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European Journal of Pharmacology

Benjamin Huyts, Christian Brabant, Ezio Tirelli
Pitolisant, a selective inverse agonist for the histamine H3 receptor, is a new treatment for adults suffering from narcolepsy. Numerous studies have shown that striatal H3 receptors can modulate the activity of the dopamine mesolimbic system, a pathway that plays a crucial role in drug addiction. Therefore, it is important to guarantee that pitolisant has no abuse potential and does not potentiate the behavioral effects of psychostimulants. The present study tested the effects of pitolisant on cocaine reinforcement in C57BL/6J mice using the intravenous self-administration technique...
February 13, 2019: European Journal of Pharmacology
Junjie Hu, Yang Yang, Minli Wang, Yi Yao, Yanmin Chang, Quanwei He, Rong Ma, Gang Li
Neurofibrillary tangles aggregated from hyperphosphorylated tau protein are the main pathological feature of Alzheimer's disease (AD). Complement C3 (or C3a) is the core component of the complement system and is associated with AD pathological processes. However, it remains unclear whether C3a or the C3a receptor has any effect on tau phosphorylation. In this study, we found that exposure of SH-SY5Y cells to okadaic acid (OA) decreased cell viabilities and induced tau hyperphosphorylation. These effects were alleviated by C3a receptor antagonist SB290157 and were further validated by C3a receptor siRNA in OA-treated SH-SY5Y cells...
February 13, 2019: European Journal of Pharmacology
Rubén López, Pura Bolaños, Alis Guillén, Marbely C Fernández, Magaly Ramos, Sergio Granados, Andrés F Milán, Carlo Caputo, Claudia Alvarado-Castillo, Omar Estrada, Juan C Calderón
Pomolic acid (PA) isolated from Licania pittieri has hypotensive effects in rats, inhibits human platelet aggregation and elicits endothelium-dependent relaxation in rat aortic rings. The present study was designed to investigate the effects of PA on cardiomyocytes. Trabeculae and enzymatically isolated cardiomyocytes from rats were used to evaluate the concentration-dependent effects of PA on cardiac muscle tension and excitation-contraction coupling (ECC) by recording Ca2+ transients reported with Fluo-3 and Fura-2, as well as L-type Ca2+ currents (LTCC)...
February 13, 2019: European Journal of Pharmacology
Aniket V Mali, Subhash B Padhye, Shrikant Anant, Mahabaleshwar V Hegde, Shivajirao S Kadam
Currently cancer is the second leading cause of death globally and worldwide incidence and mortality rates of all cancers of males and females are rising tremendously. In spite of advances in chemotherapy and radiation, metastasis and recurrence are considered as the major causes of cancer related deaths. Hence there is a mounting need to develop new therapeutic modalities to treat metastasis and recurrence in cancers. A significant amount of substantiation from epidemiological, clinical and laboratory research highlights the importance of diet and nutrition in cancer chemoprevention...
February 13, 2019: European Journal of Pharmacology
Yan-Hong Li, Wei Sun, Bao-Jin Zhou, Adam Rosenstein, Jie Zhao, Jian Wang, Zhao-Xiang Bian
Previous studies by us and others have indicated that berberine is a promising therapy for ulcerative colitis (UC). However, the mechanisms of UC and the therapeutic targets of berberine are poorly understood. iTRAQ-based proteomics was utilized to characterize the proteins and pathways associated with the development of colitis and its improvement after berberine treatment. By using a dextran sodium sulfate (DSS) colitis as the UC model, we demonstrated that berberine significantly attenuated clinical symptoms and colon shorting of the colitis mice...
February 13, 2019: European Journal of Pharmacology
Jie Wu, Dan-Dan Li, Jia-Yao Li, Yi-Cong Yin, Peng-Chang Li, Ling Qiu, Li-Meng Chen
Cisplatin is a widely used chemotherapeutic drug that often causes acute kidney injury (AKI) in cancer patients. The contribution of miRNAs to the cisplatin-induced renal tubular epithelial cell injury remains largely unknown. Here we performed an integrative network analysis of miRNA and mRNA expression profiles to shed light into the underlying mechanism of cisplatin-induced renal tubular epithelial cell injury. Microarray analysis identified 47 differentially expressed miRNAs, among them 26 were upregulated and 21 were downregulated...
February 12, 2019: European Journal of Pharmacology
Grażyna Wójcicka, Mariusz Zaręba, Anna Warpas, Anna Jamroz-Wiśniewska, Marta Rusek, Grażyna Czechowska, Jerzy Bełtowski
Inflammation and oxidative stress are the two processes crucial in atherogenesis. Platelet-activating factor acetylhydrolase (PAF-AH), a plasma lipoprotein-associated enzyme, degrades pro-inflammatory lipids generated within oxidatively modified lipoproteins. Extensive evidence shows that incretin-based drugs, a new class of anti-diabetic agents, can provide cardiovascular protection that cannot be attributed to their glucose-lowering effects. The present study was undertaken to determine whether the antiatherogenic effects of the GLP-1(glucagon-like peptide-1) receptor agonist (exenatide) and DPP-4(dipeptidyl peptidase-4) inhibitors (sitagliptin) may occur via the regulation of platelet-activating factor acetylhydrolase (PAF-AH) activity/mass and inhibition of low-density lipoprotein (LDL) oxidation in the fructose-fed rats...
February 12, 2019: European Journal of Pharmacology
Xiaojiang Qin, Xiaomin Hou, Kun Zhang, Qingshan Li
The aim of this study was to investigate the relaxation effect of farrerol on rat aortic vascular smooth muscle cells (VSMCs) and its underlying mechanism. VSMCs were cultured primarily and were used to examine the relaxation effect of farrerol. Cells surface and length were measured by dynamic observation, or by rhodamine-phalloidin labeling and hematoxylin-eosin staining. Cells contractive activity were tested using collagen gel contraction assay. The [Ca2+ ]in was measured with molecular probe fluo-4-AM...
February 12, 2019: European Journal of Pharmacology
Yu Miyahara, Hideki Funahashi, Rumi Naono-Nakayama, Ayaka Haruta-Tsukamoto, Toshikazu Nishimori, Yasushi Ishida
The contribution of serotonin and noradrenaline to the modulation of pruriceptive processing was evaluated by administrating antidepressants or noradrenaline reuptake inhibitors. The pretreatment with milnacipran, a serotonin and noradrenaline reuptake inhibitor, and mirtazapine, a noradrenergic and specific serotonergic antidepressant, attenuated the induction of scratching behavior by chloroquine, a representative pruritogen, indicating the involvement of serotonin and/or noradrenaline in the modulation of pruriceptive processing...
February 11, 2019: European Journal of Pharmacology
Milad Iranshahy, Ramin Rezaee, Gholamreza Karimi
Metformin, as a dimethyl biguanide prescribed as the first-line medication for treatment of type 2 diabetes mellitus, is one of the most frequently used drugs, worldwide. However, the beneficial effects of metformin are not limited to insulin sensitizing and blood glucose lowering effects as recent clinical trials deciphered lower cancer risk in metformin users. In addition, metformin protected the liver against chemical or viral hepatotoxicants through various mechanisms including activation of AMPK via inhibition of mitochondrial complex I, inhibition of mitogen activated protein kinase (MAPK) and inhibition of Smads phosphorylation...
February 9, 2019: European Journal of Pharmacology
Silvia Cantoni, Stefano Cavalli, Fiorella Pastore, Alessandro Accetta, Daniele Pala, Fabio Vaccaro, Nicola Cesari, Francesco De Logu, Romina Nassini, Gino Villetti, Fabrizio Facchinetti
Studies on the role of Rho kinase (ROCK) in experimental pulmonary artery hypertension (PAH) relies mainly on the use of pharmacological inhibitors. However, interpreting these data is hampered by the lack of specificity of commonly utilized inhibitors. To fill this gap, we have selected and characterized a novel ROCK inhibitor, Compound 3, previously described in a patent. Inhibitory potency of Compound 3 against enzymatic activity of ROCK-1 and 2 (IC50 = 10 ± 3.1 and 7.8 ± 0.5nM, respectively) was accompanied by a strong vasodilating effect in phenylephrine pre-contracted isolated rat pulmonary artery rings (IC50 = 51...
February 9, 2019: European Journal of Pharmacology
Xiufeng Yu, Xijuan Zhao, Junting Zhang, YiYing Li, Ping Sheng, Cui Ma, Lixin Zhang, XueWei Hao, XiaoDong Zheng, Yan Xing, Hui Qiao, Lihui Qu, Daling Zhu
Accumulating evidence suggests that epidermal growth factor receptor (EGFR) plays a role in the progression of pulmonary arterial hypertension (PAH). Clinically-approved epidermal growth factor inhibitors such as gefitinib, erlotinib, and lapatinib have been explored for PAH . However, None of them were able to attenuate PAH . So, we explored the role of dacomitinib, a new pan-EGFR inhibitor, in PAH. Adult male Sprague-Dawley rats were used to study hypoxia- or monocrotaline-induced right ventricular remodeling as well as systolic function and hemodynamics using echocardiography and a pressure-volume admittance catheter...
February 9, 2019: European Journal of Pharmacology
Gessica Marchini, Silvia Carnevali, Fabrizio Facchinetti
Cigarette smokers with asthma and chronic obstructive pulmonary disease (COPD) are less responsive to glucocorticoids (GCs). The anti-inflammatory action of GCs depends also on their ability to transactivate genes such as GC-induced leucine zipper (GILZ). We investigated the effects of aqueous cigarette smoke extract (CSE) on GILZ transactivation evoked by 17-beclomethasone monopropionate (BMP) or fluticasone propionate (FP) in the presence or absence of the long acting β2-adrenoceptor agonist (LABA) bronchodilator formoterol or salmeterol in human primary cultures of human bronchial smooth muscle cells (HBSMC)...
February 9, 2019: European Journal of Pharmacology
Hiroshi Tsuneki, Hitomi Yoshida, Kentaro Okamoto, Misako Yamaguchi, Kosuke Endo, Ayumi Nakano, Masaaki Tsuda, Naoki Toyooka, Tsutomu Wada, Toshiyasu Sasaoka
Brain-derived neurotrophic factor (BDNF), an essential factor for maintaining brain functions, has been reported to be reduced in various neurological diseases, including Alzheimer's disease and major depression. Therefore, new drugs to increase the BDNF expression need to be developed. Since phosphatidylinositol (3,4,5)-trisphosphate, a membrane signaling molecule produced by phosphoinositide 3 (PI3)-kinase in the BDNF signaling, is a candidate target of SH2 domain-containing inositol 5' phosphatase 2 (SHIP2, a 5'-lipid phosphatase), the present study examined the effect of a SHIP2 inhibitor AS1949490 on Bdnf expression in cultured cortical neurons...
February 9, 2019: European Journal of Pharmacology
Ryosuke Segawa, Mika Shiraki, Shiori Sudo, Kenichi Shigeeda, Taiji Saito, Natsumi Mizuno, Takahiro Moriya, Takayuki Yonezawa, Je-Tae Woo, Masahiro Hiratsuka, Noriyasu Hirasawa
Thymic stromal lymphopoietin (TSLP) is a key epithelial-derived factor that aggravates allergic diseases. Therefore, TSLP inhibitors are candidate compounds for the treatment of allergic diseases. Previously, we reported that KCMH-1, a mouse keratinocyte cell line, constitutively produces TSLP. In this study, we tried to identify inhibitors of TSLP by screening 2169 compounds in KCMH-1 cells and found one such chalcone derivative (code no. 16D10). 16D10 inhibited TSLP expression and TSLP promoter activation in HaCaT cells, a human keratinocyte cell line...
February 9, 2019: European Journal of Pharmacology
Congjian Shi, Weiju Xue, Bowen Han, Fengli Yang, Yaping Yin, Chengmu Hu
Non-alcoholic fatty liver disease (NAFLD) is the most common chronic liver disease which affects millions of people worldwide. Acetaminophen (APAP) overdose is the leading cause of acute liver failure. In this study, APAP (50, 100, 200mg/kg) were employed on mice fed with a high-fat diet, and APAP (2, 4, 8mM) were cultured with L02 cells in the presence of alcohol and oleic acid. APAP treatment significantly aggravated hepatic lipid accumulation, increased the serum levels of triglyceride (TG), alanine aminotransferase (ALT) and aspartate aminotransferase (AST), and increased hepatic lipid accumulation in H&E and Oil red O staining results...
February 9, 2019: European Journal of Pharmacology
Tatsunobu Matsui, Hiroshi Ichikawa, Tomoka Fujita, Shigekazu Takemura, Tomohisa Takagi, Mayuko Osada-Oka, Yukiko Minamiyama
Intestinal wound healing depends on the precise balance of restitution, proliferation, and differentiation of intestinal epithelial cells (IECs). In a previous study, we revealed that IEC proliferation was suppressed under histidine deficiency. However, the role of histidine in cell restitution is poorly understood. Meanwhile, addition of arginine to basal medium enhanced IEC restitution after wounding. However, there are no reports on whether histidine or arginine deficiency influences IEC restitution. We examined the roles of histidine and arginine in IEC restitution using the rat intestinal epithelial cell-6 (IEC-6) cell line...
February 9, 2019: European Journal of Pharmacology
Sumayya Shahzad, Somaiya Mateen, Syed Shariq Naeem, Kafil Akhtar, Waseem Rizvi, Shagufta Moin
Identification of pharmacologically potent antioxidant compounds for their use in preventive medicine is thrust area of current research. This study was undertaken with the aim of determining the protective role of syringic acid (SA) on isoproterenol (ISO) induced myocardial infarction (MI) in rats. SA was orally given to rats for 21 days at three different concentrations (12.5, 25 and 50mg/kg). At 20th and 21st day, rats were subcutaneously injected with ISO and at the end of experimental period, rats were killed...
February 4, 2019: European Journal of Pharmacology
Vincenzo Lariccia, Maria Loredana Macrì, Alessandra Matteucci, Marta Maiolino, Salvatore Amoroso, Simona Magi
Ticagrelor is a direct acting and reversibly binding P2Y12 antagonist approved for the prevention of thromboembolic events. Clinical effects of ticagrelor cannot be simply accounted for by pure platelet inhibition, and off-target mechanisms can potentially play a role. In particular, recent evidence suggests that ticagrelor may also influence heart function and improve the evolution of myocardial ischemic injury by more direct effects on myocytes. The cardiac sodium/calcium exchanger 1 (NCX1) is a critical player in the generation and control of calcium (Ca2+ ) signals, which orchestrate multiple myocyte activities in health and disease...
February 2, 2019: European Journal of Pharmacology
Kamila Środa-Pomianek, Krystyna Michalak, Anna Palko-Łabuz, Andrzej Poła, Piotr Dzięgiel, Bartosz Puła, Piotr Świątek, Olga Wesołowska
The idea of the use of anticancer drugs together with a chemosensitizer emerged as the strategy of reversal of multidrug resistance (MDR) of cancer cells expressing ABC proteins many years ago. The approaches relying on the use of a single chemosensitizer have never resulted in a clinical success. Therefore, the application of drug combinations of two or more compounds with different mechanisms of action might be an alternative approach to increase the success rate. In the present study the cytotoxic and NF-κB inhibition potential of the phenothiazine derivative, MAE-TPR, was evaluated...
February 2, 2019: European Journal of Pharmacology
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