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https://www.readbyqxmd.com/read/28645211/akr1c3-mediated-adipose-androgen-generation-drives-lipotoxicity-in-women-with-polycystic-ovary-syndrome
#1
Michael W O'Reilly, Punith Kempegowda, Mark Walsh, Angela E Taylor, Konstantinos N Manolopoulos, J William Allwood, Robert K Semple, Daniel Hebenstreit, Warwick B Dunn, Jeremy W Tomlinson, Wiebke Arlt
Context: Polycystic ovary syndrome (PCOS) is a prevalent metabolic disorder, occurring in up to 10% of women of reproductive age. PCOS is associated with insulin resistance and cardiovascular risk. Androgen excess is a defining feature of PCOS and has been suggested as causally associated with insulin resistance; however, mechanistic evidence linking both is lacking. We hypothesized that adipose tissue is an important site linking androgen activation and metabolic dysfunction in PCOS...
June 22, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28645051/enantioselective-disturbance-of-chiral-herbicide-dichlorprop-to-nitrogen-metabolism-of-arabidopsis-thaliana-regular-analysis-and-stable-isotope-attempt
#2
Zunwei Chen, Jia Wang, Siyu Chen, Yuezhong Wen
As the most essential element, nitrogen play a pivotal role in plant physiological process, which is susceptible to contaminants. However, the enantioselective effects of chiral herbicides on nitrogen metabolism have not been comprehensively understood. In this study, effects of chiral herbicide dichlorprop (DCPP) on the nitrogen behaviors in Arabidopsis thaliana were investigated. The results revealed that the uptakes of inorganic nitrogen (NO3(-) and NH4(+)) were preferentially impacted by herbicidal active (R)-DCPP, where the transportation of beneficial NO3(-) was inhibited but the toxic NH4(+) was accumulated...
June 20, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28645002/synthesis-of-s-linked-trisaccharide-glycal-of-derhodinosylurdamycin-a-discovery-of-alkyl-thiocyanate-as-an-efficient-electrophile-for-stereoselective-sulfenylation-of-2-deoxy-glycosyl-lithium
#3
Padam P Acharya, Kedar N Baryal, Cristin E Reno, Jianglong Zhu
Stereoselective synthesis of S-linked trisaccharide glycal of angucycline antitumor antibiotic derhodinosylurdamycin A is described. The synthesis has been accomplished employing our previously reported umpolung S-glycosylation strategy - stereoselective sulfenylation of 2-deoxy glycosyl lithium. It was found that sugar-derived thiocyanate was a better electrophile than corresponding asymmetric disulfide in this type of stereoselective sulfenylation.
June 15, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28644990/global-transcriptional-response-of-escherichia-coli-mg1655-cells-exposed-to-the-oxygenated-monoterpenes-citral-and-carvacrol
#4
Beatriz Chueca, Elisa Pérez-Sáez, Rafael Pagán, Diego García-Gonzalo
DNA microarrays were used to study the mechanism of bacterial inactivation by carvacrol and citral. After 10-min treatments of Escherichia coli MG1655 cells with 100 and 50ppm of carvacrol and citral, 76 and 156 genes demonstrated significant transcriptional differences (p≤0.05), respectively. Among the up-regulated genes after carvacrol treatment, we found gene coding for multidrug efflux pumps (acrA, mdtM), genes related to phage shock response (pspA, pspB, pspC, pspD, pspF and pspG), biosynthesis of arginine (argC, argG, artJ), and purine nucleotides (purC, purM)...
June 20, 2017: International Journal of Food Microbiology
https://www.readbyqxmd.com/read/28644909/a-highly-efficient-synthesis-of-z-macrocycles-using-stereoretentive-ruthenium-based-metathesis-catalysts
#5
Tonia Sarah Ahmed, Robert H Grubbs
A highly efficient, Z-selective ring-closing metathesis system for the formation of macrocycles using a stereoretentive, ruthenium-based catalyst supported by a dithiolate ligand is reported. This catalyst is demonstrated to be remarkably active as observed in initiation experiments showing complete catalyst initiation at -20 °C within 10 min. Macrocyclization reactions generated Z-products from easily accessible diene starting materials bearing a Z-olefin moiety. This stereoretentive approach provides a more efficient and selective route to Z-macrocyles than in previously reported systems...
June 23, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28644884/ligand-induced-rapid-skeletal-muscle-atrophy-in-hsa-fv2e-perk-transgenic-mice
#6
Masato Miyake, Masashi Kuroda, Hiroshi Kiyonari, Kenji Takehana, Satoshi Hisanaga, Masatoshi Morimoto, Jun Zhang, Miho Oyadomari, Hiroshi Sakaue, Seiichi Oyadomari
BACKGROUND: Formation of 43S and 48S preinitiation complexes plays an important role in muscle protein synthesis. There is no muscle-wasting mouse model caused by a repressed 43S preinitiation complex assembly. OBJECTIVE: The aim of the present study was to develop a convenient mouse model of skeletal muscle wasting with repressed 43S preinitiation complex assembly. MATERIAL AND METHODS: A ligand-activatable PERK derivative Fv2E-PERK causes the phosphorylation of eukaryotic initiation factor 2α (eIF2α), which inhibits 43S preinitiation complex assembly...
2017: PloS One
https://www.readbyqxmd.com/read/28644880/o-glcnacylation-mediates-the-control-of-cytosolic-phosphoenolpyruvate-carboxykinase-activity-via-pgc1%C3%AE
#7
Pedro Latorre, Luis Varona, Carmen Burgos, José A Carrodeguas, Pascual López-Buesa
PGC1α is a coactivator of many transcription factors and cytosolic phosphoenolpyruvate carboxykinase (PCK1) is a key enzyme for gluconeogenesis. PGC1α interacts with the transcription factor PPARγ to stimulate PCK1 expression and thus de novo glucose synthesis. These proteins are not only important for central energy metabolism but also for supplying intermediates for other metabolic pathways, including lipidogenesis and protein synthesis and might therefore be important factors in the ethiopathogenesis of metabolic disorders like diabetes but also in other pathologies like cancer...
2017: PloS One
https://www.readbyqxmd.com/read/28644859/grief-interventions-for-people-bereaved-by-suicide-a-systematic-review
#8
Katja Linde, Julia Treml, Jana Steinig, Michaela Nagl, Anette Kersting
BACKGROUND: Adaption to the loss of a loved one due to suicide can be complicated by feelings of guilt, shame, responsibility, rejection, and stigmatization. Therefore people bereaved by suicide have an increased risk for developing complicated grief which is related to negative physical and mental disorders and an increased risk for suicidal behavior. Grief interventions are needed for this vulnerable population. The aim of this systematic review was to provide an overview of the current state of evidence concerning the effectiveness of interventions that focus on grief for people bereaved by suicide...
2017: PloS One
https://www.readbyqxmd.com/read/28644754/expression-of-enzymes-related-to-glucose-metabolism-in-non-small-cell-lung-cancer-and-prognosis
#9
Alexandra Giatromanolaki, Efthimios Sivridis, Stella Arelaki, Michael I Koukourakis
Purpose/Aim: Cancer cells are addicted to glycolytic anaerobic pathways, in presence or in absence of a functional Krebs' cycle (phenomenon Warburg). This metabolic predilection relies on both extracellular (impaired vascularization and oxygenation) and intracellular (oncogenic activation of genes) causes. MATERIALS AND METHODS: We investigated the expression and prognostic relevance of enzymes involved in the glucose absorption and metabolism, monocarboxylate transporter (MCT) expression, MCT1 and MCT2, pentose pathway (Glucose-6-phospahte dehydrogenase G6PD), glycogene synthesis (glycogene synthase GYS1), glycolysis (Hexokinase HXKII, phosphofructokinase PFK1, fructose biphosphate aldolase), fate of pyruvate (pyruvate dehydrogenase PDH, phosphorylated pPDH, PDH kinase PDK1, lactate dehydrogenase LDH5 and LDH1) and key Kreb's cycle enzymes (citrate synthase CSynth and isocitrate dehydrogenase IDH)...
June 23, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/28644732/lipophilicity-and-biomimetic-properties-to-support-drug-discovery
#10
Fotios Tsopelas, Constantinos Giaginis, Anna Tsantili-Kakoulidou
Lipophilicity, expressed as the octanol-water partition coefficient, constitutes the most important property in drug action, influencing both pharmacokinetic and pharmacodynamics processes as well as drug toxicity. On the other hand, biomimetic properties defined as the retention outcome on HPLC columns containing a biological relevant agent, provide a considerable advance for rapid experimental -based estimation of ADME properties in early drug discovery stages. Areas covered: This review highlights the paramount importance of lipophilicity in almost all aspects of drug action and safety...
June 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28644621/recent-advances-in-the-synthesis-of-hydantoins-the-state-of-the-art-of-a-valuable-scaffold
#11
Laure Konnert, Evelina Colacino
The review highlights the hydantoin syntheses presented from the point of view of the preparation methods. Novel synthetic routes to various hydantoin structures, the advances brought to the classical methods in the aim of producing more sustainable and environmentally friendly procedures for the preparation of these biomolecules, and a critical comparison of the different synthetic approaches developed in the last twelve years are also described. The review is composed of 95 schemes, 8 figures and 528 references for the last 12 years and includes the description of the hydantoin-based marketed drugs and clinical candidates...
June 23, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28644550/biphasic-liquid-crystal-and-the-simultaneous-measurement-of-isotropic-and-anisotropic-parameters-by-spatially-resolved-nmr-spectroscopy
#12
Malin Reller, Svenja Wesp, Martin R M Koos, Michael Knut Reggelin, Burkhard Luy
Residual dipolar couplings and other anisotropic NMR parameters are powerful tools for molecular structure elucidation when conventional techniques do not suffice. With current liquid crystalline preparations, it is necessary to prepare two samples to extract isotropic and anisotropic data from spectra and to derive the residual dipolar couplings. Here, we present the preparation, measurement, and interpretation of a novel biphasic liquid crystalline phase where a single sample can be used to generate both isotropic and anisotropic data...
June 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28644514/polylutidines-multifunctional-surfaces-via-vapor-based-polymerization-of-substituted-pyridinophanes
#13
Joerg Lahann, Florence Bally-Le Gall, Christoph Hussal, Joshua Kramer, Kenneth Chang, Ramya Kumar, Vanessa Trouillet, Martin Nieger, Stefan Braese, Thomas Eyster, Amy Baek
We report a new class of functionalized polylutidine polymers that are prepared via chemical vapor deposition polymerization of substituted [2](1,4)benzeno[2](2,5)pyridinophanes. To prepare sufficient monomer for CVD polymerization, a new synthesis route for ethynylpyridinophane has been developed in three steps with an overall yield of 59%. Subsequent CVD polymerization yielded well-defined films of poly(2,5-lutidinylene-co-p-xylylene) and poly(4-ethynyl-2,5-lutidinylene-co-p-xylylene). All polymers were characterized by IRRAS, ellipsometry, contact angle and XPS...
June 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28644481/redox-controlled-potassium-intercalation-into-two-polyaromatic-hydrocarbon-solids
#14
F Denis Romero, M J Pitcher, C I Hiley, G F S Whitehead, S Kar, A Y Ganin, D Antypov, C Collins, M S Dyer, G Klupp, R H Colman, K Prassides, M J Rosseinsky
Alkali metal intercalation into polyaromatic hydrocarbons (PAHs) has been studied intensely after reports of superconductivity in a number of potassium- and rubidium-intercalated materials. There are, however, no reported crystal structures to inform our understanding of the chemistry and physics because of the complex reactivity of PAHs with strong reducing agents at high temperature. Here we present the synthesis of crystalline K2Pentacene and K2Picene by a solid-solid insertion protocol that uses potassium hydride as a redox-controlled reducing agent to access the PAH dianions, and so enables the determination of their crystal structures...
July 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28644471/polycyclic-aromatic-hydrocarbons-synthesis-successes
#15
Roser Valentí, Stephen M Winter
No abstract text is available yet for this article.
June 23, 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28644470/rapid-heteroatom-transfer-to-arylmetals-utilizing-multifunctional-reagent-scaffolds
#16
Hongyin Gao, Zhe Zhou, Doo-Hyun Kwon, James Coombs, Steven Jones, Nicole Erin Behnke, Daniel H Ess, László Kürti
Arylmetals are highly valuable carbon nucleophiles that are readily and inexpensively prepared from aryl halides or arenes and widely used on both laboratory and industrial scales to react directly with a wide range of electrophiles. Although C-C bond formation has been a staple of organic synthesis, the direct transfer of primary amino (-NH2) and hydroxyl (-OH) groups to arylmetals in a scalable and environmentally friendly fashion remains a formidable synthetic challenge because of the absence of suitable heteroatom-transfer reagents...
July 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28644411/on-the-reaction-of-carbonyl-diphosphonic-acid-with-hydroxylamine-and-o-alkylhydroxylamines-unexpected-degradation-of-p-c-p-bridge
#17
Olga A Khomich, Dmitry V Yanvarev, Roman A Novikov, Alexey B Kornev, Elina Puljulla, Jouko Vepsäläinen, Alex R Khomutov, Sergey N Kochetkov
Derivatives of methylenediphosphonic acid possess wide spectra of biological activities and are used in enzymology as research tools as well as in practical medicine. Carbonyl diphosphonic acid is a promising starting building block for synthesis of functionally substituted methylenediphosphonates. Investigation of the interaction of carbonyl diphosphonic acid with hydroxylamine clearly demonstrates that it is impossible to isolate oxime within the pH range 2-12, while only cyanophosphonic and phosphoric acids are the products of the fast proceeding Beckmann-like fragmentation...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644383/use-of-ultrasonication-technology-for-the-increased-production-of-plant-secondary-metabolites
#18
REVIEW
Md Mohidul Hasan, Tufail Bashir, Hanhong Bae
Plant secondary metabolites (PSMs) provide taste, color, odor, and resistance to plants, and they are also used to treat cancer and cardiovascular diseases. Synthesis of PSMs in plants is stimulated in response to different forms of external stress. Use of ultrasonication (US) to clean or decontaminate fruits and vegetables leads to physical stress that finally results in the accumulation of PSMs. US can stimulate accumulation of taxol, ginsenoside saponins, shikonin, and resveratrol, e.g., up to 319-fold increase of resveratrol synthesis has been observed in grape due to US...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644367/oral-cholic-acid-is-efficacious-and-well-tolerated-in-patients-with-bile-acid-synthesis-and-zellweger-spectrum-disorders
#19
James E Heubi, Kevin E Bove, Kenneth D R Setchell
BACKGROUND/AIMS: Patients with bile acid synthesis disorders (BASD) due to single enzyme defects (SED) or Zellweger spectrum disorders (ZSD) accumulate hepatotoxic atypical bile acids resulting in potentially fatal progressive liver disease. We evaluated the efficacy and safety of oral cholic acid in patients with BASD. METHODS: In this phase 3, open-label, single-arm, nonrandomized, noncomparative study conducted over 18 years, patients were administered cholic acid orally 10 to 15 mg/kg/day...
June 21, 2017: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/28644060/lytic-transglycosylases-concinnity-in-concision-of-the-bacterial-cell-wall
#20
David A Dik, Daniel R Marous, Jed F Fisher, Shahriar Mobashery
The lytic transglycosylases (LTs) are bacterial enzymes that catalyze the non-hydrolytic cleavage of the peptidoglycan structures of the bacterial cell wall. They are not catalysts of glycan synthesis as might be surmised from their name. Notwithstanding the seemingly mundane reaction catalyzed by the LTs, their lytic reactions serve bacteria for a series of astonishingly diverse purposes. These purposes include cell-wall synthesis, remodeling, and degradation; for the detection of cell-wall-acting antibiotics; for the expression of the mechanism of cell-wall-acting antibiotics; for the insertion of secretion systems and flagellar assemblies into the cell wall; as a virulence mechanism during infection by certain Gram-negative bacteria; and in the sporulation and germination of Gram-positive spores...
June 23, 2017: Critical Reviews in Biochemistry and Molecular Biology
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