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https://www.readbyqxmd.com/read/28527405/synthesis-and-structure-activity-relationships-of-novel-fused-ring-analogues-of-q203-as-antitubercular-agents
#1
Sunhee Kang, Young Mi Kim, Heekyung Jeon, Sejin Park, Min Jung Seo, Saeyeon Lee, Dongsik Park, Jiyeon Nam, Seokwoo Lee, Kiyean Nam, Sanghee Kim, Jaeseung Kim
A set of fused ring analogues of a new antitubercular agent, Q203, was designed and synthesized. To reduce the lipophilicity of Q203 caused by linearly extended side chains, shorter and heteroatoms containing fused rings were introduced into the side chain region. Antitubercular activity was tested against H37Rv-GFP replicating in liquid broth culture medium (extracellular) and within macrophages (intracellular). Many analogues showed potent extracellular activities as well as intracellular activities without cytotoxicity...
May 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28527391/melanin-concentrating-hormone-and-sleep
#2
REVIEW
Jozelia Gomes Pacheco Ferreira, Jackson Cioni Bittencourt, Antoine Adamantidis
The melanin-concentrating hormone (MCH) is an essential neuromodulator involved with homeostatic regulation and motivated behaviors. The majority of MCH neurons are localized within the zona incerta, lateral hypothalamic and incerto-hypothalamic areas but others regions, as the olfactory turbecle, the laterodorsal tegmental nucleus, the paramediam pontine reticular formation and the medial preoptic area, can also express the peptide depending on the gender and metabolic state of the animal. If the MCH on these novel sites of expression are also related with the control of wake-sleep cycle will be discuss in this review...
May 17, 2017: Current Opinion in Neurobiology
https://www.readbyqxmd.com/read/28527383/tributyltin-and-triphenyltin-exposure-promotes-in-vitro-adipogenic-differentiation-but-alters-the-adipocyte-phenotype-in-rainbow-trout
#3
Esmail Lutfi, Natàlia Riera-Heredia, Marlon Córdoba, Cinta Porte, Joaquim Gutiérrez, Encarnación Capilla, Isabel Navarro
Numerous environmental pollutants have been identified as potential obesogenic compounds affecting endocrine signaling and lipid homeostasis. Among them, well-known organotins such as tributyltin (TBT) and triphenyltin (TPT), can be found in significant concentrations in aquatic environments. The aim of the present study was to investigate in vitro the effects of TBT and TPT on the development and lipid metabolism of rainbow trout (Onchorynchus mykiss) primary cultured adipocytes. Results showed that TBT and TPT induced lipid accumulation and slightly enhanced peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT enhancer binding protein alpha (C/EBPα) protein expression when compared to a control, both in the presence or absence of lipid mixture...
May 8, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28527370/atherosclerotic-dyslipidemia-revealed-by-plasma-lipidomics-on-apoe-mice-fed-a-high-fat-diet
#4
Yanyan Chen, Shiyuan Wen, Miaomiao Jiang, Yan Zhu, Liqin Ding, Hong Shi, Pengzhi Dong, Jing Yang, Yue Yang
BACKGROUND AND AIMS: The pathological process of atherosclerosis is closely related to lipid accumulation at arterial wall caused by lipoproteins transporting lipids through blood. In this study, we investigate the lipid composition in the plasma of apolipoprotein E deficient (ApoE(-/-)) mice fed a high-fat diet to reveal atherosclerosis-induced dyslipidemia. METHODS: ApoE(-/-) and corresponding wild-type C57BL/6J mice were used as the pathology model and control, respectively, and were fed a high-fat or normal diet...
May 11, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28527344/harnessing-plant-metabolic-diversity
#5
REVIEW
Charlie Owen, Nicola J Patron, Ancheng Huang, Anne Osbourn
Advances in DNA sequencing and synthesis technologies in the twenty-first century are now making it possible to build large-scale pipelines for engineering plant natural product pathways into heterologous production species using synthetic biology approaches. The ability to decode the chemical potential of plants by sequencing their transcriptomes and/or genomes and to then use this information as an instruction manual to make drugs and other high-value chemicals is opening up new routes to harness the vast chemical diversity of the Plant Kingdom...
May 17, 2017: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/28527336/title-potassium-application-regulates-nitrogen-metabolism-and-osmotic-adjustment-in-cotton-gossypium-hirsutum-l-functional-leaf-under-drought-stress
#6
Rizwan Zahoor, Wenqing Zhao, Muhammad Abid, Haoran Dong, Zhiguo Zhou
To evaluate the role of potassium (K) in maintaining nitrogen metabolism and osmotic adjustment development of cotton functional leaves to sustain growth under soil drought and rewatering conditions, the plants of two cotton cultivars Siza 3 (low-K sensitive) and Simian 3 (low-K tolerant), were grown under three different K rates (K0, K1, and K2; 0, 150, and 300kgK2Oha(-1), respectively) and exposed to drought stress with 40±5% soil relative water content (SRWC). The drought stress was applied at flowering stage by withholding water for eight days followed by rewatering to a well-watered level (75±5% SRWC)...
May 4, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28527333/transcriptome-wide-analysis-of-jasmonate-treated-by-2-cells-reveals-new-transcriptional-regulators-associated-with-alkaloid-formation-in-tobacco
#7
Yuping Yang, Pengcheng Yan, Che Yi, Wenzheng Li, Yuhui Chai, Lingling Fei, Ping Gao, Heping Zhao, Yingdian Wang, Michael P Timko, Bingwu Wang, Shengcheng Han
Jasmonates (JAs) are well-known regulators of stress, defence, and secondary metabolism in plants, with JA perception triggering extensive transcriptional reprogramming, including both activation and/or repression of entire metabolic pathways. We performed RNA sequencing based transcriptomic profiling of tobacco BY-2 cells before and after treatment with methyl jasmonate (MeJA) to identify novel transcriptional regulators associated with alkaloid formation. A total of 107,140 unigenes were obtained through de novo assembly, and at least 33,213 transcripts (31%) encode proteins, in which 3419 transcription factors (TFs) were identified, representing 72 gene families, as well as 840 transcriptional regulators (TRs) distributed among 19 gene families...
May 4, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28527304/additive-effect-of-non-alcoholic-fatty-liver-disease-on-the-development-of-diabetes-in-individuals-with-metabolic-syndrome
#8
Ji Cheol Bae, Soo Kyoung Kim, Ji Min Han, Sam Kwon, Da Young Lee, Jihyun Kim, Se Eun Park, Cheol-Young Park, Won-Young Lee, Ki-Won Oh, Sung-Woo Park, Eun Jung Rhee
INTRODUCTION: Non-alcoholic fatty liver disease (NAFLD) is considered as the hepatic manifestation of the metabolic syndrome (MetS), with insulin resistance as the common pathophysiology. In a current longitudinal cohort study, we evaluated the separate and combined effects of MetS and NAFLD on incident diabetes risk. METHODS: Participants were categorized into four groups on the basis of the presence of NAFLD and MetS at baseline (i.e., with NAFLD, with MetS, with both, or without either)...
May 5, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28527257/-polyclonal-antibodies-against-recombinant-dengue-virus-ns3-protein
#9
Liliana Morales, Myriam L Velandia, María Angélica Calderon, Jaime E Castellanos, Jacqueline Chaparro-Olaya
INTRODUCTION: Dengue is a disease caused by one of four serotypes of the dengue virus (DENV) and is endemic in approximately 130 countries. The incidence of dengue has increased dramatically in recent decades, as well as the frequency and magnitude of outbreaks. Despite all efforts, there are no prophylactic or therapeutic treatments for the disease. Accordingly, research on the processes governing the DENV infection cycle is essential to develop vaccines or antiviral therapies. One of themost attractive DENV molecules to investigate is nonstructural protein 3 (NS3), which is essential for viral replication and a major immune target for infection...
January 24, 2017: Biomédica: Revista del Instituto Nacional de Salud
https://www.readbyqxmd.com/read/28527212/apolipoprotein-e4-gender-body-mass-index-inflammation-insulin-resistance-and-air-pollution-interactions-recipe-for-alzheimer-s-disease-development-in-mexico-city-young-females
#10
Lilian Calderón-Garcidueñas, Suzanne M de la Monte
Given the epidemiological trends of increasing Alzheimer's disease (AD) and growing evidence that exposure and lifestyle factors contribute to AD risk and pathogenesis, attention should be paid to variables such as air pollution, in order to reduce rates of cognitive decline and dementia. Exposure to fine particulate matter (PM2.5) and ozone (O3) above the US EPA standards is associated with AD risk. Mexico City children experienced pre- and postnatal high exposures to PM2.5, O3, combustion-derived iron-rich nanoparticles, metals, polycyclic aromatic hydrocarbons, and endotoxins...
May 17, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28527205/moderate-physical-activity-is-associated-with-cerebral-glucose-metabolism-in-adults-at-risk-for-alzheimer-s-disease
#11
Ryan J Dougherty, Stephanie A Schultz, Taylor K Kirby, Elizabeth A Boots, Jennifer M Oh, Dorothy Edwards, Catherine L Gallagher, Cynthia M Carlsson, Barbara B Bendlin, Sanjay Asthana, Mark A Sager, Bruce P Hermann, Bradley T Christian, Sterling C Johnson, Dane B Cook, Ozioma C Okonkwo
The objective of this study was to investigate the relationship between accelerometer-measured physical activity (PA) and glucose metabolism in asymptomatic late-middle-aged adults. Ninety-three cognitively healthy late-middle-aged adults from the Wisconsin Registry for Alzheimer's Prevention participated in this cross-sectional study. They underwent 18F-fluorodeoxyglucose positron emission tomography (FDG-PET) imaging and wore an accelerometer (ActiGraph GT3X+) to measure free-living PA. Accelerometer data yielded measures of light (LPA), moderate (MPA), and vigorous (VPA) intensity PA...
May 17, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28527179/making-time-conservation-of-biological-clocks-from-fungi-to-animals
#12
Jay C Dunlap, Jennifer J Loros
The capacity for biological timekeeping arose at least three times through evolution, in prokaryotic cyanobacteria, in cells that evolved into higher plants, and within the group of organisms that eventually became the fungi and the animals. Neurospora is a tractable model system for understanding the molecular bases of circadian rhythms in the last of these groups, and is perhaps the most intensively studied circadian cell type. Rhythmic processes described in fungi include growth rate, stress responses, developmental capacity, and sporulation, as well as much of metabolism; fungi use clocks to anticipate daily environmental changes...
May 2017: Microbiology Spectrum
https://www.readbyqxmd.com/read/28527155/status-of-laparoscopic-sleeve-gastrectomy-in-china-a-national-survey
#13
Shibo Lin, Wei Guan, Pankaj Hans, Hui Liang
BACKGROUND: Laparoscopic sleeve gastrectomy (LSG) is a favorable bariatric procedure. This study evaluated the status of LSG in China. METHODS: During the 4(th) International Forum of Bariatric and Metabolic Surgery in May 2016, Nanjing China, an on-the-spot questionnaire was filled out by 105 attending surgeons with experience of LSG. The feedback data was collected and analyzed. RESULTS: For preoperative preparations, surgeons preferred blood glucose control with insulin (61...
May 19, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28527150/development-of-in-silico-protocols-to-predict-structural-insights-into-the-metabolic-activation-pathways-of-xenobiotics
#14
M Kalim A Khan, Salman Akhtar, Jamal M Arif
To establish in silico model to predict the structural insight into the metabolic bioactivation pathway of xenobiotics, we considered two specific and one non-specific mammary procarcinogen [e.g., dibenzo[a,l]pyrene (DBP), 7,12-dimethylbenz[a]anthracene (DMBA), and benzo[a]pyrene (BP)]. The CYP1A1, 1B1, 2C9, 1A2 and 2B6 reported in wet-lab studies to actively metabolize DBP also showed strong binding energies (kcal/mol) of -11.50, -10.67, -10.37, -9.76 and -9.72, respectively, with inhibition constants ranging between 0...
May 19, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28527127/evaluation-of-heparg-cells-for-the-assessment-of-indirect-drug-induced-hepatotoxicity-using-inh-as-a-model-substance
#15
Anika Mann, Thomas Pelz, Knut Rennert, Alexander Mosig, Michael Decker, Amelie Lupp
HepaRG cells are widely used as an in vitro model to assess drug-induced hepatotoxicity. However, only few studies exist so far regarding their suitability to detect the effects of drugs requiring a preceding activation via the cytochrome P450 (CYP) system. A prototypic substance is the anti-tuberculosis agent INH, which is metabolized into N-acetylhydrazine, which then triggers hepatotoxicity. Therefore, the aim of the present study was to test if this effect can also be detected in HepaRG cells and if it can be counteracted by the known hepatoprotectant silibinin...
May 19, 2017: Human Cell
https://www.readbyqxmd.com/read/28527122/effects-of-cigarette-smoke-exposure-during-suckling-on-food-intake-fat-mass-hormones-and-biochemical-profile-of-young-and-adult-female-rats
#16
Patricia Cristina Lisboa, Patricia Novaes Soares, Thamara Cherem Peixoto, Janaine Cavalcanti Carvalho, Camila Calvino, Vanessa Silva Tavares Rodrigues, Dayse Nascimento Bernardino, Viviane Younes-Rapozo, Alex Christian Manhães, Elaine de Oliveira, Egberto Gaspar de Moura
PURPOSE: Children from smoking mothers have a higher risk of developing obesity and associated comorbidities later in life. Different experimental models have been used to assess the mechanisms involved with this increased risk. Using a rat model of neonatal nicotine exposure via implantation of osmotic minipumps in lactating dams, we have previously shown marked sexual dimorphisms regarding metabolic and endocrine outcomes in the adult progeny. Considering that more than four thousand substances are found in tobacco smoke besides nicotine, we then studied a rat model of neonatal tobacco smoke exposure: adult male offspring had hyperphagia, obesity, hyperglycemia, hypertriglyceridemia, secondary hyperthyroidism and lower adrenal hormones...
May 19, 2017: Endocrine
https://www.readbyqxmd.com/read/28527084/neurobiology-of-chronicization
#17
Gian Camillo Manzoni, Marco Russo, Arens Taga, Paola Torelli
In the past few years, research on chronicization of headache has focussed primarily on migraine, even though there are other types of primary headache that over time can turn into chronic forms. Only a minority of migraine sufferers will develop a chronic condition, with attacks that are likely to vary in their clinical features. As a result, in chronic migraine the specific diagnostic criteria for this headache type do not always exhibit the typical features of migraine. Among the factors that play a major role in favouring chronicization are a high frequency of migraine attacks since the beginning, overuse of symptomatic medication and onset of depression or arterial hypertension...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28527061/ketogenic-diet-in-migraine-rationale-findings-and-perspectives
#18
Piero Barbanti, Luisa Fofi, Cinzia Aurilia, Gabriella Egeo, Massimiliano Caprio
Ketogenic diet (KD) is an established treatment for refractory pediatric epilepsy and a promising therapy for diverse neurological diseases. Clinical data on KD in migraine-obtained from 150 patients investigated in case reports and prospective studies-suggest that KD may be a rapid onset effective prophylaxis for episodic and chronic migraine. KD would contribute to restore brain excitability and metabolism and to counteract neuroinflammation in migraine, although its precise mechanism is still unclear. Randomized controlled studies are needed to confirm the usefulness of KD in migraine and to investigate its optimal duration, repeatability, feasibility in normal weight subjects, efficacy in pediatric population and association to conventional migraine prophylaxis...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28527056/pathogenesis-of-chronic-cluster-headache-and-bouts-role-of-tryptamine-arginine-metabolism-and-%C3%AE-1-agonists
#19
G D'Andrea, G Bussone, P Di Fiore, F Perini, A Gucciardi, A Bolner, M Aguggia, G Saracco, E Galloni, G Giordano, A Leon
The aim of this study was to explore the possible role of tryptamine in the pathogenesis of chronic cluster headache along with that of adrenaline and noradrenaline (α-agonists) together with arginine metabolism in the origin of cluster bouts. Plasma levels of tyramine, tryptamine, serotonin, 5-hydroxyindolacetic acid, noradrenalin, adrenalin and the markers of arginine metabolism such as arginine, homoarginine, citrulline, ADMA and NMMA, were measured in 23 chronic cluster headache patients (10 chronic cluster ab initio and 13 transformed from episodic cluster) and 28 control subjects...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28527050/interplay-between-sirt-3-metabolism-and-its-tumor-suppressor-role-in-hepatocellular-carcinoma
#20
REVIEW
Serena De Matteis, Anna Maria Granato, Roberta Napolitano, Chiara Molinari, Martina Valgiusti, Daniele Santini, Francesco Giuseppe Foschi, Giorgio Ercolani, Umberto Vespasiani Gentilucci, Luca Faloppi, Mario Scartozzi, Giovanni Luca Frassineti, Andrea Casadei Gardini
Sirtuins (SIRT), first described as nicotinamide adenine dinucleotide (NAD(+))-dependent type III histone deacetylases, are produced by cells to support in the defense against chronic stress conditions such as metabolic syndromes, neurodegeneration, and cancer. SIRT-3 is one of the most studied members of the mitochondrial sirtuins family. In particular, its involvement in metabolic diseases and its dual role in cancer have been described. In the present review, based on the evidence of SIRT-3 involvement in metabolic dysfunctions, we aimed to provide an insight into the multifaceted role of SIRT-3 in many solid and hematological tumors with a particular focus on hepatocellular carcinoma (HCC)...
May 19, 2017: Digestive Diseases and Sciences
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