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https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#1
Andrea Chicca, Chiara Arena, Simone Bertini, Francesca Gado, Elena Ciaglia, Mario Abate, Maria Digiacomo, Margherita Lapillo, Giulio Poli, Maurizio Bifulco, Marco Macchia, Tiziano Tuccinardi, Jürg Gertsch, Clementina Manera
The endocannabinoid system (ECS) represents one of the major neuromodulatory systems involved in different physiological and pathological processes. Multi-target compounds exert their activities by acting via multiple mechanisms of action and represent a promising pharmacological modulation of the ECS. In this work we report 4-substituted and 4,5-disubstituted 1,2-dihydro-2-oxo-pyridine-3-carboxamide derivatives with a broad spectrum of affinity and functional activity towards both cannabinoid receptors and additional effects on the main components of the ECS...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29792957/high-activity-production-of-xylanase-by-pichia-stipitis-purification-characterization-kinetic-evaluation-and-xylooligosaccharides-production
#2
Changhe Ding, Mengxing Li, Yuqi Hu
As an industrially important biological macromolecule, xylanase hydrolyzes xylan to produce xylooligosaccarides (XOS). XOS, with a degree of polymerization (DP) 2 to 4, are important prebiotics used as food ingredients. In this study, xylanase (5536 U/g substrate) was produced by Pichia stipitis using corncob and wheat bran mixture under solid state fermentation. Crude xylanase were purified and biochemically characterized. XOS hydrolyzed by crude and purified xylanases were quantified. Molecular weight of the purified enzyme was around 31...
May 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29792943/the-development-of-a-screening-protocol-for-salmonella-spp-and-enteropathogenic-yersinia-spp-in-samples-from-wild-boar-sus-scrofa-also-generating-mlva-data-for-y-enterocolitica-and-y-pseudotuberculosis
#3
Axel Sannö, Magdalena Jacobson, Sandra Sterner, Susanne Thisted-Lambertz, Anna Aspán
Salmonellosis and yersiniosis are notifiable human diseases that are commonly associated with contaminated food. Domestic pigs as well as wild boars and other wild-life have been identified as reservoirs of these bacteria. Methods for cultivation and molecular epidemiological investigations of Salmonella spp. are well established, however, cultivation of enteropathogenic Yersinia spp. is time- consuming and the commonly used method for molecular epidemiological investigations, pulsed-field gel electrophoresis, lack in discriminatory power...
May 21, 2018: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/29792906/four-novel-antibacterial-sesquiterpene-%C3%AE-amino-acid-quaternary-ammonium-hybrids-from-the-mycelium-of-mushroom-stereum-hirsutum
#4
Yuan-Chang Duan, Jun Feng, Na Bai, Guo-Hong Li, Ke-Qin Zhang, Pei-Ji Zhao
The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D (1-4), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium, with the minimum inhibitory concentration (MIC) values of 12...
May 21, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29792869/preferential-inputs-from-cholecystokinin-positive-neurons-to-the-somatic-compartment-of-parvalbumin-expressing-neurons-in-the-mouse-primary-somatosensory-cortex
#5
Hiroyuki Hioki, Jaerin Sohn, Hisashi Nakamura, Shinichiro Okamoto, Jungwon Hwang, Yoko Ishida, Megumu Takahashi, Hiroshi Kameda
Parvalbumin-positive (PV+) neurons in the cerebral cortex, mostly corresponding to fast-spiking basket cells, have been implicated in higher-order brain functions and psychiatric disorders. We previously demonstrated that the somatic compartment of PV+ neurons received inhibitory inputs mainly from vasoactive intestinal polypeptide (VIP)+ neurons, whereas inhibitory inputs to the dendritic compartment were derived mostly from PV+ and somatostatin (SOM)+ neurons. However, a substantial number of the axosomatic inputs have remained unidentified...
May 21, 2018: Brain Research
https://www.readbyqxmd.com/read/29792860/diphenyleneiodonium-enhances-oxidative-stress-and-inhibits-japanese-encephalitis-virus-induced-autophagy-and-er-stress-pathways
#6
Manish Sharma, Kiran Bala Sharma, Shailendra Chauhan, Sankar Bhattacharyya, Sudhanshu Vrati, Manjula Kalia
Diphenyleneiodonium (DPI) and N-acetyl-L-cysteine (NAC), two widely used anti-oxidants, were employed to evaluate the role of oxidative stress in Japanese encephalitis virus (JEV) induced autophagy, stress responses and replication. DPI and NAC exerted opposite effects on ROS levels in JEV infected mouse neuronal cells (Neuro2a), mouse embryonic fibroblasts (MEFs) and human epithelial cells (HeLa). While NAC effectively quenched ROS, DPI enhanced ROS levels, suggesting that DPI induces oxidative stress in JEV infected cells...
May 21, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29792810/optogenetic-inhibition-of-g%C3%AE-q-protein-signaling-reduces-calcium-oscillation-stochasticity
#7
Pimkhuan Hannanta-Anan, Brian Y Chow
As fast terminators of G-protein coupled receptor (GPCR) signaling, regulators of G-protein signaling (RGS) serve critical roles in fine-tuning second messenger levels and, consequently, cellular responses to external stimuli. Here, we report the creation of an optogenetic RGS2 (opto-RGS2) that suppresses agonist-evoked calcium oscillations by the inactivation of Gαq protein. In this system, cryptochrome-mediated hetero-dimerization of the catalytic RGS2-box with its N-terminal amphipathic helix reconstitutes a functional membrane-localized complex that can dynamically suppress store-operated release of calcium...
May 24, 2018: ACS Synthetic Biology
https://www.readbyqxmd.com/read/29792707/nano-scale-conductive-filament-with-alternating-rectification-as-an-artificial-synapse-building-block
#8
Dan Berco, Yu Zhou, Sankara Rao Gollu, Pranav Sairam Kalaga, Abhisek Kole, Mohamed Hassan, Diing Shenp Ang
A popular approach for resistive memory (RRAM) based hardware implementation of neural networks utilizes one (or two) device that functions as an analog synapse in a crossbar structure of perpendicular pre- and post-synaptic neurons. An ideal fully automated, large scale artificial neural network, that matches a biologic counterpart (in terms of density and energy consumption), thus requires nano sized, extremely low power devices with a wide dynamic range and multi level functionality. Unfortunately the tradeoff between these traits proves to be a serious obstacle in the realization of brain inspired computing platforms yet to be overcome...
May 24, 2018: ACS Nano
https://www.readbyqxmd.com/read/29792702/peniisocoumarins-a-j-isocoumarins-from-penicillium-commune-qqf-3-an-endophytic-fungus-of-the-mangrove-plant-kandelia-candel
#9
Runlin Cai, Yingnan Wu, Senhua Chen, Hui Cui, Zhaoming Liu, Chunyuan Li, Zhigang She
Ten new isocoumarins, named peniisocoumarins A-J (1-9 and 11), along with three known analogues (10, 12, and 13) were obtained from the fermentation of an endophytic fungus, Penicillium commune QQF-3, which was isolated from a fresh fruit of the mangrove plant Kandelia candel. Their structures were elucidated through extensive spectroscopic analysis. The absolute configurations of 1-7 were determined by single-crystal X-ray diffraction and modified Mosher's method, and those of 8, 9, and 11 were assigned on the basis of experimental and calculated electronic circular dichroism data...
May 24, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29792562/combined-effects-and-cross-interactions-of-different-antibiotics-and-polypeptides-in-salmonella-bredeney
#10
Xiangyu Ju, Mengjiao Zhu, Jinzhi Han, Zhaoxin Lu, Haizhen Zhao, Xiaomei Bie
Salmonella spp. are health-threatening foodborne pathogens. The increasingly common spread of antibiotic-resistant Salmonella spp. is a major public healthcare issue worldwide. In this study, we wished to explore (1) antibiotic or polypeptide combinations to inhibit multidrug-resistant Salmonella bredeney and (2) the regulation of cross-resistance and collateral sensitivity of antibiotics and polypeptides. We undertook a study to select antibiotic combinations. Then, we promoted drug-resistant strains of S...
May 24, 2018: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/29792473/cognitive-and-affective-associations-with-an-ecologically-valid-test-of-theory-of-mind-across-the-lifespan
#11
Emilie Johansson Nolaker, Kim Murray, Francesca Happé, Rebecca A Charlton
OBJECTIVES: Many studies have demonstrated that theory of mind (ToM) ability declines with increasing age. Research has found that ToM-age associations are often mediated by other cognitive abilities particularly executive function. However, older adults rarely complain about real-world ToM difficulties. It has been suggested that older adults may perform better in real-world situations compared with experimental settings. METHOD: We examined performance on the Strange Stories Film Task (SSFT) which has been designed to assess ToM using naturalistic, video scenarios...
May 24, 2018: Neuropsychology
https://www.readbyqxmd.com/read/29792415/two-photon-active-organotin-iv-complexes-for-antibacterial-function-and-superresolution-bacteria-imaging
#12
Lei Hu, Hui Wang, Tingting Xia, Bin Fang, Yu Shen, Qiong Zhang, Xiaohe Tian, Hongping Zhou, Jieying Wu, Yupeng Tian
Antibacterial agents with two-photon absorption are expected to play a significant role in biomedical science. Herein, two novel organotin complexes, HLSn1 and HLSn2, based on coumarin were designed, synthesized, and systematically investigated. It was found that these complexes possessed suitable two-photon-active cross sections in the near-infrared region. Moreover, complex HLSn1 could efficiently inhibit the growth of Gram-negative Escherichia coli and Gram-positive Bacillus subtilis, especially the latter with a minimum inhibitory concentration (MIC; 90%) of 2 ± 0...
May 24, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29792367/visual-and-visuomotor-processing-of-hands-and-tools-as-a-case-study-of-cross-talk-between-the-dorsal-and-ventral-streams
#13
Jorge Almeida, Lénia Amaral, Frank E Garcea, Diana Aguiar de Sousa, Shan Xu, Bradford Z Mahon, Isabel Pavão Martins
A major principle of organization of the visual system is between a dorsal stream that processes visuomotor information and a ventral stream that supports object recognition. Most research has focused on dissociating processing across these two streams. Here we focus on how the two streams interact. We tested neurologically-intact and impaired participants in an object categorization task over two classes of objects that depend on processing within both streams-hands and tools. We measured how unconscious processing of images from one of these categories (e...
May 24, 2018: Cognitive Neuropsychology
https://www.readbyqxmd.com/read/29792346/synthesis-of-novel-camphene-based-thiosemicarbazones-and-evaluation-of-anti-mycobacterium-tuberculosis-activity
#14
Mariana R P Souza, Narcimário P Coelho, Vanessa P Baldin, Regiane B L Scodro, Rosilene F Cardoso, Cleuza C da Silva, Fábio Vandresen
In this work the aim of study was the synthesis and evaluation of in vitro anti-Mycobacterium tuberculosis activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of M. tuberculosis H37 Rv, especially the derivatives 3, 4a-c, 4f, 4i, 4k, 5 and 6a-b. MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL...
May 24, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29792335/synthesis-of-novel-thymol-derivatives-against-mrsa-and-esbl-producing-pathogenic-bacteria
#15
Shasank S Swain, Sudhir K Paidesetty, Rabindra N Padhy
Twelve substituted aryl-azo-thymol derivatives (4a to 4 l) were synthesized and characterized by several spectral techniques such as, FTIR, UV-vis, proton NMR, Mass spectrometry and elemental analysis. Antimicrobial activities were evaluated by agar-well diffusion method against isolated MRSA, ESBL-producing pathogenic bacteria and antifungal resistant fungi, in vitro. In addition, drug likeness properties of derivatives were assessed through bioinformatic tools such as, PASS prediction, molecular docking and Lipinski rules of five, along with determination of toxic nature and LD50 values...
May 24, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29792329/residual-complexity-does-impact-organic-chemistry-and-drug-discovery-the-case-of-rufomyazine-and-rufomycin
#16
Mary P Choules, Larry L Klein, David C Lankin, James B McAlpine, Sang-Hyun Cho, Jinhua Cheng, Hanki Lee, Joo-Won Suh, Birgit U Jaki, Scott G Franzblau, Guido F Pauli
Residual complexity (RC) involves the impact of subtle but critical structural and biological features on drug lead validation, including unexplained effects related to unidentified impurities. RC commonly plagues drug discovery efforts due to the inherent imperfections of chromatographic separation methods. The new diketopiperazine, rufomyazine (6), and the previously known antibiotic, rufomycin (7), represent a prototypical case of RC that (almost) resulted in the misassignment of biological activity. The case exemplifies that impurities well below the natural abundance of 13 C (1...
May 24, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29792197/antimicrobial-susceptibility-of-campylobacter-jejuni-and-campylobacter-coli-comparison-between-etest-and-a-broth-dilution-method
#17
Maya Azrad, Linda Tkhawkho, Natalia Isakovich, Orna Nitzan, Avi Peretz
BACKGROUND: Campylobacter is a leading cause of foodborne gasteroenteritis worldwide. Antimicrobial susceptibility testing for Campylobacter spp. is not routinely performed by most clinical laboratories. However, the emergence of resistant isolates strengthens the importance of antimicrobial susceptibility testing and the critical need for epidemiologic surveillance. The aim of this study was to compare the efficacy of Etest and Sensititre kit (a broth microdilution method) as methods for susceptibility tests and the critical need for epidemiologic surveillance...
May 23, 2018: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/29792155/design-synthesis-and-investigation-of-new-diphenyl-substituted-pyridazinone-derivatives-as-both-cholinesterase-and-a%C3%AE-aggregation-inhibitors
#18
Burcu Kilic, Merve Erdogan, Hayrettin O Gulcan, Fatma Aksakal, Nihan Oruklu, E Umit Bagriacik, Deniz S Dogruer
Backround: With respect to the increase in the average life expectancy, Alzheimer Disease (AD), the most common form of age-related dementia, has become a major threat to the population over the age of 65 during the past several decades. The majority of AD treatments are focused on cholinergic and amyloid hypotheses. OBJECTIVE: In this study, three series of diphenyl-2-(2-(4-substitutedpiperazin-1-yl)ethyl)pyridazin-3(2H)-one derivatives were designed, synthesized and investigated for their ability to inhibit both cholinesterase enzymes and amyloid-β aggregation...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792154/exploration-of-hetero-aryl-derived-thienylchalcones-for-antiviral-and-anticancer-activities
#19
Vikrant Patil, Siddappa A Patil, Renukadevi Patil, Alejandro Bugarin, Kenneth Beaman, Shivaputra A Patil
BACKGROUND: Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents. OBJECTIVE: With the aim of identifying the broad acting antiviral and anticancer agents, we discovered substituted aryl/heteroaryl derived thienyl chalcones as antiviral and anticancer agents...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792153/antimicrobial-evaluation-of-erythrinan-alkaloids-from-erythrina-crista-galli-l
#20
Janaina M de Avila, Ionara I Dalcol, Alessandra O Pereira, Eveline W Santos, Adriano Ferraz, Maura Z Santos, Marco Aurelio Mostardeiro, Ademir F Morel
BACKGROUND: Several species of the genus Erythrina have been used as sedative, antidepressant, and anticonvulsant. Erythrina crista-galli is native to the Pampa Biome and is widely used for medicinal purposes. Erythrinan alkaloids exhibit a range of pharmacological properties. OBJECTIVE: The aim of this study was to evaluate the basic fractions and the alkaloids isolated from E. crista-galli bark against a collection of bacteria and fungi for the first time. METHODS: Erythrina crista-galli stem bark was extracted with MeOH under reflux...
May 23, 2018: Medicinal Chemistry
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