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https://www.readbyqxmd.com/read/28434194/cytotoxic-triterpenoids-from-the-stalks-of-microtropis-triflora
#1
Xiao-Wei Zhang, Kui-Wu Wang, Man-Qing Zhou
Bioassay-guided phytochemcal investigation of the stalks of Microtropis triflora Merr. et Freem led to the isolation of ten triterpenes 1-10, including one novel compound 24-epoxy-2α, 24-dihydroxy-29-friedelanoic acid (1). Their chemical structures were identified on the basis of spectroscopic analysis, including HRESI mass spectrometry, 1D and 2D NMR ((1) H, (13) C, (1) H-(1) H COSY, HSQC, HMBC and NOESY), and by comparison with the data reported. The cytotoxicities of the compounds 1-10 against a panel of cultured human tumor cell lines (Bcap37, SMMC7721, Hela, CNE) were evaluated...
April 23, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28434186/new-thiourea-and-1-3-thiazolidin-4-one-derivatives-effective-on-the-hiv-1-virus
#2
Anna Bielenica, Giuseppina Sanna, Silvia Madeddu, Marta Struga, Michał Jóźwiak, Anna E Kozioł, Aleksandra Sawczenko, Ilona B Materek, Alessandra Serra, Gabriele Giliberti
Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. As part of our continuing effort to develop new active compounds, we report the synthesis and the evaluation of new fifteen thiourea derivatives with 1,3-benzothiazol-2-yl moiety, among them a group of biologically active (1-7) also underwent cyclisation to 1,3-thiazolidin-4-ones. Molecular structure of four compounds (4, 13, 15 and 3a) was determined by an X-ray crystallography. We here report the evaluation of their cytotoxicity against human leukaemia/lymphoma- and solid tumour-derived cell lines and of their antiviral activity against HIV-1 and representatives of ssRNA and dsDNA viruses...
April 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28434137/cholesterol-hydroperoxide-generation-translocation-and-reductive-turnover-in-biological-systems
#3
Albert W Girotti, Witold Korytowski
Cholesterol is like other unsaturated lipids in being susceptible to peroxidative degradation upon exposure to strong oxidants like hydroxyl radical or peroxynitrite generated under conditions of oxidative stress. In the eukaryotic cell plasma membrane, where most of the cellular cholesterol resides, peroxidation leads to membrane structural and functional damage from which pathological states may arise. In low density lipoprotein, cholesterol and phospholipid peroxidation have long been associated with atherogenesis...
April 22, 2017: Cell Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28434116/activation-of-the-serotonin-pathway-is-associated-with-poor-outcome-in-copd-exacerbation-results-of-a-long-term-cohort-study
#4
Marc A Meier, Manuel Ottiger, Alaadin Vögeli, Christian Steuer, Luca Bernasconi, Robert Thomann, Mirjam Christ-Crain, Christoph Henzen, Claus Hoess, Werner Zimmerli, Andreas Huber, Beat Mueller, Philipp Schuetz
BACKGROUND/INTRODUCTION: Indoleamine 2,3-dioxygenase (IDO) metabolizes tryptophan to kynurenine. An increase of its activity is associated with severity in patients with pneumonia. In chronic obstructive pulmonary disease (COPD) patients, an elevation of serotonin has been reported. Experimental models showed that cigarette smoke inhibits monoamine oxidase (MAO) leading to higher levels of serotonin. We investigated the prognostic ability of tryptophan, serotonin, kynurenine, IDO, and tryptophan hydroxylase (TPH) to predict short- and long-term outcomes in patients with a COPD exacerbation...
April 22, 2017: Lung
https://www.readbyqxmd.com/read/28433990/two-dimensional-ultrasound-evaluation-of-the-fetal-cerebral-aqueduct-improving-the-antenatal-diagnosis-and-counseling-of-aqueductal-stenosis
#5
Fernando Viñals, Pilar Ruiz, Gabriel Quiroz, Francisco A Guerra, Flavia Correa, Daniel Martínez, Bienvenido Puerto
OBJECTIVE: To describe a technique for the visualization and measurement of cerebral aqueduct diameter through a 2D sagittal median plane, and to report its aspect and measurement in fetuses with aqueductal stenosis (AS). METHODS: This was a cross-sectional study of 207 morphologically normal fetuses in low-risk pregnancies between 20 and 36 weeks of gestation. The cerebral aqueduct was visualized transvaginally in a midsagittal plane, and measurements of its greatest diameter (ampulla) were taken independently by an expert and a nonexpert sonographer...
April 22, 2017: Fetal Diagnosis and Therapy
https://www.readbyqxmd.com/read/28433941/self-assembled-dual-responsive-micelles-stabilized-with-protein-for-co-delivery-of-drug-and-sirna-in-cancer-therapy
#6
M R Aji Alex, Chetan Nehate, Srivani Veeranarayanan, D Sakthi Kumar, Ritu Kulshreshtha, Veena Koul
Design of safe and efficient vehicles for the combinatorial delivery of drugs and genetic agents is an emerging requisite for achieving enhanced therapeutic effect in cancer. Even though several nanoplatforms have been explored for the co-delivery of drugs and genetic materials the translation of these systems to clinical phase is still a challenge, mainly due to tedious synthesis procedures, lack of serum stability, inefficient scalability etc. Here in, we report development of reduction and pH sensitive polymeric graft of low molecular weight poly (styrene -alt -maleic anhydride) and evaluation of its efficacy in co-delivering drug and siRNA...
April 17, 2017: Biomaterials
https://www.readbyqxmd.com/read/28433935/distinct-on-off-fluorescence-signals-from-dual-responsive-activatable-nanoprobes-allows-detection-of-inflammation-with-improved-contrast
#7
Mathieu L Viger, Guillaume Collet, Jacques Lux, Viet Anh Nguyen Huu, Monica Guma, Alexandra Foucault-Collet, Jason Olejniczak, Shivanjali Joshi-Barr, Gary S Firestein, Adah Almutairi
Visualization of biochemical changes associated with disease is of great clinical significance, as it should allow earlier, more accurate diagnosis than structural imaging, facilitating timely clinical intervention. Herein, we report combining stimuli-responsive polymers and near-infrared fluorescent dyes (emission max: 790 nm) to create robust activatable fluorescent nanoprobes capable of simultaneously detecting acidosis and oxidative stress associated with inflammatory microenvironments. The spectrally-resolved mechanism of fluorescence activation allows removal of unwanted background signal (up to 20-fold reduction) and isolation of a pure activated signal, which enables sensitive and unambiguous localization of inflamed areas; target-to-background ratios reach 22 as early as 3 h post-injection...
March 28, 2017: Biomaterials
https://www.readbyqxmd.com/read/28433926/discredited-legacy-stigma-and-familial-amyloid-polyneuropathy-in-northwestern-portugal
#8
Álvaro Mendes, Liliana Sousa, Jorge Sequeiros, Angus Clarke
RATIONALE: Genetic inherited conditions may result in feelings of stigmatisation, mainly because of visible physical appearance and its transmissibility to offspring. OBJECTIVE: This article reports accounts of stigmatisation from Portuguese patients affected by the inherited neurodegenerative disease, familial amyloid polyneuropathy (FAP), living in the largest cluster of patients worldwide. METHOD: We draw on semi-structured interviews conducted with individuals at-risk or affected by FAP, recruited through the national patients' association, about their experiences of stigmatisation related to the illness...
April 15, 2017: Social Science & Medicine
https://www.readbyqxmd.com/read/28433879/sulfamethoxazole-degradation-in-anaerobic-sulfate-reducing-bacteria-sludge-system
#9
Yanyan Jia, Samir Kumar Khanal, Huiqun Zhang, Guang-Hao Chen, Hui Lu
Sulfamethoxazole (SMX) is one of the most commonly used antibiotics. SMX degradation in sulfate-reducing bacteria (SRB) sludge systems has not been reported so far. This research investigated the SMX degradation using SRB sludge in a sulfate-reducing up-flow sludge bed reactor. Moreover, the mechanisms and kinetics of SMX removal were also investigated using SRB sludge via a series of batch experiments. The results showed that SMX removal was characterized by a rapid sorption onto SRB sludge, and desorption from SRB sludge to aqueous phase until achieving equilibrium, and then followed by slow biodegradation...
April 17, 2017: Water Research
https://www.readbyqxmd.com/read/28433826/data-summarization-method-for-chronic-disease-tracking
#10
Dejan Aleksić, Petar Rajković, Dušan Vučković, Dragan Janković, Aleksandar Milenković
OBJECTIVES: Bearing in mind the rising prevalence of chronic medical conditions, the chronic disease management is one of the key features required by medical information systems used in primary healthcare. Our research group paid a particular attention to this specific area by offering a set of custom data collection forms and reports in order to improve medical professionals' daily routine. The main idea was to provide an overview of history for chronic diseases, which, as it seems, had not been properly supported in previous administrative workflows...
April 19, 2017: Journal of Biomedical Informatics
https://www.readbyqxmd.com/read/28433789/macromolecular-crowding-for-tailoring-tissue-derived-fibrillated-matrices
#11
Valentina Magno, Jens Friedrichs, Heather M Weber, Marina C Prewitz, Mikhail V Tsurkan, Carsten Werner
Tissue-derived fibrillated matrices can be instrumental for the in vitro reconstitution of multiphasic extracellular microenvironments. However, despite of several advantages, the obtained scaffolds so far offer a rather narrow range of materials characteristics only. In this work, we demonstrate how macromolecular crowding (MMC) - the supplementation of matrix reconstitution media with synthetic or natural macromolecules in ways to create excluded volume effects (EVE) - can be employed for tailoring important structural and biophysical characteristics of kidney-derived fibrillated matrices...
April 19, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28433787/facile-encapsulation-of-hydroxycamptothecin-nanocrystals-into-zein-based-nanocomplexes-for-active-targeting-drug-delivery-and-cell-imaging
#12
Hongdi Wang, Wei Zhu, Yunna Huang, Zhixian Li, Yanbin Jiang, Qiuling Xie
Nano-drug delivery systems that integrate inorganic and organic or even bioactive components into a single nanoscale platform are playing a greatly important role in cancer treatment. Here, the fabrication of a versatile nanocarrier based on self-assembled structures of gold nanoparticles (AuNPs)-zein is reported, which displays high drug-loading efficiency for needle-shaped hydroxycamptothecin (HCPT) nanocrystals. The surface modification with folate-conjugated polydopamine (PFA) renders them stable and also facilitates their selective cellular internalization and enhancement of endocytosis...
April 19, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28433718/three-new-piscidins-from-orange-spotted-grouper-epinephelus-coioides-phylogeny-expression-and-functional-characterization
#13
Ze-Rui Zhuang, Xiao-Dong Yang, Xia-Zi Huang, Hui-Xian Gu, Han-Yin Wei, Yi-Jun He, Li Deng
The present study reports the identification, and characterization of three new putative piscidin paralogues, ecPis-2, ecPis-3 and ecPis-4, from orange-spotted grouper (Epinephelus coioides). The cDNA of the three piscidins with the 207, 216, and 231 nt open reading frame encoded respectively a 68-, 71-, and 76-amino acid preprotein consisting of the predicted signal peptide, and putative mature peptide and prodomain. The phylogenetic analysis indicated that multiple piscidin paralogues in one fish species are highly diversified, the analysis suggested that the piscidins should be a family belonging to the superfamily of ancient cationic, linear, and amphipathic host defence peptides widespread across invertebrate and vertebrate taxa comprising insect cecropins and ceratotoxins, and the amphibian dermaseptins...
April 19, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/28433653/self-awareness-and-the-medial-temporal-lobe-in-neurodegenerative-diseases
#14
REVIEW
Chantal Chavoix, Ricardo Insausti
Accurate self-awareness is essential for adapting one's behaviour to one's actual abilities, to avoid risky behaviour. Impaired self-awareness of deficits is common in neurodegenerative diseases. Numerous studies show an involvement of midline cortical areas in impaired self-awareness. Among the other brain regions implicated stand the medial temporal lobe (MTL) structures (i.e. hippocampus, amygdala, and temporopolar, entorhinal, perirhinal and posterior parahippocampal cortices). This review aims at evaluating the role of those structures in self-awareness in neurodegenerative diseases...
April 19, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28433636/malassezia-globosa-mgmdl2-lipase-crystal-structure-and-rational-modification-of-substrate-specificity
#15
Dongming Lan, Huan Xu, JinXin Xu, Grzegorz Dubin, Jinsong Liu, Yonghua Wang
Lipases play an important role in physiological metabolism and diseases, and also have multiple industrial applications. Rational modification of lipase specificity may increase the commercial utility of this group of enzymes, but is hindered by insufficient mechanistic understanding. Here, we report the 2.0 Å resolution crystal structure of a mono- and di-acylglycerols lipase from Malassezia globosa (MgMDL2). Interestingly, residues Phe278 and Glu282 were found to involve in substrate recognition because mutation on each residue led to convert MgMDL2 to a triacylglycerol (TAG) lipase...
April 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28433539/rationally-designed-pi3k%C3%AE-mutants-to-mimic-atr-and-their-use-to-understand-binding-specificity-of-atr-inhibitors
#16
Yipin Lu, Mark Knapp, Kenneth Crawford, Robert Warne, Robert Elling, Kelly Yan, Michael Doyle, Gwynn Pardee, Li Zhang, Sylvia Ma, Mulugeta Mamo, Elizabeth Ornelas, Yue Pan, Dirksen Bussiere, Johanna Jansen, Isabel Zaror, Albert Lai, Paul Barsanti, Janet Sim
ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response and is an attractive anticancer drug target. Several potent and selective inhibitors of ATR have been reported showing significant antitumor efficacy, with most advanced ones entering clinical trials. However, due to the absence of an experimental ATR structure, the determinants contributing to ATR inhibitors' potency and specificity are not well understood. Here we present the mutations in the ATP-binding site of PI3Kα to progressively transform the pocket to mimic that of ATR...
April 19, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28433538/the-ns1-protein-from-influenza-virus-stimulates-translation-initiation-by-enhancing-ribosome-recruitment-to-mrnas
#17
Baptiste Panthu, Olivier Terrier, Coralie Carron, Aurélien Traversier, Antoine Corbin, Laurent Balvay, Bruno Lina, Manuel Rosa-Calatrava, Théophile Ohlmann
The non-structural protein NS1 of influenza A viruses exerts pleiotropic functions during infection. Amongst these functions, NS1 was shown to be involved both in the control of viral and cellular translation; however the mechanism by which this occurs remains to be determined. Thus, we have revisited the role of NS1 in translation by using a combination of influenza infection, mRNA reporter transfection, in vitro functional and biochemical assays. Our data show that the NS1 protein is able to enhance translation of virtually all tested mRNAs with the exception of constructs bearing the Dicistroviruses IRESes (DCV and CrPV), suggesting a role at the level of translation initiation...
April 19, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28433511/design-synthesis-and-pharmacological-evaluation-of-4-azolyl-benzamide-derivatives-as-novel-gpr52-agonists
#18
Kazuyuki Tokumaru, Yoshiteru Ito, Izumi Nomura, Takashi Nakahata, Yuji Shimizu, Emi Kurimoto, Kazunobu Aoyama, Kazuyoshi Aso
G protein-coupled receptor 52 (GPR52) agonists are expected to improve the symptoms of psychiatric disorders. During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC50)=75nM, maximal response (Emax)=122%) starting from a high-throughput screening hit 3 (EC50=470nM, Emax=56%). The structural features of a reported GPR52 agonist were applied to 3, led to design 4-azolylbenzamides as novel GPR52 agonists...
April 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28433488/guided-internet-based-psycho-educational-intervention-using-cognitive-behavioral-therapy-and-self-management-for-individuals-with-chronic-pain-a-feasibility-study
#19
Jennifer Perry, Elizabeth G VanDenKerkhof, Rosemary Wilson, Dean A Tripp
When considering barriers to chronic pain treatment, there is a need to deliver nonpharmacological therapies in a way that is accessible to all individuals who may benefit. To conduct feasibility testing using a guided, Internet-based intervention for individuals with chronic pain, a novel, Internet-based, chronic pain intervention (ICPI) was developed, using concepts proven effective in face-to-face interventions. This study was designed to assess usability of the ICPI and feasibility of conducting larger-scale research, and to collect preliminary data on effectiveness of the intervention...
April 19, 2017: Pain Management Nursing: Official Journal of the American Society of Pain Management Nurses
https://www.readbyqxmd.com/read/28433423/prefrontal-cortex-expression-of-chromatin-modifier-genes-in-male-wsp-and-wsr-mice-changes-across-ethanol-dependence-withdrawal-and-abstinence
#20
Joel G Hashimoto, David P Gavin, Kristine M Wiren, John C Crabbe, Marina Guizzetti
Alcohol-use disorder (AUD) is a relapsing disorder associated with excessive ethanol consumption. Recent studies support the involvement of epigenetic mechanisms in the development of AUD. Studies carried out so far have focused on a few specific epigenetic modifications. The goal of this project was to investigate gene expression changes of epigenetic regulators that mediate a broad array of chromatin modifications after chronic alcohol exposure, chronic alcohol exposure followed by 8 h withdrawal, and chronic alcohol exposure followed by 21 days of abstinence in Withdrawal-Resistant (WSR) and Withdrawal Seizure-Prone (WSP) selected mouse lines...
March 14, 2017: Alcohol
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