keyword
MENU ▼
Read by QxMD icon Read
search

Inhibition

keyword
https://www.readbyqxmd.com/read/29793215/in-silico-insight-into-voltage-gated-sodium-channel-1-7-inhibition-for-anti-pain-drug-discovery
#1
Mingxing Wang, Wei Li, Ying Wang, Yongbo Song, Jian Wang, Maosheng Cheng
Studies on human genetics have implicated the voltage-gated sodium channel Nav1.7 as an appealing target for the treatment of pain. In this study, we put forward a ligand-based pharmacophore for the first time, which was generated by a set of multiple chemical scaffolds including sulfonamide and non-sulfonamide derivatives and consisted of four chemical features: an aromatic ring, a hydrophobic group and two hydrogen acceptors. The active cavity was divided into three regions according to the properties of the amino acids surrounded and was used for the docking of 16 known active inhibitors...
May 18, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#2
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/29793205/comprehensive-assessment-of-three-typical-antibiotics-on-cyanobacteria-microcystis-aeruginosa-the-impact-and-recovery-capability
#3
Yingxiang Du, Jing Wang, Fengyi Zhu, Dina Mai, Zhongrun Xiang, Jianqiu Chen, Ruixin Guo
This innovative study provided a comprehensive evaluation of the effects of three typical antibiotics exposures (cefradine, norfloxacin and amoxicillin) on Microcystis aeruginosa in two periods (exposure and post-exposure) at a new perspective. The results indicated that the irreversible growth inhibition of M. aeruginosa attributed to the norfloxacin in the exposure and the re-exposure stages. In contrast, although the algal cell size recovered to the control level after the exposure of 20 mg/L of cefradine, the significant stimulation on glutathione (GSH) still persisted even if the contaminants were removed...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793199/effects-of-acute-and-chronic-exposures-of-fluoxetine-on-the-chinese-fish-topmouth-gudgeon-pseudorasbora-parva
#4
Hongxing Chen, Xiangfeng Zeng, Lei Mu, Liping Hou, Bin Yang, Jianliang Zhao, Daniel Schlenk, Wu Dong, Lingtian Xie, Qianru Zhang
Fluoxetine is a selective serotonin reuptake inhibitor used as an antidepressant and has been frequently detected in aquatic environments. However, its effects in fish from Asia remain relatively less studied. In this study, the topmouth gudgeon Pseudorasbora parva was exposed to 0, 50, and 200 µg/L of fluoxetine for 4 h and 42 d. The effects of fluoxetine on biometrics were compared to biochemical endpoints indicative of stress in different fish tissues (brain, liver, gills and intestine) following exposures...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793181/exogenously-applied-spermidine-alleviates-photosynthetic-inhibition-under-drought-stress-in-maize-zea-mays-l-seedlings-associated-with-changes-in-endogenous-polyamines-and-phytohormones
#5
Lijie Li, Wanrong Gu, Jing Li, Congfeng Li, Tenglong Xie, Danyang Qu, Yao Meng, Caifeng Li, Shi Wei
Drought stress (DS) is a major environmental factor limiting plant growth and crop productivity worldwide. It has been established that exogenous spermidine (Spd) stimulates plant tolerance to DS. The effects of exogenous Spd on plant growth, photosynthetic performance, and chloroplast ultrastructure as well as changes in endogenous polyamines (PAs) and phytohormones were investigate in DS-resistant (Xianyu 335) and DS-sensitive (Fenghe 1) maize seedlings under well-watered and DS treatments. Exogenous Spd alleviated the stress-induced reduction in growth, photosynthetic pigment content, photosynthesis rate (Pn ) and photochemical quenching (qP ) parameters, including the maximum photochemistry efficiency of photosystem II (PSII) (Fv /Fm ), PSII operating efficiency (ФPSII), and qP coefficient...
May 15, 2018: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/29793180/insulin-is-a-potential-antioxidant-for-diabetes-associated-cognitive-decline-via-regulating-nrf2-dependent-antioxidant-enzymes
#6
Ying Song, Wei Ding, Yun Bei, Yan Xiao, Hai-Da Tong, Li-Bo Wang, Li-Yao Ai
PURPOSE: To investigate the neuroprotective effects of insulin on diabetic encephalopathy and its mechanism. EXPERIMENTAL AND APPROACH: The diabetic model was established by injection of streptozotocin. Behavior examinations were conducted by the Morris water maze. Histopathological alterations were detected by HE staining. ROS, CAT levels and SOD activity were measured using a microplate reader. In vitro, the viability of wild type and knock-down PC12 cells was detected by MTT assay, the morphology of cells was monitored under a microscope...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793179/nano-strategies-for-berberine-delivery-a-natural-alkaloid-of-berberis
#7
REVIEW
Elaheh Mirhadi, Mehdi Rezaee, Bizhan Malaekeh-Nikouei
Berberine, as a phytochemical component of some medicinal Chinese herbs (most frequently Berberis vulgaris), is an isoquinoline alkaloid with many therapeutic effects including anti-viral, anti-microbial, anti-diarrhea, anti-inflammatory and anti-tumor effects. Berberine has some significant effects on type 2 diabetes through adenosine monophosphate-activated protein kinase activation, glycolysis stimulation, and mitochondrial function inhibition which subsequently improves both lipid and glucose metabolism...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793178/nrf2-p-glycoprotein-axis-is-associated-with-clinicopathological-characteristics-in-colorectal-cancer
#8
Mohammad Reza Sadeghi, Farhad Jeddi, Narges Soozangar, Mohammad Hossein Somi, Masoud Shirmohamadi, Vahid Khaze, Nasser Samadi
Colorectal cancer (CRC) is the fourth leading cause of cancer-related death worldwide. Activation of ABCB1 gene and its main product, P-glycoprotein, is the common reason for chemoresistance. The nuclear factor-erythroid 2-related factor2 (Nrf2) is directly regulated by Kelch like ECH-associated protein1 (Keap1). In addition, Nrf2 is a key transcriptional factor that regulates efflux transporters, including P-gp. The aim of this study was to investigate the expression levels of Nrf2, Keap1 and ABCB1 in the biopsy samples and their association with clinicopathological features in CRC patients...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793177/long-noncoding-rna-gas5-suppresses-triple-negative-breast-cancer-progression-through-inhibition-of-proliferation-and-invasion-by-competitively-binding-mir-196a-5p
#9
Shuqin Li, Jun Zhou, Zhaoxin Wang, Peishun Wang, Xitao Gao, Yan Wang
Triple-negative breast cancer (TNBC) is considered to be the most aggressive and lethal type of breast cancer. Many studies have suggested that the dysfunction of long noncoding RNAs (lncRNAs) is correlated with breast cancer metastasis and progression. Here, we show that levels of the lncRNA, growth arrest-specific transcript 5 (GAS5), are decreased in TNBC tissues, and this down-regulation of GAS5 is associated with an aggressive tumor phenotype in patients, affecting clinical stage, lymph node metastasis and overall survival...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793168/olive-oil-polyphenols-reduce-oxysterols-induced-redox-imbalance-and-pro-inflammatory-response-in-intestinal-cells
#10
Gessica Serra, Alessandra Incani, Gabriele Serreli, Laura Porru, M Paola Melis, Carlo I G Tuberoso, Daniela Rossin, Fiorella Biasi, Monica Deiana
Dietary habits may strongly influence intestinal homeostasis. Oxysterols, the oxidized products of cholesterol present in cholesterol-containing foodstuffs, have been shown to exert pro-oxidant and pro-inflammatory effects, altering intestinal epithelial layer and thus contributing to the pathogenesis of human inflammatory bowel diseases and colon cancer. Extra virgin olive oil polyphenols possess antioxidant and anti-inflammatory properties, and concentrate in the intestinal lumen, where may help in preventing intestinal diseases...
May 16, 2018: Redox Biology
https://www.readbyqxmd.com/read/29793167/improvement-of-neuronal-differentiation-by-carbon-monoxide-role-of-pentose-phosphate-pathway
#11
Ana S Almeida, Nuno L Soares, Catarina O Sequeira, Sofia A Pereira, Ursula Sonnewald, Helena L A Vieira
Over the last decades, the silent-killer carbon monoxide (CO) has been shown to also be an endogenous cytoprotective molecule able to inhibit cell death and modulate mitochondrial metabolism. Neuronal metabolism is mostly oxidative and neurons also use glucose for maintaining their anti-oxidant status by generation of reduced glutathione (GSH) via the pentose-phosphate pathway (PPP). It is established that neuronal differentiation depends on reactive oxygen species (ROS) generation and signalling, however there is a lack of information about modulation of the PPP during adult neurogenesis...
May 15, 2018: Redox Biology
https://www.readbyqxmd.com/read/29793165/inhibition-of-acetaminophen-induced-hepatotoxicity-in-mice-by-exogenous-thymosin%C3%AE-4-treatment
#12
Lei Wang, Xiankui Li, Cai Chen
OBJECTIVE: To study the effects of exogenous thymosinβ4 (Tβ4) treatment in acetaminophen (APAP)-induced hepatotoxicity. METHODS: Liver injury was induced in mice by a single intraperitoneal injection of APAP (500 mg/kg). Exogenous Tβ4 was intraperitoneally administrated at 0 h, 2 h and 4 h after APAP injection. Chloroquine (CQ) (60 mg/kg) was intraperitoneally injected 2 h before APAP administration to inhibit autophagy. Six hours after APAP injection liver injury was evaluated by histological examinations, biochemical measurements and enzyme linked immunosorbent assay (ELISAs)...
May 21, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29793154/juvenile-treatment-with-mglur2-3-agonist-prevents-schizophrenia-like-phenotypes-in-adult-by-acting-through-gsk3%C3%AE
#13
Bo Xing, Genie Han, Min-Juan Wang, Melissa A Snyder, Wen-Jun Gao
Prodromal memory deficits represent an important marker for the development of schizophrenia (SZ), in which glutamatergic hypofunction occurs in the prefrontal cortex (PFC). The mGluR2/3 agonist LY379268 (LY37) attenuates excitatory N-methyl-D-aspartate receptor (NMDAR)-induced neurotoxicity, a central pathological characteristic of glutamatergic hypofunction. We therefore hypothesized that early treatment with LY37 would rescue cognitive deficits and confer benefits for SZ-like behaviors in adults. To test this, we assessed whether early intervention with LY37 would improve learning outcomes in the Morris Water Maze for rats prenatally exposed to methylazoxymethanol acetate (MAM), a neurodevelopmental SZ model...
May 14, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29793153/effects-of-mg-2-on-recovery-of-nmda-receptors-from-inhibition-by-memantine-and-ketamine-reveal-properties-of-a-second-site
#14
Nathan G Glasgow, Madeleine R Wilcox, Jon W Johnson
Memantine and ketamine are NMDA receptor (NMDAR) open channel blockers that are thought to act via similar mechanisms at NMDARs, but exhibit divergent clinical effects. Both drugs act by entering open NMDARs and binding at a site deep within the ion channel (the deep site) at which the endogenous NMDAR channel blocker Mg2+ also binds. Under physiological conditions, Mg2+ increases the IC50 s of memantine and ketamine through competition for binding at the deep site. Memantine also can inhibit NMDARs after associating with a second site accessible in the absence of agonist, a process termed second site inhibition (SSI) that is not observed with ketamine...
May 12, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29793143/oxidation-at-c-16-enhances-butyrylcholinesterase-inhibition-in-lupane-triterpenoids
#15
María Julia Castro, Victoria Richmond, María Belén Faraoni, Ana Paula Murray
A set of triterpenoids with different grades of oxidation in the lupane skeleton were prepared and evaluated as cholinesterase inhibitors. Allylic oxidation with selenium oxide and Jones's oxidation were employed to obtain mono-, di- and tri-oxolupanes, starting from calenduladiol (1) and lupeol (3). All the derivatives showed a selective inhibition of butyrylcholinesterase over acetylcholinesterase (BChE vs. AChE). A kinetic study proved that compounds 2 and 9, the more potent inhibitors of the series, act as competitive inhibitors...
May 17, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793142/synthesis-of-aryl-pyrazole-via-suzuki-coupling-reaction-in-vitro-mushroom-tyrosinase-enzyme-inhibition-assay-and-in-silico-comparative-molecular-docking-analysis-with-kojic-acid
#16
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Bakhtawar Batool, Saima Kalsoom, M M Hasan, Mauricio F Erben, Hesham R El-Seedi, Musrat Ali, Zaman Ashraf
Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50  = 1.568 ± 0.01 µM) showed relatively better potential compared to reference kojic acid (IC50  = 16...
April 30, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793136/effects-of-gestational-hypertension-and-pre-eclampsia-in-mrna-expression-of-fibrinolysis-genes-in-primary-cultured-human-umbilical-vein-endothelial-cells
#17
Irais Poblete-Naredo, Yury Rodríguez-Yáñez, Rogelio O Corona-Núñez, Stuart González-Monroy, Juan E Salinas, Arnulfo Albores
Hypertension disorders (HD) and pre-eclampsia (PRE) are leading causes of maternal deaths worldwide. PRE is associated with vascular endothelial dysfunction and with deregulation of the fibrinolysis pathway genes. Fibrinolysis is the fibrin clot hydrolysis process catalyzed by plasmin, a proteolytic enzyme formed from plasminogen. Plasminogen is cleaved by tissue-type (tPA) and urokinase-type (uPA) activators and inhibited by the plasminogen activator inhibitors type-1 (PAI-1) and type-2 (PAI-2). The whole process maintains blood hemostasis...
May 17, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29793089/gold-and-gold-silver-alloy-nanoparticles-enhance-the-myogenic-differentiation-of-myoblasts-through-p38-mapk-signaling-pathway-and-promote-in-vivo-skeletal-muscle-regeneration
#18
Juan Ge, Kai Liu, Wen Niu, Mi Chen, Min Wang, Yumeng Xue, Chuanbo Gao, Peter X Ma, Bo Lei
Under the severe trauma condition, the skeletal muscles regeneration process is inhibited by forming fibrous scar tissues. Understanding the interaction between bioactive nanomaterials and myoblasts perhaps has important effect on the enhanced skeletal muscle tissue regeneration. Herein, we investigate the effect of monodispersed gold and gold-silver nanoparticles (AuNPs and Au-AgNPs) on the proliferation, myogenic differentiation and associated molecular mechanism of myoblasts (C2C12), as well as the in vivo skeletal muscle tissue regeneration...
May 18, 2018: Biomaterials
https://www.readbyqxmd.com/read/29793087/skin-allografting-activates-anti-tumor-immunity-and-suppresses-growth-of-colon-cancer-in-mice
#19
Xiang Li, Xu Lan, Grace Wang, Yi Liu, Ke Zhao, Shan-Zheng Lu, Xiao-Xi Xu, Gang-Gang Shi, Kui Ye, Bao-Ren Zhang, Yi-Ming Zhao, Hong-Qiu Han, Cai-Gan Du, Thomas E Ichim, Hao Wang
INTRODUCTION: The tumor cells could escape from the immune elimination through the immunoediting mechanisms including the generation of immunosuppressive or immunoregulative cells. By contrast, allograft transplantation could activate the immune system and induce a strong allogenic response. The aim of this study was to investigate the efficacy of allogenic skin transplantation in the inhibition of tumor growth through the activation of allogenic immune response. METHODS: Full-thickness skin transplantation was performed from C57BL/6 (H-2b ) donors to BALB/c (H-2d ) recipients that were receiving subcutaneous injection of isogenic CT26 colon cancer cells (2 × 106 cells) at the same time...
May 21, 2018: Translational Oncology
https://www.readbyqxmd.com/read/29793076/porcine-circovirus-type-2-inhibits-inter-%C3%AE-expression-by-targeting-karyopherin-alpha-3-in-pk-15-cells
#20
Jiansheng Li, Mingqing Lu, Bei Huang, Yingjun Lv
Interferon (IFN)-mediated antiviral response is an important part of host defense. Previous studies reported that porcine circovirus type 2 (PCV2) inhibits interferon production, but the mechanism is still poorly understood. In this study, PCV2 suppresses IFN-β and IRF3 promoters and mRNA level of IFN-β induced by ISD or Poly(I:C), but has no effect on the activation of AP-1 and NF-κB. Furthermore, PCV2 decreases the mRNA level of IFN-β and IFN-β promoter activity driven by STING, TBK1, IRF3, and IRF3/5D, and causes a reduction in the protein level of nuclear p-IRF3...
May 21, 2018: Virology
keyword
keyword
36104
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"