ashish Sharma, Shilpa Sharma, Mansi Gupta, Shehnaz Fatima, Ravi Saini, Subhash Mohan Agarwal
INTRODUCTION: Natural products exhibit diverse scaffolds and are considered as suitable candidates for development of leads. However, poor pharmacokinetics often acts as a hindrance during the drug discovery process. OBJECTIVE: With a view of exploring the absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of plant-based anticancer compounds, open-access databases (NPACT, CancerHSP and TaxKB) were analysed to identify molecules having properties favourable for drug ability...
April 18, 2018: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/29667748/accumulation-and-sublethal-effects-of-triclosan-and-its-transformation-product-methyl-triclosan-in-the-earthworm-eisenia-andrei-exposed-to-environmental-concentrations-in-an-artificial-soil
#20
Fanny Chevillot, Mélanie Guyot, Mélanie Desrosiers, Nicole Cadoret, Éloïse Veilleux, Hubert Cabana, Jean-Philippe Bellenger
Municipal biosolids are increasingly used as a low-cost fertilizer in agricultural soil. Biosolids are contaminated by low concentrations (ng g-1 dw range) of a large variety of organic contaminants, such as triclosan (TCS). The effect of exposure to low concentrations of organic contaminants on soil biota remains largely undocumented. We evaluated the sublethal effects of TCS on the earthworm Eisenia andrei using an artificial soil amended with a nominal concentration of TCS of 50 ng g-1 dry weight soil...
April 18, 2018: Environmental Toxicology and Chemistry
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