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https://www.readbyqxmd.com/read/29458190/cannabinoids-prevent-depressive-like-symptoms-and-alterations-in-bdnf-expression-in-a-rat-model-of-ptsd
#1
Or Burstein, Noa Shoshan, Ravid Doron, Irit Akirav
Posttraumatic stress disorder (PTSD) is a debilitating condition highly comorbid with depression. The endocannabinoid (eCB) system and brain-derived neurotrophic factor (BDNF) are suggestively involved in both disorders. We examined whether cannabinoids can prevent the long-term depressive-like symptoms induced by exposure to the shock and situational reminders (SRs) model of PTSD. The CB1/2 receptor agonist WIN55,212-2 (0.5 mg/kg; i.p.), the fatty acid hydrolase (FAAH) inhibitor URB597 (0.3 mg/kg, i.p.) or vehicle were administered 2 h after severe shock...
February 16, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29458170/downregulation-of-metabotropic-glutamate-receptor-5-inhibits-hepatoma-development-in-a-neurotoxin-rotenone-induced-parkinson-s-disease-model
#2
Xiao Xu Bai, Li Gu, Hui Min Yang, Shao Song Xi, Ning Xia, Song Zhang, Hong Zhang
Clinical epidemiological studies have shown that there is a link between Parkinson's disease (PD) and cancer, but how PD regulates cancer development remains unknown. In our study, the effect of metabotropic glutamate receptor 5 (mGlu5 ) on hepatoma was explored in a rotenone-induced PD model both in vitro and in vivo. We found that conditioned media derived from MN9D dopaminergic neuronal cells by rotenone-induced toxicity inhibited the growth, migration, invasion and promoted apoptosis of Hepa1-6 cells, which corresponded with decreased expression of mGlu5 ...
February 16, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29458169/inhibition-of-microsomal-prostaglandin-e-synthase-1-facilitates-liver-repair-after-hepatic-injury-in-mice
#3
Nobuyuki Nishizawa, Yoshiya Ito, Koji Eshima, Hirotoki Ohkubo, Ken Kojo, Tomoyoshi Inoue, Joan Raouf, Per-Johan Jakobsson, Satoshi Uematsu, Shizuo Akira, Shuh Narumiya, Masahiko Watanabe, Masataka Majima
BACKGROUND & AIMS: Liver repair following hepatic ischemia/reperfusion (I/R) injury is crucial to survival. This study aims to examine the role of endogenous prostaglandin E2 (PGE2 ) produced by inducible microsomal PGE synthase-1 (mPGES-1), a terminal enzyme of PGE2 generation, in liver injury and repair following hepatic I/R. METHODS: mPGES-1 deficient (mPGES-1-/- ) mice or their wild counterparts (WT) were subjected to partial hepatic ischemia followed by reperfusion...
February 16, 2018: Journal of Hepatology
https://www.readbyqxmd.com/read/29458160/gambogic-acid-sensitizes-breast-cancer-cells-to-trail-induced-apoptosis-by-promoting-the-crosstalk-of-extrinsic-and-intrinsic-apoptotic-signalings
#4
Shengpeng Wang, Yingqi Xu, Chenyang Li, Hongxun Tao, Anqi Wang, Chenyu Sun, Zhangfeng Zhong, Xu Wu, Peng Li, Yitao Wang
Due to the ability of tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) to induce cancer cell apoptosis selectively, TRAIL has attracted significant interest in the treatment of cancer. However, although TRAIL triggers apoptosis in a broad range of cancer cells, most primary cancers are often intrinsically TRAIL-resistant, or acquire resistance after TRAIL treatment, evocating new strategies to overcome TRAIL resistance. Gambogic acid (GA), an active constituent of Garcinia Hanburyi (Teng Huang in Chinese), has been applied for thousands of years for medicinal uses, however, the potential effect of GA in combating cancer resistance remains poorly investigated...
February 16, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29458110/investigation-of-adhesive-interactions-in-the-specific-targeting-of-triptorelin-conjugated-peg-coated-magnetite-nanoparticles-to-breast-cancer-cells
#5
Jingjie Hu, Sina Youssefian, John Obayemi, Karen Malatesta, Nima Rahbar, Winston Soboyejo
The understanding of adhesive interaction at the nanoscale between functionalized nanoparticles and biological cells is of great importance to develop effective theranostic nanocarriers for targeted cancer therapy. Here, we report a combination of experimental and computational approaches to evaluate the adhesion between Triptorelin (a Luteinizing Hormone-Releasing Hormone (LHRH) agonist)-conjugated poly-(ethylene glycol) (PEG)-coated magnetite nanoparticles (Triptorelin-MNPs) and breast cells. The adhesion forces between Triptorelin-MNPs and normal/cancerous breast cells are obtained using atomic force microscopy...
February 16, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29458108/the-relaxin-receptor-as-a-therapeutic-target-perspectives-from-evolution-and-drug-targeting
#6
REVIEW
Ross A D Bathgate, Martina Kocan, Daniel J Scott, M Akhter Hossain, Sara V Good, Sergey Yegorov, Jan Bogerd, Paul Gooley
The peptide relaxin was first identified as an important circulating hormone during pregnancy over 90 years ago. Research over many years defined the numerous biological roles that relaxin plays throughout pregnancy in many mammalian species. These important biological actions have led to the testing of relaxin as a therapeutic agent for a number of indications. The discovery of the relaxin receptor, RXFP1, in 2002 facilitated the better understanding of the cellular targets of relaxin, its mechanism of action and enabled the development of relaxin mimetics and screening for small molecule agonists...
February 16, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29458080/transcriptomic-and-phenotypic-profiling-in-developing-zebrafish-exposed-to-thyroid-hormone-receptor-agonists
#7
Derik E Haggard, Pamela D Noyes, Katrina M Waters, Robert L Tanguay
There continues to be a need to develop in vivo high-throughput screening (HTS) and computational methods to screen chemicals for interaction with the estrogen, androgen, and thyroid pathways and as complements to in vitro HTS assays. This study explored the utility of an embryonic zebrafish HTS approach to identify and classify endocrine bioactivity using phenotypically-anchored transcriptome profiling. Transcriptome analysis was conducted on zebrafish embryos exposed to 25 estrogen-, androgen-, or thyroid-active chemicals at concentrations that elicited adverse malformations or mortality at 120 hours post-fertilization in 80% of animals exposed...
February 16, 2018: Reproductive Toxicology
https://www.readbyqxmd.com/read/29458074/subthalamic-nucleus-stimulation-dopaminergic-treatment-and-impulsivity-in-parkinson-s-disease
#8
Frédérique Fluchère, Borís Burle, Franck Vidal, Wery van den Wildenberg, Tatiana Witjas, Alexandre Eusebio, Jean-Philippe Azulay, Thierry Hasbroucq
BACKGROUND: Deep brain stimulation of the subthalamic nucleus (STN DBS) is known to increase response speed and lower response accuracy in Parkinson's disease (PD) patients. It has been proposed that this speed-accuracy tradeoff is due to enhanced sensitivity of the motor system to sensory information. An alternative possibility is that this effect is due to weakened suppressive processes. The two alternative interpretations can be tested by analyzing the electromyographic activity (EMG) of the response agonists when the patients perform conflict reaction time tasks...
February 16, 2018: Neuropsychologia
https://www.readbyqxmd.com/read/29458055/brain-activation-associated-to-olfactory-conditioned-same-sex-partner-preference-in-male-rats
#9
Genaro A Coria-Avila, Tamara Cibrian-Llanderal, Victor X Díaz-Estrada, Luis I García, Rebeca Toledo-Cárdenas, James G Pfaus, Jorge Manzo
Sexual preferences can be strongly modified by Pavlovian learning. For instance, olfactory conditioned same-sex partner preference can occur when a sexually naïve male cohabits with an scented male during repeated periods under the effects of enhanced D2-type activity. Preference is observed days later via social and sexual behaviors. Herein we explored brain activity related to learned same-sex preference (Fos-Immunoreactivity, IR) following exposure to a conditioned odor paired with same-sex preference. During conditioning trials males received either saline or the D2-type receptor agonist quinpirole (QNP) and cohabitated during 24 h with a stimulus male that bore almond scent on the back as conditioned stimulus...
February 16, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29457969/an-evaluation-of-the-operational-model-when-applied-to-quantify-functional-selectivity
#10
Xiao Zhu, David B Finlay, Michelle Glass, Stephen B Duffull
BACKGROUND AND PURPOSE: Functional selectivity describes the ability of ligands to differentially regulate multiple signalling pathways when coupled to a single receptor and the operational model is commonly used to analyse these data. Here, we assess the mathematical properties of the operational model and evaluate the impact of fixing parameters on model performance. EXPERIMENTAL APPROACH: The operational model was evaluated using both a mathematical identifiability analysis and simulation...
February 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29457784/hiv-latency-is-reversed-by-acss2-driven-histone-crotonylation
#11
Guochun Jiang, Don Nguyen, Nancie M Archin, Steven A Yukl, Gema Méndez-Lagares, Yuyang Tang, Maher M Elsheikh, George R Thompson, Dennis J Hartigan-O'Connor, David M Margolis, Joseph K Wong, Satya Dandekar
Eradication of HIV-1 (HIV) is hindered by stable viral reservoirs. Viral latency is epigenetically regulated. While the effects of histone acetylation and methylation at the HIV long-terminal repeat (LTR) have been described, our knowledge of the proviral epigenetic landscape is incomplete. We report that a previously unrecognized epigenetic modification of the HIV LTR, histone crotonylation, is a regulator of HIV latency. Reactivation of latent HIV was achieved following the induction of histone crotonylation through increased expression of the crotonyl-CoA-producing enzyme acyl-CoA synthetase short-chain family member 2 (ACSS2)...
February 19, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29456930/review-of-the-evidence-for-the-management-of-co-morbid-tic-disorders-in-children-and-adolescents-with-attention-deficit-hyperactivity-disorder
#12
REVIEW
Michael O Ogundele, Hani F Ayyash
Attention deficit hyperactivity disorder (ADHD) is the most common neurodevelopmental disorder in children and adolescents, with prevalence ranging between 5% and 12% in the developed countries. Tic disorders (TD) are common co-morbidities in paediatric ADHD patients with or without pharmacotherapy treatment. There has been conflicting evidence of the role of psychostimulants in either precipitating or exacerbating TDs in ADHD patients. We carried out a literature review relating to the management of TDs in children and adolescents with ADHD through a comprehensive search of MEDLINE, EMBASE, CINAHL and Cochrane databases...
February 8, 2018: World Journal of Clinical Pediatrics
https://www.readbyqxmd.com/read/29456864/curative-gnrha-treatment-has-an-unexpected-repressive-effect-on-sertoli-cell-specific-genes
#13
Katharina Gegenschatz-Schmid, Gilvydas Verkauskas, Philippe Demougin, Vytautas Bilius, Darius Dasevicius, Michael B Stadler, Faruk Hadziselimovic
Background: Follicle stimulating hormone and testosterone stimulate Sertoli cells to support germ cell function and differentiation. During mini-puberty, when gonadotropin (GnRH) stimulates increases in plasma luteinizing hormone (LH) and testosterone levels, gonocytes are transformed into Ad spermatogonia. In cryptorchidism, impaired gonadotropin secretion during mini-puberty results in insufficient LH and testosterone secretion, impaired gonocyte transition to Ad spermatogonia, and perturbed Sertoli cell proliferation...
2018: Basic and Clinical Andrology
https://www.readbyqxmd.com/read/29456799/from-ror%C3%AE-t-agonist-to-two-types-of-ror%C3%AE-t-inverse-agonists
#14
Yonghui Wang, Wei Cai, Ting Tang, Qian Liu, Ting Yang, Liuqing Yang, Yingli Ma, Guifeng Zhang, Yafei Huang, Xiaoxia Song, Lisa A Orband-Miller, Qianqian Wu, Ling Zhou, Zhijun Xiang, Jia-Ning Xiang, Stewart Leung, Liming Shao, Xichen Lin, Mercedes Lobera, Feng Ren
Biaryl amides as new RORγt modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with RORγt ligand binding domain (LBD) was resolved, and both "short" and "long" inverse agonists were obtained by removing from 6 or adding to 6 a proper structural moiety. While "short" inverse agonist ( 8 ) recruits a corepressor peptide and dispels a coactivator peptide, "long" inverse agonist ( 9 ) dispels both. The two types of inverse agonists can be utilized as potential tools to study mechanisms of Th17 transcriptional network inhibition and related disease biology...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456644/eudesmin-attenuates-helicobacter-pylori-induced-epithelial-autophagy-and-apoptosis-and-leads-to-eradication-of-h-pylori-infection
#15
Jai-Sing Yang, Chao-Min Wang, Chiu-Hsian Su, Han-Chen Ho, Chiung-Hung Chang, Chang-Hung Chou, Yuan-Man Hsu
Eudesmin has been proven to possess anti-inflammatory effects. In the present study, the effects of eudesmin on Helicobacter pylori (H. pylori) -mediated autophagy, apoptosis, immune response and inflammation were determined in human gastric adenocarcinoma (AGS) cells in vitro and in C57BL/6 mice in vivo . Detection of the production of interleukin (IL)-8, IL-1β and immunoglobulin M (IgM) was performed using ELISA. Identification of the activation of apoptosis-associated caspase-3, -8 and -9 proteins, Bcl-2-associated X protein (Bax) and BH3 interacting domain death agonist (Bid) protein, was determined through western blot analysis...
March 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29456535/liver-x-receptor-agonist-therapy-prevents-diffuse-alveolar-hemorrhage-in-murine-lupus-by-repolarizing-macrophages
#16
Shuhong Han, Haoyang Zhuang, Stepan Shumyak, Jingfan Wu, Chao Xie, Hui Li, Li-Jun Yang, Westley H Reeves
The generation of CD138+ phagocytic macrophages with an alternative (M2) phenotype that clear apoptotic cells from tissues is defective in lupus. Liver X receptor-alpha (LXRα) is an oxysterol-regulated transcription factor that promotes reverse cholesterol transport and alternative (M2) macrophage activation. Conversely, hypoxia-inducible factor 1-α (HIF1α) promotes classical (M1) macrophage activation. The objective of this study was to see if lupus can be treated by enhancing the generation of M2-like macrophages using LXR agonists...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29456511/p2y-12-receptors-in-tumorigenesis-and-metastasis
#17
REVIEW
Patrizia Ballerini, Melania Dovizio, Annalisa Bruno, Stefania Tacconelli, Paola Patrignani
Platelets, beyond their role in hemostasis and thrombosis, may sustain tumorigenesis and metastasis. These effects may occur via direct interaction of platelets with cancer and stromal cells and by the release of several platelet products. Platelets and tumor cells release several bioactive molecules among which a great amount of adenosine triphosphate (ATP) and adenosine diphosphate (ADP). ADP is also formed extracellularly from ATP breakdown by the ecto-nucleoside-triphosphate-diphosphohydrolases. Under ATP and ADP stimulation the purinergic P2Y1 receptor (R) initiates platelet activation followed by the ADP-P2Y12 R-mediated amplification...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456508/the-molecular-determinants-of-small-molecule-ligand-binding-at-p2x-receptors
#18
Gaia Pasqualetto, Andrea Brancale, Mark T Young
P2X receptors are trimeric eukaryotic ATP-gated cation channels. Extracellular ATP-their physiological ligand-is released as a neurotransmitter and in conditions of cell damage such as inflammation, and substantial evidence implicates P2X receptors in diseases including neuropathic pain, cancer, and arthritis. In 2009, the first P2X crystal structure, Danio rerio P2X4 in the apo - state, was published, and this was followed in 2012 by the ATP-bound structure. These structures transformed our understanding of the conformational changes induced by ATP binding and the mechanism of ligand specificity, and enabled homology modeling of mammalian P2X receptors for ligand docking and rational design of receptor modulators...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456505/deletion-of-trace-amine-associated-receptor-1-attenuates-behavioral-responses-to-caffeine
#19
Michael D Schwartz, Jeremiah B Palmerston, Diana L Lee, Marius C Hoener, Thomas S Kilduff
Trace amines (TAs), endogenous amino acid metabolites that are structurally similar to the biogenic amines, are endogenous ligands for trace amine-associated receptor 1 (TAAR1), a GPCR that modulates dopaminergic, serotonergic, and glutamatergic activity. Selective TAAR1 full and partial agonists exhibit similar pro-cognitive, antidepressant- and antipsychotic-like properties in rodents and non-human primates, suggesting TAAR1 as a novel target for the treatment of neurological and psychiatric disorders. We previously reported that TAAR1 partial agonists are wake-promoting in rats and mice, and that TAAR1 knockout (KO) and overexpressing mice exhibit altered sleep-wake and EEG spectral composition...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456408/inhibitory-effects-of-patchouli-alcohol-on-stress-induced-diarrhea-predominant-irritable-bowel-syndrome
#20
Tian-Ran Zhou, Jing-Jing Huang, Zi-Tong Huang, Hong-Ying Cao, Bo Tan
AIM: To elucidate the mechanism of patchouli alcohol (PA) in treatment of rat models of diarrhea-predominant irritable bowel syndrome (IBS-D). METHODS: We studied the effects of PA on colonic spontaneous motility using its cumulative log concentration (3 × 10-7 mol/L to 1 × 10-4 mol/L). We then determined the responses of the proximal and distal colon segments of rats to the following stimuli: (1) carbachol (1 × 10-9 mol/L to 1 × 10-5 mol/L); (2) neurotransmitter antagonists including Nω -nitro-L-arginine methyl ester hydrochloride (10 μmol/L) and (1R*, 2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3...
February 14, 2018: World Journal of Gastroenterology: WJG
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