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European Journal of Pharmacology

Bruno Lima Linhares, Nilberto Robson Falcão Nascimento, Lúcio Flávio Gonzaga-Silva, Cláudia Ferreira Santos, Manoel Odorico Moraes, Lucas Bernardo Marinho, Ana Patrícia Gonçalves Silva, Manassés Claudino Fonteles, Ricardo Reges
The purpose of this study was to evaluate in vitro the effect of the combination of BRL 37344 (ß3 -adrenoceptor agonist) with tadalafil (phosphodiesterase type 5 inhibitor) or rolipram (phosphodiesterase type 4 inhibitor) in an experimental model of detrusor overactivity. The experiments were carried out in two phases using bladder strips of mice. In the first phase, on the top of 40mM potassium-induced contraction, strips isolated from control mice were exposed to increasing concentrations of each study drug...
June 15, 2018: European Journal of Pharmacology
Yu Wan, Lu Xu, Yunxia Wang, Nuerbiya Tuerdi, Min Ye, Rong Qi
Cardiac fibrosis is a common feature of many cardiac pathophysiologic conditions. Recently, it has been shown that the activation of NLRP3 inflammasome plays an important role in the pathophysiology of cardiac fibrosis. Here, the inhibitory effects and possible mechanism of astragaloside IV (AST) and its active sapogenin cycloastragenol (CAG) on isoproterenol (ISO)-induced cardiac fibrosis were investigated. In our study, BALB/c mice were subcutaneously injected with 5mg/kg ISO for 7 consecutive days to induce cardiac fibrosis...
June 15, 2018: European Journal of Pharmacology
Xu-Hua Duan, Hao Li, Xin-Wei Han, Jian-Zhuang Ren, Feng-Yao Li, Shu-Guang Ju, Peng-Fei Chen, Dong-Lin Kuang
Increasing evidences suggested that insufficient radiofrequency ablation (RFA) can paradoxically promote tumor invasion and metastatic processes, while the effects of moderate hyperthermia on cancer progression are not well illustrated. Our present study confirmed moderate hyperthermia treatment can promote the proliferation, migration and invasion of hepatocellular carcinoma (HCC) cells, which was evidenced by the results that moderate hyperthermia induced up regulation of proliferating cell nuclear antigen (PCNA) and matrix metalloproteinase-2 (MMP-2)...
June 9, 2018: European Journal of Pharmacology
Anders Sonne Munch, Arnela Saljic, Kim Boddum, Morten Grunnet, Charlotte Hougaard, Thomas Jespersen
Progressive myoclonus epilepsies (PMEs) constitute a cluster of inherent, genetically diverse, rare seizure disorders characterized by ataxia, tonic-clonic seizures, and action myoclonus. Recently, a mutation in the KCNC1 gene (Arg320His) was described in a group of PME patients. The KCNC1 gene encodes the Kv 3.1 potassium ion channel responsible for the rapid repolarization of the membrane potential following action potential firing in fast spiking GABAergic interneurons (FSI), thereby enabling high firing frequency...
June 9, 2018: European Journal of Pharmacology
Branka Djordjevic, Tatjana Cvetkovic, Tatjana Jevtovic Stoimenov, Milena Despotovic, Slavoljub Zivanovic, Jelena Basic, Andrej Veljkovic, Aleksandra Velickov, Gordana Kocic, Dusica Pavlovic, Dusan Sokolovic
Hyperglycemia mediated oxidative stress and pro-angiogenic molecules such as vascular endothelial growth factor (VEGF) and matrix metalloproteinase 9 (MMP9) are considered important for diabetic retinopathy onset and progression. Melatonin is a pineal hormone that regulates circadian and seasonal rhythms and most likely is involved in regulating glucose metabolism. We aimed to evaluate the potential benefit of melatonin supplementation to the pre-diabetic retina by assessing melatonin effects on lipid peroxidation (thiobarbituric acid reactive substances, TBARS), protein oxidation (advanced oxidation protein products, AOPP) and concentrations of inducible nitric oxide synthase (iNOS), VEGF and MMP9 in the retina of rats with pre-diabetes...
June 8, 2018: European Journal of Pharmacology
Meng Chen, Wenyan Zou, Miaomiao Chen, Liang Cao, Jianhua Ding, Wei Xiao, Gang Hu
Ginkgolide K (GK) is a new compound extracted from the leaves of Ginkgo biloba, which has been recognized to exert anti-oxidative stress and neuroprotective effect on ischemic stroke. While whether it plays an enhanced effect on angiogenesis during ischemic stroke remains unknown. The aim of this study was to investigate the effect of ginkgolide K on promoting angiogenesis as well as the protective mechanism after cerebral ischemia-reperfusion. Using the transient middle cerebral artery occlusion (tMCAO) mouse model, we found that GK (3...
June 8, 2018: European Journal of Pharmacology
Manuella da L D Barros, Raul Manhães-de-Castro, Daniele T Alves, Omar Guzmán Quevedo, Ana Elisa Toscano, Alexandre Bonnin, Ligia Galindo
Serotonin exerts a modulating function on the development of the central nervous system, including hypothalamic circuits controlling feeding behavior and energy expenditure. Based on the developmental plasticity theory, early disturbances of synaptic availability of serotonin may promote phenotypic adaptations and late disorders of energy balance regulation leading to obesity and associated diseases. The aim of this systematic review is to determine the effects of pharmacological neonatal inhibition of serotonin reuptake by fluoxetine, on parameters related to feeding behavior and energy balance...
June 8, 2018: European Journal of Pharmacology
Masahide Fujita, Ryuta Tamano, Sosuke Yoneda, Shigeki Omachi, Erika Yogo, Masatomo Rokushima, Shunji Shinohara, Gaku Sakaguchi, Minoru Hasegawa, Toshiyuki Asaki
Microglia exhibit various activation phenotypes in the spinal cord after peripheral nerve injury, and promote neuropathic pain. Ibudilast is a phosphodiesterase inhibitor with anti-inflammatory activity, but its effect on activated microglia in chronic neuropathic pain is poorly understood. We investigated whether ibudilast was effective on established allodynia associated with activated microglial phenotypes in two rat models of peripheral and central neuropathic pain. A single intrathecal injection of ibudilast (25μg) inhibited established allodynia on days 7-21 after sciatic nerve injury in rats...
June 7, 2018: European Journal of Pharmacology
Chao Zhang, George W Booz, Qing Yu, Xiaochen He, Shaoxun Wang, Fan Fan
20-HETE is a cytochrome P450-derived metabolite of arachidonic acid that has both pro- and anti-hypertensive actions that result from modulation of vascular and kidney function. In the vasculature, 20-HETE sensitizes vascular smooth muscle cells to constrictor stimuli and increases myogenic tone. By promoting smooth muscle cell migration and proliferation, as well as by acting on the vascular endothelium to cause endothelial dysfunction, angiotensin converting enzyme (ACE) expression, and inflammation, 20-HETE contributes to adverse vascular remodeling and increased blood pressure...
June 7, 2018: European Journal of Pharmacology
Akira Shinohara, Tsugunobu Andoh, Ikuo Saiki, Yasushi Kuraishi
Fentanyl is an opioid commonly prescribed for cancer pain. Using melanoma-bearing mice, we investigated whether peripheral action would contribute to fentanyl analgesia in cancer pain. Intravenous injection of fentanyl inhibited mechanical nociception in healthy mice, which was markedly inhibited by the opioid antagonist naloxone, but not naloxone methiodide, a peripherally acting opioid antagonist. Melanoma-bearing mice showed mechanical allodynia and spontaneous licking, a pain-related behavior, which were suppressed by intravenous and local injections of fentanyl...
June 7, 2018: European Journal of Pharmacology
Rita Romani, Giorgia Manni, Chiara Donati, Irene Pirisinu, Caterina Bernacchioni, Marco Gargaro, Matteo Pirro, Mario Calvitti, Giorgia Manni, Francesco Bagaglia, Amirhossein Sahebkar, Graziano Clerici, Davide Matino, Giovanni Pomili, Gian Carlo Di Renzo, Vincenzo Nicola Talesa, Paolo Puccetti, Francesca Fallarino
Stem cells have high potential for cell therapy in regenerative medicine. We previously isolated stem cell types from human amniotic fluid, derived from prenatal amniocentesis. One type, characterized by a fast doubling time, was designated as fast human amniotic stem cells (fHASCs). These cells exhibited high differentiation potential and immunoregulatory properties. Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid metabolite that influences stem-cell pluripotency, differentiation, mobility, and regulates immune functions...
June 7, 2018: European Journal of Pharmacology
Shiwei Song, Abul Fajol, Yan Chen, Baogang Ren, Songsheng Shi
Epilepsy is associated with increased morbidity and mortality together and places a large financial burden on individuals and society. To evaluate the anticonvulsant action of protodioscin (PDSN) in experiments with animals with pilocarpine-induced convulsions. We assessed the activity of PDSN in pilocarpine induced seizures in combination with different agents which are acting via diverse receptors, such as atropine, memantine, nimodipine, diazepam, and flumazenil, to determine the exact receptors responsible for the action of PDSN...
June 7, 2018: European Journal of Pharmacology
Wei Han, Yu Zhu, Binchuan Chen, Subing Liu, Yalong Dang
In this study, we investigate the mechanism of 7,8,3'-Trihydroxyflavone (THF) on retinal oxidative stress and retinal ganglion cell (RGC) growth. Oxidative stress was induced by ocular hypertension (O.H.) in rat retina in vivo. Rats were then systemically injected with THF. We found THF ameliorated O.H.-induced oxidative stress in retina by reducing caspase-3 activity, downregulating MDA level and augmenting glutathione peroxidase expression. In addition, neonatal RGCs were cultured in vitro, and treated with THF...
June 7, 2018: European Journal of Pharmacology
Takaaki Kawano, Hidehiro Oshibuchi, Masahiko Kawano, Hiroyuki Muraoka, Takahiro Tsutsumi, Makiko Yamada, Jun Ishigooka, Katsuji Nishimura, Ken Inada
Although the benzodiazepine class of drugs has proven useful in treating anxiety symptoms, recent studies yield no consistent empirical support for their use in treating psychiatric disorders. However, animal studies using a fear conditioning paradigm have suggested that benzodiazepines facilitate fear memory extinction, dependent on treatment timing and subject conditions. However, we have no data on the effect of subject conditions. The purpose of this study was to investigate whether the effect of benzodiazepines depends on hypersensitivity to fear-memory processing...
June 6, 2018: European Journal of Pharmacology
Qinglian Wang, Fajuan Cheng, Ying Xu, Jing Zhang, Jianjun Qi, Xiang Liu, Rong Wang
Thymol is one of the most important dietary constituents in the thyme species and has been shown to possess anti-inflammatory properties both in vivo and in vitro. We investigated the protective effects of thymol on the lipopolysaccharide (LPS)-induced inflammatory responses in the human peritoneal mesothelial cell line (HMrSV5) to clarify the potential mechanism. HMrSV5 cells were stimulated with LPS in the presence or absence of thymol. Our results showed that thymol markedly suppressed the production of cytokines such as tumour necrosis factor α (TNF-α), interleukin (IL)-6, monocyte chemoattractant protein 1 (MCP-1) and α-smooth muscle actin (α-SMA) in a dose-dependent manner...
June 5, 2018: European Journal of Pharmacology
Joel A Johnson, Aaron P Montgomery, Eric R Starr, Justin Ludwig, Jennifer Trevitt
The present study examines the effect of three adenosine receptor antagonists on tremulous jaw movements (TJMs), an animal model of tremor. Forty-five rats were pre-treated with one adenosine antagonist: caffeine (0.0, 5.0, or 10.0mg/kg; non-selective adenosine receptor antagonist), 8-cyclopentyltheophylline (CPT; 0.0, 5.0, or 10.0mg/kg; selective adenosine A1 receptor antagonist), or SCH 58261 (0.0 or 8.0mg/kg; selective adenosine A2A receptor antagonist) followed by TJM induction with tacrine (0.0, 0.75, or 2...
June 5, 2018: European Journal of Pharmacology
Mohammad Reza Dorvash, Mohammad Javad Khoshnood, Hossein Saber, Amirreza Dehghanian, Pourya Mosaddeghi, Negar Firouzabadi
Gallstone disease (GD) is highly correlated with metabolic syndrome and its related illnesses including type II diabetes (DMII) and polycystic ovary syndrome (PCOS). While previous studies claimed that metformin decreases the chance of developing GD in PCOS patients, this phenomenon has not been investigated in animal models to date. Here we fed a high fat diet (HFD) containing 2% of cholesterol and 1% of cholic acid to ten-week-old male C57Bl/6 mice for 105 days. The groups were as follows: Low fat diet; HFD; HFD + Ursodeoxycholic acid (UDCA) (day 1-105); HFD + Metformin (day 1-105); HFD + Metformin (Met) (day 64-105)...
June 5, 2018: European Journal of Pharmacology
Davoud Sanajou, Amir Ghorbani Haghjo, Hassan Argani, Somayeh Aslani
Diabetic nephropathy is one of the most frequent micro-vascular complications both in type 1 and type 2 diabetic patients and is the leading cause of end-stage renal disease worldwide. Although disparate mechanisms give rise to the development of diabetic nephropathy, prevailing evidence accentuates that hyperglycemia-associated generation of advanced glycation end products (AGEs) plays a central role in the disease pathophysiology. Engagement of the receptor for AGE (RAGE) with its ligands provokes oxidative stress and chronic inflammation in renal tissues, ending up with losses in kidney function...
June 5, 2018: European Journal of Pharmacology
Rania G Abdel-Latif, Gehan H Heeba, Ashraf Taye, Mohamed M A Khalifa
Ischemic stroke is a major cause of neurological damage and brain dysfunction with consequent strong cerebral oxidative imbalance, inflammatory and apoptotic responses. Lixisenatide is a new potent glucagon-like peptide -1 (GLP-1) analogue that has been used clinically in the treatment of type II diabetes. Recent studies suggested the beneficial central effects of GLP-1-based therapies on different neurodegenerative diseases. This study aimed to investigate the ameliorative effect of lixisenatide in global cerebral ischemia-reperfusion (I/R) rat model and elaborate the underline mechanisms that could mediate the proposed activity...
June 1, 2018: European Journal of Pharmacology
Yan-Hong Chen, Wen-Jing Zeng, Zhi-Peng Wen, Quan Chen, Xiao-Ping Chen
Patients with somatic mutations of epigenetic regulators are characterized by aberrant chromatin modification patterns. Recent mechanistic studies pairing chemical tool compounds and deep-sequencing technology have greatly broadened our understanding of epigenetic regulation in glioma progression and underpinned alternative treatment of epigenetic inhibitors. However, the effect of most inhibitors is condition-dependent, and the overall results of clinical trials still have not been applied to patients. There is an intense need to develop more potent and specific compounds as well as identify the population who may achieve clinical benefits...
June 1, 2018: European Journal of Pharmacology
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