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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/29793206/effects-on-the-hepatic-transcriptome-of-chicken-embryos-in-ovo-exposed-to-phenobarbital
#2
Jiahua Guo, Shohei Ito, Hoa Thanh Nguyen, Kimika Yamamoto, Hisato Iwata
This work aimed at evaluating the toxic effects of in ovo exposure to phenobarbital (PB) and unveiling the mode of action by transcriptome analysis in the embryonic liver of a model avian species, chicken (Gallus gallus). Embryos were initially treated with saline or 1 μg PB /g egg at Hamburger Hamilton Stage (HHS) 1 (1st day), followed by 20 days of incubation to HHS 46. At 21st day, chicks that pipped successfully were euthanized and dissected for assessing the PB caused effects on phenotypes and the liver transcriptome in both genders...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793154/juvenile-treatment-with-mglur2-3-agonist-prevents-schizophrenia-like-phenotypes-in-adult-by-acting-through-gsk3%C3%AE
#3
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
#4
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/29793137/3-o-sulfation-of-heparin-leads-to-hepatotropism-and-longer-circulatory-half-life
#5
Colton M Miller, Yongmei Xu, Katrina M Kudrna, Blake E Hass, Brianna M Kellar, Andrew W Egger, Jian Liu, Edward N Harris
INTRODUCTION: Heparins are common blood anticoagulants that are critical for many surgical and biomedical procedures used in modern medicine. In contrast to natural heparin derived from porcine gut mucosa, synthetic heparins are homogenous by mass, polymer length, and chemistry. MATERIALS & METHODS: Stable cell lines expressing the human and mouse Stabilin receptors were used to evaluate endocytosis of natural and synthetic heparin. We chemoenzymatically produced synthetic heparin consisting of 12 sugars (dodecamers) containing 14 sulfate groups resulting in a non-3-O sulfated structure (n12mer)...
May 17, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29793103/disruption-of-the-gonadal-endocannabinoid-system-in-zebrafish-exposed-to-diisononyl-phthalate
#6
Isabel Forner-Piquer, Stefania Santangeli, Francesca Maradonna, Alessandro Rabbito, Fabiana Piscitelli, Hamid R Habibi, Vincenzo Di Marzo, Oliana Carnevali
DiNP (Di-isononyl phthalate) has been recently introduced as DEHP (Bis (2-ethylhexyl) phthalate) substitute and due to its chemical properties, DiNP is commonly used in a large variety of plastic items. The endocannabinoid system (ECS) is a lipid signaling system involved in a plethora of physiological pathways including the control of the reproductive and metabolic processes. In this study, the effects of DiNP on the ECS of zebrafish (male and female) gonads were analyzed. Adult zebrafish were chronically exposed for 21 days via water to 3 environmentally relevant concentrations of DiNP (42 μg/L; 4...
May 21, 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29793095/sex-hormones-affect-acute-and-chronic-stress-responses-in-sexually-dimorphic-patterns-consequences-for-depression-models
#7
Lei Guo, Yi-Xi Chen, Yu-Ting Hu, Xue-Yan Wu, Yang He, Juan-Li Wu, Man-Li Huang, Matthew Mason, Ai-Min Bao
BACKGROUND: Alterations in peripheral sex hormones may play an important role in sex differences in terms of stress responses and mood disorders. It is not yet known whether and how stress-related brain systems and brain sex steroid levels fluctuate in relation to changes in peripheral sex hormone levels, or whether the different sexes show different patterns. We aimed to investigate systematically, in male and female rats, the effect of decreased circulating sex hormone levels following gonadectomy on acute and chronic stress responses, manifested as changes in plasma and hypothalamic sex steroids and hypothalamic stress-related molecules...
May 21, 2018: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29793048/dna-methylation-differences-at-the-glucocorticoid-receptor-gene-in-depression-are-related-to-functional-alterations-in-hypothalamic-pituitary-adrenal-axis-activity-and-to-early-life-emotional-abuse
#8
Chloё Farrell, Kelly Doolin, Niamh O' Leary, Chaitra Jairaj, Darren Roddy, Leonardo Tozzi, Derek Morris, Andrew Harkin, Thomas Frodl, Zsófia Nemoda, Moshe Szyf, Linda Booij, Veronica O'Keane
Depression is associated with alterations in hypothalamic-pituitary-adrenal (HPA) axis activity. A proposed mechanism to explain these alterations are changes in DNA methylation levels, secondary to early life adversity (ELA), at stress-related genes. Two gene regions that have been implicated in the literature, the glucocorticoid receptor gene (NR3C1) exon 1F and the FKBP5 gene intron 7 were examined in 67 individuals (33 depressed patients and 34 controls). We investigated whether cortisol concentrations, evaluated in 25 depressed patients and 20 controls, and measures of ELA were associated with the degree of methylation at these candidate gene regions...
May 8, 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29793020/epha2-stimulates-vcam-1-expression-through-calcium-dependent-nfat1-activity
#9
Steven Daniel Funk, Alexandra C Finney, Arif Yurdagul, Christopher B Pattillo, A Wayne Orr
Endothelial cell activation by proinflammatory stimuli drives leukocyte recruitment through enhanced expression of counter-receptors such as vascular cell adhesion molecule-1 (VCAM-1). We previously demonstrated that activation of the receptor tyrosine kinase EphA2 with its ligand ephrin-A1 induces VCAM-1 expression. Here, we sought to characterize the proinflammatory signaling pathways involved. Analysis of over-represented transcription factors in ephrin-A1-induced genes identified multiple potential transcriptional regulators, including the Rel family members nuclear factor-κB (NF-κB/p65) and nuclear factor of activated T-cells (NFAT)...
May 21, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29793000/effect-of-a-bisphosphonate-and-selective-estrogen-receptor-modulator-on-bone-remodeling-in-streptozotocin-induced-diabetes-and-ovariectomized-rat-model
#10
Young-Seok Lee, Rishab Gupta, Jeong-Taik Kwon, Dae-Chul Cho, Ye Jin Seo, Sung Young Seu, Eui Kyun Park, Inbo Han, Chi-Heon Kim, Joo-Kyung Sung, Kyoung-Tae Kim
BACKGROUND CONTEXT: Diabetes and menopause can cause severe osteoporosis. In general, menopause and diabetes can lead to an imbalance in bone turnover, which results in secondary osteoporosis. However, the efficacy of antiresorptive drugs against this form of osteoporosis has not been extensively evaluated. OBJECTIVE: The aim of this study was to determine the changes in vertebral bone remodeling when postmenopausal osteoporosis is accompanied by diabetes and the efficacy of bisphosphonates and selective estrogen-receptor modulators (SERMs) against these outcomes...
May 21, 2018: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/29792951/an-analysis-of-variability-in-genome-organisation-of-intracellular-calcium-release-channels-across-insect-orders
#11
Bartlomiej J Troczka, Ewan Richardson, Rafael Homem, T G Emyr Davies
Using publicly available genomic data, combined with RT-PCR validation, we explore structural genomic variation for two major ion channels across insect classes. We have manually curated Ryanodine receptor (RyR) and inositol 1,4,5-trisphosphate receptor (IP3 R) ORFs and their corresponding genomic structures from 26 different insects covering major insect orders. We found that, despite high protein identity for both RyRs (>75%) and IP3 Rs (~67%), the overall complexity of the gene structure varies greatly between different insect orders with the simplest genes (fewest introns) found in Diptera and the most complex in Lepidoptera...
May 21, 2018: Gene
https://www.readbyqxmd.com/read/29792947/trail-attenuates-sulforaphane-mediated-nrf2-and-sustains-ros-generation-leading-to-apoptosis-of-trail-resistant-human-bladder-cancer-cells
#12
Cheng-Yun Jin, Ilandarage Menu Neelaka Molagoda, Wisurumuni Arachchilage Hasitha Maduranga Karunarathne, Sang-Hyuck Kang, Cheol Park, Gi-Young Kim, Yung Hyun Choi
Tumor necrosis factor-related apoptosis inducing ligand (TRAIL) can preferentially initiate apoptosis in malignant cells with minimal toxicity to normal cells. Unfortunately, many human cancer cells are refractory to TRAIL-induced apoptosis through many unknown mechanisms. Here, we report that TRAIL resistance can be reversed in human bladder cancer cell lines by treatment with sulforaphane (SFN), a well-known chemopreventive isothiocyanate in various cruciferous vegetables. Combined treatment with SFN and TRAIL (SFN/TRAIL) significantly induced apoptosis concomitant with activation of caspases, loss of mitochondrial membrane potential (MMP), Bid truncation, and induction of death receptor 5...
May 21, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29792915/the-cd44-ha-axis-and-inflammation-in-atherosclerosis-a-temporal-perspective
#13
REVIEW
Mia Krolikoski, James Monslow, Ellen Puré
Cardiovascular disease (CVD) due to atherosclerosis is a disease of chronic inflammation at both the systemic and the tissue level. CD44 has previously been implicated in atherosclerosis in both humans and mice. This multi-faceted receptor plays a critical part in the inflammatory response during the onset of CVD, though little is known of CD44's role during the latter stages of the disease. This review focuses on the role of CD44-dependent HA-dependent effects on inflammatory cells in several key processes, from disease initiation throughout the progression of atherosclerosis...
May 21, 2018: Matrix Biology: Journal of the International Society for Matrix Biology
https://www.readbyqxmd.com/read/29792904/monoclonal-antibody-dl11c8-identifies-adam23-as-a-component-of-lipid-raft-microdomains
#14
Zaine L M Borgonovo, Caroline F Ribeiro, Michele D M Costa, Ingrid L M Souza, Gustavo R Rossi, Monica V Alcantara, Max Ingberman, Luciano G Braga, Adriana F Mercadante, Lia S Nakao, Silvio M Zanata
A disintegrin and metalloprotease protein 23 (ADAM23) is a transmembrane type I glycoprotein involved with the development and maintenance of the nervous system, including neurite outgrowth, neuronal adhesion and differentiation and regulation of synaptic transmission. In addition, ADAM23 seems to participate in immune response and tumor establishment through interaction with different members of integrin receptors. Here, we describe a novel monoclonal antibody (DL11C8) that specifically recognizes the cysteine-rich domain of both pre-protein (100kDa) and mature (70 kDa) forms of ADAM23 from different species, including human, rodents and avian orthologs...
May 21, 2018: Neuroscience
https://www.readbyqxmd.com/read/29792888/oral-vitamin-a-coupled-valsartan-nanomedicine-high-hepatic-stellate-cell-receptors-accessibility-and-prolonged-enterohepatic-residence
#15
Nesrine S El-Mezayen, Wessam F El-Hadidy, Wessam M El-Refaie, Thanaa I Shalaby, Mahmoud M Khattab, Aiman S El-Khatib
So far, liver fibrosis still has no clinically-approved treatment. The loss of stored vitamin-A (VA ) in hepatic stellate cells (HSCs), the main regulators to hepatic fibrosis, can be applied as a mechanism for their targeting. Valsartan is a good candidate for this approach; it is a marketed oral-therapy with inverse- and partial-agonistic activity to the over-expressed angiotensin-II type1 receptor (AT1R) and depleted nuclear peroxisome proliferator-activated receptor-gamma (PPAR-γ), respectively, in activated HSCs...
May 21, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29792879/astragaloside-suppresses-apoptosis-of-the-podocytes-in-rats-with-diabetic-nephropathy-via-mir-378-traf5-signaling-pathway
#16
Xiao Lei, Bo-da Zhang, Ji-Gang Ren, Fang-Li Luo
AIMS: Apoptosis of podocytes plays a crucial role in diabetic nephropathy (DN) development, and astragaloside (AS-IV) has a significant impact on podocyte apoptosis. This study aims to explore the effect of AS-IV on diabetic nephropathy progression. MATERIALS AND METHODS: The diabetic nephropathy model was established in rats with streptozotocin (STZ) injection. The albuminuria was examined by using the enzyme linked immunosorbent assay (ELISA). The expression of miR-378, tumor-necrosis factor (TNF) receptor (TNFR)-associated factor 5 (TRAF5) mRNA and protein was analyzed by qRT-PCR and western blot, respectively...
May 21, 2018: Life Sciences
https://www.readbyqxmd.com/read/29792870/peripheral-complement-interactions-with-amyloid-%C3%AE-peptide-in-alzheimer-s-disease-polymorphisms-structure-and-function-of-complement-receptor-1
#17
Jenny U Johansson, William D Brubaker, Harold Javitz, Andrew W Bergen, Denise Nishita, Abhishek Trigunaite, Andrés Crane, Justine Ceballos, Diego Mastroeni, Andrea J Tenner, Marwan Sabbagh, Joseph Rogers
INTRODUCTION: Genome-wide association studies consistently show that single nucleotide polymorphisms (SNPs) in the complement receptor 1 (CR1) gene modestly but significantly alter Alzheimer's disease (AD) risk. Follow-up research has assumed that CR1 is expressed in the human brain despite a paucity of evidence for its function there. Alternatively, erythrocytes contain >80% of the body's CR1, where, in primates, it is known to bind circulating pathogens. METHODS: Multidisciplinary methods were employed...
May 21, 2018: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/29792868/ah6809-decreases-production-of-inflammatory-mediators-by-pge-2-ep2-camp-signaling-pathway-in-an-experimentally-induced-pure-cerebral-concussion-in-rats
#18
Ping Li, Hongyan Jiang, Haiying Wu, Deye Wu, Hengxi Li, Jianyun Yu, Jianghua Lai
Increasing evidence suggests that PGE2 metabolic pathway is involved in pathological changes of the secondary brain injury after traumatic brain injury. However, the underlying mechanisms, in particular, the correlation between various key enzymes and the brain injury, has remained to be fully explored. More specifically, it remains to be ascertained whether AH6809 (an EP2 receptor antagonist) would interfere with the downstream of the PGE2 , regulate the inflammatory mediators and improve neuronal damage in the hippocampus by PGE2 - EP2 - cAMP signaling pathway...
May 21, 2018: Brain Research
https://www.readbyqxmd.com/read/29792867/effects-of-amphetamine-exposure-during-adolescence-on-behavior-and-prelimbic-cortex-neuron-activity-in-adulthood
#19
Luke K Sherrill, Joshua M Gulley
Repeated exposure to psychostimulants during adolescence produces long-lasting changes in behavior that may be mediated by disrupted development of the mesocorticolimbic dopamine system. Here, we tested this hypothesis by assessing the effects of amphetamine (AMPH) and dopamine receptor-selective drugs on behavior and neuron activity in the prelimbic region of the medial prefrontal cortex (PFC). Adolescent male, Sprague-Dawley rats were given saline or 3 mg/kg AMPH between postnatal day (P) 27 and P45. In Experiment 1, locomotor behavior was assessed during adulthood following challenges with a dopamine D1 (SKF 82958) or D2 (quinpirole) receptor-selective agonist...
May 21, 2018: Brain Research
https://www.readbyqxmd.com/read/29792859/long-non-coding-rna-miat-is-estrogen-responsive-and-promotes-estrogen-induced-proliferation-in-er-positive-breast-cancer-cells
#20
Yuehua Li, Baohong Jiang, Xiaoping Wu, Qin Huang, Wenqi Chen, Hongbo Zhu, Xiaofei Qu, Liming Xie, Xin Ma, Guo Huang
Estrogen drives the development and progression of estrogen receptor (ER)-positive breast cancer. However, the detailed mechanism underlying ER-driven carcinogenesis remains unclear despite extensive studies. Previously reports indicated higher expression of long non-coding RNA (lncRNA) myocardial infarction associated transcript (MIAT) in ER-positive breast cancer tissues than in ER-negative tissues. However, the functional relevance of MIAT in ER-positive breast cancer tumorigenesis was poorly understood...
May 21, 2018: Biochemical and Biophysical Research Communications
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