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European Journal of Pharmacology

Eduardo C Alexandre, Fabiano B Calmasini, Amanda C da S Sponton, Mariana G de Oliveira, Diana M André, Fábio H Silva, Maria Andréia Delbin, Fabíola Z Mónica, Edson Antunes
Obese mice display overactive bladder (OAB) associated with impaired urethra smooth muscle (USM) function. In this study, we evaluated the role of the adipose tissue surrounding the urethra and prostate in obese mice (here referred as periprostatic adipose tissue; PPAT) to the USM dysfunction. Male C57BL6/JUnib mice fed with either a standard-chow or high-fat diet to induce obesity were used. In PPAT, histological analysis, and qPCR analysis for gp91phox, tumor necrosis factor-α (TNF-α) and superoxide dismutase (SOD) were conducted...
August 10, 2018: European Journal of Pharmacology
Isadora Braga Contreiras Carneiro, Ana Elisa Toscano, Diego Cabral Lacerda, Marcela de Sá Barreto da Cunha, Raul Manhães de Castro, Tereza Cristina Bonfim de Jesus Deiró, Jairza Maria Barreto Medeiros
The amino acid tryptophan (2-Amino-3-(lH-indol-3-yl)-propanoic acid; Trp) is a precursor of the neurotransmitter serotonin (5-hydroxytryptamine; 5-HT) that performs various brain functions. The administration of Trp is used in experimental studies to manipulate the serotonergic system, however the dose of Trp required to raise brain 5-HT levels is controversial. The aim of this study was to systemically review the effect of the administration of different doses of Trp on cerebral 5-HT levels. Two independent authors conducted a systematic review in the electronic databases...
August 8, 2018: European Journal of Pharmacology
M Carmen Blanco-Gandía, Marta Rodríguez-Arias
Addiction pharmacotherapy aims to prevent drug abstinence symptoms, reduce drug craving and relapse, and normalize physiologic functions disrupted by chronic use of the drug. During the last 50 years, there has been an enormous revolution in pharmacotherapy for drug addiction. From abstinence as practically the only treatment option available, there are now multiple drugs on the market that have proved their efficacy in treating opiate and alcohol disorders. The present review will focus on the pharmacological treatments of the drugs whose consumption most affects individuals and society: alcohol and opiates...
August 7, 2018: European Journal of Pharmacology
Sung Pyo Hong, Dongoh Han, Ki-Ho Chang, Soon Kil Ahn
11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is a cortisol regenerating enzyme that amplifies tissue glucocorticoid levels, especially in the liver and adipose tissue. Knockout mice or a selective inhibitor of 11β-HSD1 improves metabolic syndrome parameters in preclinical models and human clinical trials. Here, we evaluated the therapeutic potential of INU-101, a potent and selective oral inhibitor of 11β-HSD1. The in vitro activity of 11β-HSD1 was measured using the homogeneous time-resolved fluorescence (HTRF) assay...
August 7, 2018: European Journal of Pharmacology
Hongshuang Qin, Wei Li, Ying Sun, Yongli Bao, Luguo Sun, Zhenbo Song, Lihua Zheng, Yuqing Zhao, Yuxin Li
Endoplasmic reticulum (ER) stress, together with unfolded protein response (UPR), can remove unfolded proteins and promote survival. However, severe and prolonged ER stress leads to cell death, tissue injury, and many serious diseases. Therefore, it is essential to identify drugs that can attenuate ER stress for ER-related disease treatment. A great deal of research shows that selenoprotein S (SelS) is a sensitive and ideal marker of ER stress. Here, we used a firefly luciferase reporter driven by SelS gene promoter to screen natural compounds that can attenuate ER stress...
August 7, 2018: European Journal of Pharmacology
Hong-Bo Xiao, Lin Liang, Zhi-Feng Luo, Zhi-Liang Sun
N-acetylgalactosaminyltransferase 2-Angiopoietin-like protein 3-lipoprotein lipase (GALNT2-ANGPTL3-LPL) pathway may be a useful pharmacologic objective for dyslipidemia. The present study was conducted to test the effect of paeoniflorin, a monoterpene Glycoside, on dyslipidemia in mice. Fifty mice were randomly divided into five groups (n =10): three groups of apolipoprotein E-null (ApoE-/- ) mice treated with paeoniflorin (10 or 20 or 30mg/kg/day), untreated ApoE-/- mice group, and C57BL/6J control group. Six weeks after treatment, expression of hepatic ANGPTL3, hepatic GALNT2 and adipose tissue LPL, lipid levels in the liver and blood were quantified...
August 7, 2018: European Journal of Pharmacology
Joshua A Burk, Sarah A Blumenthal, Eden B Maness
Early philosophers and psychologists defined and began to describe attention. Beginning in the 1950's, numerous models of attention were developed. This corresponded with an increased understanding of pharmacological approaches to manipulate neurotransmitter systems. The present review focuses on the knowledge that has been gained about these neurotransmitter systems with respect to attentional processing, with emphasis on the functions mediated within the medial prefrontal cortex. Additionally, the use of pharmacotherapies to treat psychiatric conditions characterized by attentional dysfunction are discussed...
August 6, 2018: European Journal of Pharmacology
Phil Skolnick
Naloxone is a specific, high affinity opioid antagonist that has been used to treat suspected or confirmed overdose for more than 40 years. Naloxone use was initially confined to an emergency room setting, but the dramatic rise in opioid overdose events over the past two decades has, with increasing frequency, shifted naloxone use to first responders including police, emergency medical technicians, and the friends and family of overdose victims. The opioids responsible for overdose events have also evolved, from prescription opioids to heroin and most recently, very high potency synthetic opioids such as fentanyl...
August 6, 2018: European Journal of Pharmacology
Mahsa Hassanipour, Nazanin Rajai, Nastaran Rahimi, Iman Fatemi, Mitra Jalali, Reihaneh Akbarian, Ali Shahabaddini, Amirhossein Nazari, Hossein Amini-Khoei, Ahmad Reza Dehpour
Sumatriptan, a 5HT (5-hydroxytryptamine)1B/1D receptor agonist, showed neuroprotection in different studies. The aim of the present study was to investigate the effect of sumatriptan on morphine-induced antinociceptive tolerance and physical dependence. We also investigated the possible role of nitric oxide (NO) on sumatriptan effects. Tolerance was induced by morphine injection (50, 50, 75 mg/kg) three times daily for five days. Antinociceptive latency after acute and chronic treatment with sumatriptan (0...
August 6, 2018: European Journal of Pharmacology
Artur Beberok, Zuzanna Rzepka, Michalina Respondek, Jakub Rok, Daniel Sierotowicz, Dorota Wrześniok
Fluoroquinolones are a known synthetic group of antibiotics that have been the subject of many research interests. This class of antibiotics was shown to be cytotoxic towards various cancer cell lines, thus representing a potentially important source of new anticancer agents. The present study was designed to examine the effect of ciprofloxacin and moxifloxacin on cell viability, redox balance and apoptosis in U87MG glioblastoma cells. Herein, we found that both fluoroquinolones decrease the viability and exert an anti-proliferative effect on U87MG cells...
August 4, 2018: European Journal of Pharmacology
Yuriko Watanabe, Yuri Aono, Masamichi Komiya, John L Waddington, Tadashi Saigusa
The nucleus accumbens contains delta-opioid receptors that may decrease inhibitory neurotransmission. As GABAB receptors inhibit dopamine release, decrease in activation of GABAB receptors may be a mediator of delta-opioid receptor-induced accumbal dopamine efflux. If so, accumbal dopamine efflux induced by delta-opioid receptor activation should be suppressed by stimulating GABAB receptors. As delta-opioid receptors are further subdivided into delta1- and delta2-opioid receptors, we analysed the effects of the GABAB receptor agonist baclofen on delta1- and delta2-opioid receptor-mediated accumbal dopamine efflux in freely moving rats using in vivo microdialysis...
August 4, 2018: European Journal of Pharmacology
Karl-Ludwig Bruchhage, Michael Koennecke, Maren Drenckhan, Kirstin Plötze-Martin, Ralph Pries, Barbara Wollenberg
Chronic rhinosinusitis with nasal polyps (CRSwNP) represents a benign neoplasm of the nasal mucosa, which leads to a decreased breathing capacity and reduced olfaction. The pathogenesis and the molecular mechanisms driving nasal polyps are not very well known. GSK-3 is involved in the regulation of various biosynthetic pathways and various kinases are able to regulate the GSK-3. Therefore, we investigated the effect of the monoterpene oxide 1,8-cineol on the regulation of the Wnt/β-catenin signaling pathway with its central regulator protein GSK-3 in vitro...
August 3, 2018: European Journal of Pharmacology
Shilpi Singh, Vijaya Dubey, Abha Meena, Lubna Siddiqui, Anil Kumar Maurya, Suaib Luqman
Rutin, a polyphenolic plant flavonoid, is found in citrus fruits, mulberry, cranberries and buckwheat with reported anti-diabetic, anti-fungal, anti-inflammatory and anti-bacterial activity. We appraise the effect of rutin on hydrogen peroxide (H2 O2 ) mediated deregulation of antioxidant enzyme activity, non-enzymatic biomarkers, reactive oxygen species production (in vitro and in vivo) and on echinocyte formation (ex-vivo). In addition to it the interaction studies (in silico) against targeted enzymes and membrane proteins were also performed...
July 31, 2018: European Journal of Pharmacology
Zhiwen Wang, Ai Zhang, Weixin Meng, Tingting Wang, Dandan Li, Zonghong Liu, Hongyu Liu
Ischemia-reperfusion injury (IRI) is a major cause of lung dysfunction during cardiovascular surgery, heart transplantation and cardiopulmonary bypass procedures, and the inflammatory response, oxidative stress, and apoptosis play key and allegedly maladaptive roles in its pathogenesis. The aim of this study was to initially elucidate whether ozone induces oxidative preconditioning by activating nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and secondly to determine whether ozone oxidative preconditioning (OzoneOP) protects the lung from IRI by attenuating nucleotide-binding oligomerization domain-like receptor containing pyrin domain 3 (NLRP3)-mediated inflammation, enhancing the antioxidant activity of Nrf2 and inhibiting apoptosis...
July 31, 2018: European Journal of Pharmacology
Hayley Heers, Jennifer Stanislaw, John Harrelson, Michael W Lee
Breast cancer is one of the leading causes of cancer-related death among women. A significant challenge in treating breast cancer is the limited array of therapeutic options and the rapid development of resistance to existing agents. Indeed, breast cancer patients, particularly those with hormone-receptor (HR)-positive breast cancer, initially respond to systemic treatment with cytotoxic, hormonal, and immunotherapeutic agents but frequently progress to a more advanced disease that is refractory to therapy...
July 31, 2018: European Journal of Pharmacology
Xiao-Wen Zhang, Shu Wang, Peng-Fei Tu, Ke-Wu Zeng
Apoptosis is an essential type of programmed cell death. Previous studies have demonstrated that a wide range of natural-derived anticancer agents induce apoptosis by trigging oxidative stress. Artemisia argyi is a traditional Chinese herb for treating diverse diseases including dyspepsia, arthroncus, and anaphylactic disease. In this study, sesquiterpene lactone 3 (SL3), a bioactive ingredient isolated from Artemisia argyi was found to show obvious inhibitory effect on two gastric carcinoma cells. Mechanism study revealed that SL3 promoted the membrane translocation of p47, activated nicotinamide adenine dinucleotide (NADPH) oxidase, and evaluated intracellular reactive oxygen species production, leading to the activation of mitochondria-dependent caspase apoptosis pathway...
July 31, 2018: European Journal of Pharmacology
S Maya, T Prakash, Divakar Goli
Al exposure causes an alteration in the several ions in the body and causes toxicity. Such as apoptosis, oxidative stress, disruption in neuronal transport, mitochondrial damage, excitotoxicity, generation of inflammatory mediators, and microglial activation. These multiple mechanisms lead to the several neurodegenerative diseases, including sporadic amyotrophic lateral sclerosis (sALS). The study aims to unravel the mechanisms behind the neuroprotective effects of wedelolactone (WL) and gallic acid (GA) against aluminium-induced neurodegeneration and thereby to unlock a platform to find a cure for sALS...
July 31, 2018: European Journal of Pharmacology
Ashish Mourya, Ansab Akhtar, Swati Ahuja, Sangeeta Pilkhwal Sah, Anil Kumar
Chronic restraint stress (CRS) is known to cause metabolic and neurological complications in a number of ways. Prolonged exposure to stress evident by increased corticosterone level led to impaired altered insulin signaling and oxidative stress in mice, in the present study. Impaired insulin signaling or insulin resistance was characterised by hyperglycemia, hyperinsulinemia, hyperlipidmia, hypoadiponectinemia, increased glycosylated hemoglobin and HOMA-IR. It was also associated with increased proinflammatory cytokine TNF-α levels...
July 31, 2018: European Journal of Pharmacology
Ziyi Li, Fazhang Zhao, Yonggang Cao, Jingyan Zhang, Pilong Shi, Xueying Sun, Feng Zhang, Liquan Tong
Hepatic ischemia reperfusion (I/R) injury is very common in liver transplantation and major liver surgeries and may cause liver failure or even death. Docosahexaenoic acid (DHA) has displayed activities in reducing oxidative stress and inflammatory reaction in many disorders. In the present study, we investigated the protective effects of DHA against I/R-induced injury and the underlying mechanisms. Here, we show that DHA protected hepatic I/R injury by reducing aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels and decreasing the oxidative stress in liver tissues...
July 31, 2018: European Journal of Pharmacology
Noha M Shawky, Lakshman Segar
Diet-induced obesity (DIO) is commonly associated with hyperleptinemia and leptin resistance. Leptin acts centrally to inhibit food intake and increase energy expenditure, thereby preventing body weight gain. Resistance to the biological effects of leptin represents a major obstacle in utilizing exogenously administered leptin as a treatment option for obesity. Of importance, recent studies demonstrate that naturally occurring compounds improve leptin sensitivity in DIO mice, as revealed by anorectic and body weight-lowering effects...
July 28, 2018: European Journal of Pharmacology
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