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https://www.readbyqxmd.com/read/27913584/nitro-fatty-acid-pharmacokinetics-in-the-adipose-tissue-compartment
#1
Marco Fazzari, Nicholas K H Khoo, Steven R Woodcock, Diane K Jorkasky, Lihua Li, Francisco J Schopfer, Bruce A Freeman
Electrophilic nitro-fatty acids (NO2-FAs) promote adaptive and anti-inflammatory cell signaling responses as a result of an electrophilic character that supports post-translational protein modifications. A unique pharmacokinetic profile is expected for NO2-FAs because of an ability to undergo reversible reactions including Michael additions with biological cysteine-containing proteins and esterification into complex lipids. Herein we report via quantitative whole-body autoradiography analysis of rats gavaged with radiolabeled 10-nitro-[14C]oleic acid, preferential accumulation in adipose tissue over two weeks...
December 2, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27913142/candida-species-from-oral-cavity-of-hiv-infected-children-exhibit-reduced-virulence-factors-in-the-haart-era
#2
Maristela Barbosa Portela, Elaine Lima de Amorim, Adrielle Mangabeira Santos, José Alexandre da Rocha Curvelo, Karol de Oliveira Martins, Cauli Lima Capillé, Rosangela Maria de Araújo Soares, Gloria Fernanda Barbosa de Araújo Castro
This study aimed to assess, in vitro, the biofilm viability and the phospholipase and protease production of Candida spp. from the saliva of HIV infected children and healthy controls, and to correlate the results with the use of medical data. A total of 79 isolates were analyzed: 48 Candida albicans isolates (33/15) and 20 Candida parapsilosis sensu lato complex isolates (12/8) (from HIV/control patients, respectively), and 8 Candida krusei, 1 Candida tropicalis, 1 Candida dubliniensis and 1 Candida guilliermondii from HIV patients...
November 29, 2016: Microbial Pathogenesis
https://www.readbyqxmd.com/read/27912206/irisin-lowers-blood-pressure-by-improvement-of-endothelial-dysfunction-via-ampk-akt-enos-no-pathway-in-the-spontaneously-hypertensive-rat
#3
Jinjuan Fu, Yu Han, Jialiang Wang, Yukai Liu, Shuo Zheng, Lin Zhou, Pedro A Jose, Chunyu Zeng
BACKGROUND: Exercise is a major nonpharmacological treatment for hypertension, but its underlying mechanisms are still not completely elucidated. Irisin, a polypeptide containing 112 amino acids, which is secreted mainly by skeletal muscle cells during exercise, exerts a protective role in metabolic diseases, such as diabetes mellitus and obesity. Because of the close relationship between irisin and metabolic diseases, we hypothesized that irisin may play a role in the regulation of blood pressure...
October 26, 2016: Journal of the American Heart Association
https://www.readbyqxmd.com/read/27910842/comparison-of-hydrogen-bonds-and-diverse-weak-interactions-of-the-nitro-group-in-2-methyl-4-nitroanilinium-nitrate-bisulfate-and-two-hexafluoridosilicates-elementary-graph-set-approach
#4
Marek Daszkiewicz, Agnieszka Mielcarek
Crystal structures of (H2m4na)NO3 (1), (H2m4na)HSO4 (2), (H2m4na)2SiF6 (3) and (H2m4na)2SiF6·2H2O (4), where 2m4na = 2-methyl-4-nitroaniline, are presented. Two layers of interactions occur in the structures, N-H...O/F hydrogen bonds and interactions with the nitro group. Although diverse, hydrogen-bonding patterns are compared with each other by means of interrelations among elementary graph-set descriptors and descriptors of hydrogen-bonding patterns. Using mathematical relations, the gradual expansion of the ring patterns was shown in the crystal structures...
December 1, 2016: Acta Crystallographica Section B, Structural Science, Crystal Engineering and Materials
https://www.readbyqxmd.com/read/27908969/synthesis-and-evaluation-of-the-new-estrogen-receptor-%C3%AE-selective-radioligand-18f-fhnp-comparison-with-18f-fes
#5
Inês F Antunes, Aren van Waarde, Rudi A Dierckx, Elisabeth G E de Vries, Geke A P Hospers, Erik F de Vries
: Estrogen receptors (ER) are targets for endocrine treatment of estrogen-dependent cancers. The ER consists of 2 isoforms, ERα and ERβ, which have distinct biological functions. While activation of ERα stimulates cell proliferation and cell survival, ERβ promotes apoptosis. Positron emission tomography (PET) of ERα and ERβ levels could provide more insight in response to hormonal treatment. 16α-(18)F-Fluoro-17β-estradiol ((18)F-FES) is a PET tracer for ER with relative selectivity for ERα...
December 1, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#6
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27906419/sch-79797-a-selective-par1-antagonist-protects-against-ischemia-reperfusion-induced-arrhythmias-in-the-rat-hearts
#7
O Y Mohamed, A A Al-Masri, E A El Eter, R Lateef
OBJECTIVE: Thrombin is implicated in the genesis of arrhythmias and activation of thrombin receptors exacerbated ventricular arrhythmias following coronary artery ligation. The present study was designed to investigate the possible protective effect of the protease-activated receptor-1 antagonist, SCH79797 against ischemia and reperfusion arrhythmias in the rat heart. MATERIALS AND METHODS: Healthy male Wistar rats (250-350 g) were anesthetized with urethane. Coronary artery ligation was performed for 5 minutes followed by 10 minutes reperfusion...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27903843/downregulation-of-l-arginine-metabolism-in-dendritic-cells-induces-tolerance-to-exogenous-antigen
#8
Patricia U Simioni, Luis Gr Fernandes, Wirla Msc Tamashiro
Dendritic cells (DC) are potential tools for therapeutic applications and several strategies to generate tolerogenic DCs are under investigation. When activated by cytokines and microbial products, DCs express mediators that modulate immune responses. In this regard, the metabolites generated by the activities of inducible nitric oxide synthase (iNOS) and arginase in DCs seem to play important roles. Here, we evaluated the effects of adoptive transfer of DCs generated in vitro from bone marrow precursors (BMDC) modulated with L-NAME (Nω-nitro-L-arginine methyl ester) and NOHA (NG-Hydroxy-L-arginine), inhibitors of iNOS and arginase, respectively, upon the immune response of the wild type (BALB/c) and OVA-TCR transgenic (DO11...
November 30, 2016: International Journal of Immunopathology and Pharmacology
https://www.readbyqxmd.com/read/27902966/photo-induced-toxicity-and-oxidative-stress-responses-in-tigriopus-japonicus-exposed-to-nitro-polycyclic-aromatic-hydrocarbons-and-artificial-light
#9
Toshimitsu Onduka, Daisuke Ojima, Katsutoshi Ito, Kazuhiko Mochida, Mana Ito, Jiro Koyama, Kazunori Fujii
Photo-induced toxicity is an important phenomenon in ecotoxicology because sunlight reaches many organisms in their natural habitats. To elucidate whether sunlight enhances the toxicity of nitro-polycyclic aromatic hydrocarbons (nitro-PAHs), the acute toxicities of 10 nitro-PAHs and the related compound 1-nitropyrene (1-NP) to Tigriopus japonicus were assessed in darkness or under light conditions. In addition, the relationships among the toxicity of 1-NP to T. japonicus, lighting condition, and the concentration of reactive oxygen species (ROS) formed were investigated in the presence or absence of the ROS scavenger ascorbic acid in the test solutions...
November 27, 2016: Chemosphere
https://www.readbyqxmd.com/read/27901503/in-situ-hybridization-and-histopathological-observations-during-ostreid-herpesvirus-1-associated-mortalities-in-pacific-oysters-crassostrea-gigas
#10
Rudolfo Bueno, Matthew Perrott, Magda Dunowska, Cara Brosnahan, Colin Johnston
In a previous longitudinal study conducted during a mortality investigation associated with ostreid herpesvirus-1 (OsHV-1) microvariant in New Zealand Pacific oysters in 2010-2011, temporality of OsHV-1 nucleic acid detection by real-time PCR assay and onset of Pacific oyster mortality was observed. The present study further elucidated the role of OsHV-1 using an in situ hybridization (ISH) assay on sections of Pacific oysters collected from the same longitudinal study. Hybridization of the labelled probe with the target region of the OsHV-1 genome in infected cells was detected colorimetrically using nitro blue tetrazolium (NBT)...
November 22, 2016: Diseases of Aquatic Organisms
https://www.readbyqxmd.com/read/27899097/antinociception-of-petroleum-ether-fraction-derived-from-crude-methanol-extract-of-melastoma-malabathricum-leaves-and-its-possible-mechanisms-of-action-in-animal-models
#11
Z A Zakaria, E S Jaios, M H Omar, S Abd Rahman, S S A Hamid, S M Ching, L K Teh, M Z Salleh, S Deny, M Taher
BACKGROUND: Melastoma malabathricum L. (family Melastomaceae) has been traditionally used as remedies against various ailments including those related to pain. The methanol extract of M. malabathricum leaves has been proven to show antinociceptive activity. Thus, the present study aimed to determine the most effective fraction among the petroleum ether- (PEMM), ethyl acetate- (EAMM) and aqueous- (AQMM) fractions obtained through successive fractionation of crude, dried methanol extract of M...
November 29, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27898366/synthesis-characterization-and-serum-albumin-binding-studies-of-vitamin-k3-derivatives
#12
Murugesan Suganthi, Kuppanagounder P Elango
Synthesis, characterization and bovine serum albumin (BSA) binding properties of three derivatives of vitamin K3 have been described. Results of UV-Vis and fluorescence spectra indicate complexation between BSA and the ligands with conformational changes in protein, which is strongly supported by synchronous and three dimensional fluorescence studies. Addition of the ligands quenches the fluorescence of BSA which is accompanied by reduction in quantum yield (Ф) from 0.1010 to 0.0775-0.0986 range. Thermodynamic investigations reveal that hydrophobic interaction is the major binding force in the spontaneous binding of these ligands with BSA...
November 22, 2016: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/27898188/modern-approaches-to-discovering-new-hydroxynitrile-lyases-for-biocatalysis
#13
REVIEW
Santosh Kumar Padhi
Hydroxynitrile lyases (HNLs) have grown in importance from laboratory to industry due to their potential to catalyze stereoselective C-C bond-formation reactions in the synthesis of several chiral intermediates, such as enantiopure α-cyanohydrins, β-nitro alcohols, and their derivatives with multiple functional groups. With these wide applications, the demand for finding new HNLs has increased, and this has led to exploration not only of new HNLs but also of new ways to discover them. An exclusive review article on HNLs by Asano et al...
November 29, 2016: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/27897331/a-convenient-and-validated-enantiomer-separation-of-chiral-aliphatic-amines-as-nitrobenzoxadiazole-derivatives-on-polysaccharide-derived-chiral-stationary-phases-under-simultaneous-ultraviolet-and-fluorescence-detection
#14
Suraj Adhikari, Jong Seong Kang, Wonjae Lee
A convenient method using a fluorogenic agent, 4-chloro-7-nitro-1,2,3-benzoxadiazole (NBD-Cl), was developed for enantiomer separation of chiral aliphatic amines including amino alcohols by normal high-performance liquid chromatography. The enantiomer separation of chiral aliphatic amines as NBD derivatives was performed on six covalently bonded and four coated-type polysaccharide-derived chiral stationary phases (CSPs) under simultaneous ultraviolet (UV) and fluorescence detection (FLD). Among the covalently bonded CSPs, Chiralpak IE showed the best enantiomer separation for most analytes...
December 2016: Chirality
https://www.readbyqxmd.com/read/27896836/radiosynthesis-and-biological-evaluation-of-the-new-pde10a-radioligand-18-f-aq28a
#15
Sally Wagner, Rodrigo Teodoro, Winnie Deuther-Conrad, Mathias Kranz, Matthias Scheunemann, Steffen Fischer, Barbara Wenzel, Ute Egerland, Norbert Hoefgen, Jörg Steinbach, Peter Brust
Cyclic nucleotide phosphodiesterase 10A (PDE10A) regulates the level of the second messengers cAMP and cGMP in particular in brain regions assumed to be associated with neurodegenerative and psychiatric diseases. A better understanding of the pathophysiological role of the expression of PDE10A could be obtained by quantitative imaging of the enzyme by positron emission tomography (PET). Thus, in this study we developed, radiolabeled, and evaluated a new PDE10A radioligand, 8-bromo-1-(6-[(18) F]fluoropyridin-3-yl)-3,4-dimethylimidazo[1,5-a]quinoxaline ([(18) F]AQ28A)...
November 29, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27895421/carbon-monoxide-contributes-to-the-constipating-effects-of-granisetron-in-rat-colon
#16
Carmela Nacci, Margherita Fanelli, Maria Assunta Potenza, Valentina Leo, Monica Montagnani, Maria Antonietta De Salvia
AIM: To investigate the mechanisms underlying the potential contribution of the heme oxygenase/carbon monoxide (HO/CO) pathway in the constipating effects of granisetron. METHODS: For in vivo studies, gastrointestinal motility was evaluated in male rats acutely treated with granisetron [25, 50, 75 μg/kg/subcutaneous (sc)], zinc protoporphyrin IX [ZnPPIX, 50 μg/kg/intraperitoneal (ip)] and hemin (50 μmol/L/kg/ip), alone or in combination. For in vitro studies, the contractile neurogenic response to electrical field stimulation (EFS, 3, 5, 10 Hz, 14 V, 1 ms, pulse trains lasting 10 s), as well as the contractile myogenic response to acetylcholine (ACh, 0...
November 14, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27895230/an-arginase-1-snp-that-protects-against-the-development-of-pulmonary-hypertension-in-bronchopulmonary-dysplasia-enhances-no-mediated-apoptosis-in-lymphocytes
#17
Jennifer K Trittmann, Yi Jin, Louis G Chicoine, Yusen Liu, Bernadette Chen, Leif D Nelin
Arginase and nitric oxide synthase (NOS) share a common substrate, l-arginine, and have opposing effects on vascular remodeling. Arginase is the first step in polyamine and proline synthesis necessary for cellular proliferation, while NO produced from NOS promotes apoptosis. Previously, we identified a single nucleotide polymorphism (SNP) in the arginase-1 (ARG1) gene, rs2781666 (T-allele) that was associated with a decreased risk for developing pulmonary hypertension (PH) in a cohort of infants with bronchopulmonary dysplasia (BPD)...
November 2016: Physiological Reports
https://www.readbyqxmd.com/read/27889629/terminal-functionalized-thiourea-containing-dipeptides-as-multidrug-resistance-reversers-that-target-20s-proteasome-and-cell-proliferation
#18
Jian-Mei Qin, Ri-Zhen Huang, Gui-Yang Yao, Zhi-Xin Liao, Ying-Ming Pan, Heng-Shan Wang
A series of inhibitors of 20S proteasome based on terminal functionalized dipeptide derivatives containing the thiourea moiety were synthesized and evaluated for inhibition of 20S proteasome and the effects of multidrug-resistance reversers. These compounds exhibited significant selectivity to the β5-subunit of the human 20S proteasome with IC50 values at submicromolar concentrations. A docking study of the most active compound 6i revealed key interactions between 6i and the active site of the 20S proteasome in which the thiourea moiety and a nitro group were important for improving activity...
November 11, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27886546/biology-oriented-drug-synthesis-biods-in%C3%A2-vitro-%C3%AE-glucuronidase-inhibitory-and-in-silico-studies-on-2-2-methyl-5-nitro-1h-imidazol-1-yl-ethyl-aryl-carboxylate-derivatives
#19
Uzma Salar, Khalid Mohammed Khan, Muhammad Taha, Nor Hadiani Ismail, Basharat Ali, Qurat-Ul-Ain, Shahnaz Perveen, Mehreen Ghufran, Abdul Wadood
Current study is based on the biology-oriented drug synthesis (BIODS) of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl carboxylate derivatives 1-26, by treating metronidazole with different aryl and hetero-aryl carboxylic acids in the presence of 1,1'-carbonyl diimidazole (CDI) as a coupling agent. Structures of all synthetic derivatives were confirmed with the help of various spectroscopic techniques such as EI-MS, (1)H -NMR and (13)C NMR. CHN elemental analyses were also found in agreement with the calculated values...
November 14, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27885780/synthesis-and-investigation-of-advanced-energetic-materials-based-on-bispyrazolylmethanes
#20
Dennis Fischer, Jennifer L Gottfried, Thomas M Klapötke, Konstantin Karaghiosoff, Jörg Stierstorfer, Tomasz G Witkowski
Herein we present the preparation and characterization of three new bispyrazolyl-based energetic compounds with great potential as explosive materials. The reaction of sodium 4-amino-3,5-dinitropyrazolate (5) with dimethyl iodide yielded bis(4-amino-3,5-dinitropyrazolyl)methane (6), which is a secondary explosive with high heat resistance (Tdec =310 °C). The oxidation of this compound afforded bis(3,4,5-trinitropyrazolyl)methane (7), which is a combined nitrogen- and oxygen-rich secondary explosive with very high theoretical and estimated experimental detonation performance (Vdet (theor)=9304 m s(-1) versus Vdet (exp)=9910 m s(-1) ) in the range of that of CL-20...
November 25, 2016: Angewandte Chemie
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