33,788 results match your criteria European journal of pharmacology[Journal]


Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.

Eur J Pharmacol 2019 Feb 16. Epub 2019 Feb 16.

Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117597, Singapore. Electronic address:

Destructive glucose and lipid metabolism in the liver is a crucial characteristic of type 2 diabetes mellitus (T2DM), eventually leading to insulin resistance and subsequent hyperglycemia and hyperlipidemia. Vaccarin is an active flavonoid glycoside associated with various biological functions, but its effects on glucose and lipid metabolic disorder in T2DM are still unclear. In this study, glucosamine (GlcN) and free fatty acids (FFAs, oleate/palmitate, 2:1 ratio) were applied to mimic insulin resistance and lipid deposition in HepG2 cells, respectively. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.029DOI Listing
February 2019

Triptolide prevents proliferation and migration of Esophageal Squamous Cell Cancer via MAPK/ERK signaling pathway.

Eur J Pharmacol 2019 Feb 16. Epub 2019 Feb 16.

Department of Pathology, Shanxi Medical University, Taiyuan, Shanxi 030001, P.R. China; Shanxi Key Laboratory of Carcinogenesis and Translational Research of Esophageal Cancer, Shanxi Medical University, Taiyuan, Shanxi 030001, P.R. China; Key Laboratory of Cellular Physiology, Ministry of Education, Shanxi Medical University, Taiyuan, Shanxi 030001, P.R. China. Electronic address:

Triptolide, the component of traditional Chinese herb, has been used as an inflammatory medicine and reported to be anti-tumor for various cancers recently. However, the effect of triptolide on Esophageal Squamous Cell Cancer (ESCC) has not yet been elucidated. In the study, we found that triptolide significantly inhibited cell proliferation, invasion, migration and survivability of ESCC cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.030DOI Listing
February 2019

Exogenous obestatin decreases beta-cell apoptosis and alfa-cell proliferation in high fat diet and streptozotocin induced type 2 diabetic rats.

Eur J Pharmacol 2019 Feb 15. Epub 2019 Feb 15.

Department of Endocrinology and Metabolism, Second Affiliated Hospital of Harbin Medical University, Harbin 150086, China. Electronic address:

Type 2 diabetes is a chronic metabolic disease characterized by progressive decrease of islet cell function. Delaying the process of islet failure remains a challenging goal in diabetes care. Previous studies have confirmed the role of obestatin, a gut peptide that belongs to ghrelin family, in the mediation of glucose metabolism. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.028DOI Listing
February 2019

MicroRNA-30c abrogation protects against spinal cord ischemia reperfusion injury through modulating SIRT1.

Eur J Pharmacol 2019 Feb 15. Epub 2019 Feb 15.

Spine area of orthopedics, Xi'an Hospital of Traditional Chinese Medicine, 710021, Shanxi, China. Electronic address:

Spinal cord ischemia/reperfusion (I/R) injury is a severe complication in many surgeries. Although microRNAs (miRNAs) are involved in I/R-caused spinal cord injury (SCI), the mechanism that underlies miR-30c interacted with SCI remains elusive. In this study, I/R surgery or oxygen-glucose deprivation (OGD) were performed to establish SCI model in vivo or in vitro, respectively. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.027DOI Listing
February 2019

Berberine promotes osteogenic differentiation of mesenchymal stem cells with therapeutic potential in periodontal regeneration.

Eur J Pharmacol 2019 Feb 15. Epub 2019 Feb 15.

Department of Periodontology, Nanjing Stomatological Hospital, Medical School of Nanjing University, 30 Zhongyang Road, Nanjing, Jiangsu 210008, China. Electronic address:

Periodontal disease is a bacterial infection-associated disease of the periodontal tissues characterized by the destruction of tooth-supporting structures, including alveolar bone. The ideal goal of periodontal therapy is the complete regeneration of alveolar bone in a healthy microenvironment free of infection. In this study, we found that berberine, a benzylisoquinoline plant alkaloid from Coptidis Rhizoma, strongly inhibited the growth of Porphyromonas gingivalis. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.026DOI Listing
February 2019
1 Read

20(S)-ginsenoside Rg3 sensitizes human non-small cell lung cancer cells to icotinib through inhibition of autophagy.

Eur J Pharmacol 2019 Feb 14. Epub 2019 Feb 14.

Department of Radiation Oncology, Hangzhou Cancer Hospital, Hangzhou, Zhejiang 310002, P. R. China. Electronic address:

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have become a standard therapy for non-small cell lung cancer (NSCLC) patients with sensitive mutations. However, acquired resistance inevitably emerges after a median of 6~12 months. It has been demonstrated that autophagy plays an important role in EGFR-TKI resistance. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.023DOI Listing
February 2019
1 Read

IPP-1 controls Akt/CREB phosphorylation extension in A adenosine receptor signaling cascade in MIN6 Pancreatic β-cell line.

Eur J Pharmacol 2019 Feb 14. Epub 2019 Feb 14.

Department of Clinical Biochemistry, School of Pharmacy & Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran. Electronic address:

Signaling through A adenosine receptor specifically prevent pancreatic β-cells (PBCs) loses under diabetogenic conditions. However, signaling mediators of this receptor in PBCs remained unidentified. Thus, we aimed to investigate the possible involvement of PKA/Akt/IPP-1/CREB pathway in MIN6 β-cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.017DOI Listing
February 2019

Obeticholic acid differentially regulates hepatic injury and inflammation at different stages of D-galactosamine/lipopolysaccharide-evoked acute liver failure.

Eur J Pharmacol 2019 Feb 14. Epub 2019 Feb 14.

Department of Toxicology, Anhui Medical University, Hefei, 230032, China. Electronic address:

The farnesoid X receptor (FXR) is a ligand-activated transcription factor that regulates genes involved in bile acid metabolism. Accumulating data demonstrate that FXR has an anti-inflammatory activity. The present study aimed to investigate the effect of obeticholic acid (OCA), a novel synthetic FXR agonist, on D-galactosamine (GalN)/lipopolysaccharide (LPS)-evoked acute liver injury. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.011DOI Listing
February 2019
1 Read

Pitolisant and intravenous cocaine self-administration in mice.

Eur J Pharmacol 2019 Feb 13. Epub 2019 Feb 13.

Département de Psychologie, Cognition et Comportement, Université de Liège, Place des Orateurs, 2/B-32, Liège, Belgium.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.019DOI Listing
February 2019

Complement C3a receptor antagonist attenuates tau hyperphosphorylation via glycogen synthase kinase 3β signaling pathways.

Eur J Pharmacol 2019 Feb 13. Epub 2019 Feb 13.

Department of Neurology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.020DOI Listing
February 2019

Pomolic acid reduces contractility and modulates excitation-contraction coupling in rat cardiomyocytes.

Eur J Pharmacol 2019 Feb 13. Epub 2019 Feb 13.

Laboratory of Cellular Physiology, Centre of Biophysics and Biochemistry, Venezuelan Institute for Scientific Research (IVIC), Caracas, Venezuela; Physiology and Biochemistry Research Group-PHYSIS, Department of Physiology and Biochemistry, Faculty of Medicine, University of Antioquia, Medellín, Colombia. Electronic address:

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 Ca transients reported with Fluo-3 and Fura-2, as well as L-type Ca currents (LTCC). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.016DOI Listing
February 2019
1 Read

Anticancer and antimetastatic potential of enterolactone: clinical, preclinical and mechanistic perspectives.

Eur J Pharmacol 2019 Feb 13. Epub 2019 Feb 13.

Pharmaceutical Sciences, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune, Maharashtra 411038, India.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.022DOI Listing
February 2019
1 Read

iTRAQ-based pharmacoproteomics reveals potential targets of berberine, a promising therapy for ulcerative colitis.

Eur J Pharmacol 2019 Feb 13. Epub 2019 Feb 13.

Hong Kong Baptist University Shenzhen Research Institute and Continuing Education, Shenzhen, China; Laboratory of Brain and Gut Research, Hong Kong Chinese Medicine Research Center, School of Chinese Medicine, Hong Kong, China. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.021DOI Listing
February 2019
2 Reads

Identification of microRNA-mRNA networks involved in cisplatin-induced renal tubular epithelial cells injury.

Eur J Pharmacol 2019 Feb 12. Epub 2019 Feb 12.

Department of Nephrology, Peking Union Medical College Hospital, Peking Union Medical College & Chinese Academy of Medical Science, Beijing, 100730, China. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.015DOI Listing
February 2019
1 Read

The effect of exenatide (a GLP-1 analog) and sitagliptin (a DPP-4 inhibitor) on plasma platelet-activating factor acetylhydrolase (PAF-AH) activity and concentration in normal and fructose-fed rats.

Eur J Pharmacol 2019 Feb 12. Epub 2019 Feb 12.

Department of Pathophysiology, Medical University of Lublin, ul. Jaczewskiego 8b, 20-090 Lublin, Poland. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.014DOI Listing
February 2019

α-adrenoceptor involves the relaxation effect of farrerol in rat aortic vascular smooth muscle cells.

Eur J Pharmacol 2019 Feb 12. Epub 2019 Feb 12.

Shanxi University of Chinese medicine, No. 121, Daxuejie, Jinzhong 030619, Shanxi Province, China; School of Pharmaceutical Science, Shanxi Medical University, No. 56, Xinjian South Road, Taiyuan 030001, Shanxi Province, China. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.012DOI Listing
February 2019

Role of serotonin and noradrenaline in the acute itch processing in mice.

Eur J Pharmacol 2019 Feb 11. Epub 2019 Feb 11.

Department of Psychiatry, Faculty of Medicine, University of Miyazaki, 5200 Kihara, Kiyotake, Miyazaki city, Miyazaki 889-1692, Japan. Electronic address:

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. By contrast, the single administration of noradrenaline reuptake inhibitor such as atomoxetine and nisoxetine or serotonin reuptake inhibitor such as fluvoxamine and escitalopram had little effect on chloroquine-induced scratching, whereas the induction of scratching behavior by chloroquine was significantly ameliorated by co-administration of serotonin reuptake inhibitors and noradrenaline reuptake inhibitors. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.013DOI Listing
February 2019

Hepatoprotective activity of metformin: A new mission for an old drug?

Eur J Pharmacol 2019 Feb 10;850:1-7. Epub 2019 Feb 10.

Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; Pharmaceutical Research Center, Institute of Pharmaceutical Technology, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.004DOI Listing
February 2019
1 Read

Pharmacological characterization of a highly selective Rho-kinase (ROCK) inhibitor and its therapeutic effects in experimental pulmonary hypertension.

Eur J Pharmacol 2019 Feb 9. Epub 2019 Feb 9.

Corporate Pre-clinical R&D, Chiesi Farmaceutici S.p.A., Italy. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.009DOI Listing
February 2019
1 Read

Dacomitinib, a new pan-EGFR inhibitor, is effective in attenuating pulmonary vascular remodeling and pulmonary hypertension.

Eur J Pharmacol 2019 Feb 9. Epub 2019 Feb 9.

Central Laboratory of Harbin Medical University (Daqing), Daqing 163319, P. R. China; Department of Biopharmaceutical Sciences, College of Pharmacy, Harbin Medical University, Harbin 150081, P. R. China. Electronic address:

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 . Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.008DOI Listing
February 2019
1 Read

Formoterol counteracts the inhibitory effect of cigarette smoke on glucocorticoid-induced leucine zipper (GILZ) transactivation in human bronchial smooth muscle cells.

Eur J Pharmacol 2019 Feb 10;850:8-14. Epub 2019 Feb 10.

Department of Pharmacology and Toxicology, Corporate Pre-Clinical R&D, Chiesi Farmaceutici S.p.A., Parma, Italy. Electronic address:

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). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.010DOI Listing
February 2019
1 Read

AS1949490, an inhibitor of 5'-lipid phosphatase SHIP2, promotes protein kinase C-dependent stabilization of brain-derived neurotrophic factor mRNA in cultured cortical neurons.

Eur J Pharmacol 2019 Feb 9. Epub 2019 Feb 9.

Department of Clinical Pharmacology, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.003DOI Listing
February 2019
1 Read

A chalcone derivative suppresses the induction of TSLP in mice and human keratinocytes and attenuates OVA-induced antibody production in mice.

Eur J Pharmacol 2019 Feb 9. Epub 2019 Feb 9.

Laboratory of Pharmacotherapy of Life-Style Related Diseases, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Miyagi, Japan. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.007DOI Listing
February 2019

Acetaminophen aggravates fat accumulation in NAFLD by inhibiting autophagy via the AMPK/mTOR pathway.

Eur J Pharmacol 2019 Feb 10;850:15-22. Epub 2019 Feb 10.

Institute for Liver Diseases of Anhui Medical University, School of Pharmacy, Anhui Medical University, Hefei 230032, China; Key Laboratory of anti-inflammatory and Immune Medicine, Ministry of Education, Hefei 230032, China. Electronic address:

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, 200 mg/kg) were employed on mice fed with a high-fat diet, and APAP (2, 4, 8 mM) were cultured with L02 cells in the presence of alcohol and oleic acid. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.005DOI Listing
February 2019
1 Read

Histidine and arginine modulate intestinal cell restitution via transforming growth factor-β.

Eur J Pharmacol 2019 Feb 10;850:35-42. Epub 2019 Feb 10.

Food Hygiene and Environmental Health, Division of Applied Life Science, Graduate School of Life and Environmental Sciences, Kyoto Prefectural University, Kyoto, Japan. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00142999193009
Publisher Site
http://dx.doi.org/10.1016/j.ejphar.2019.02.006DOI Listing
February 2019
1 Read

Syringic acid protects from isoproterenol induced cardiotoxicity in rats.

Eur J Pharmacol 2019 Feb 4;849:135-145. Epub 2019 Feb 4.

Department of Biochemistry, Jawaharlal Nehru Medical College, Faculty of Medicine, Aligarh Muslim University, Aligarh 202002, Uttar Pradesh, India. Electronic address:

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.056DOI Listing
February 2019
1 Read

Effects of ticagrelor on the sodium/calcium exchanger 1 (NCX1) in cardiac derived H9c2 cells.

Eur J Pharmacol 2019 Feb 2. Epub 2019 Feb 2.

Department of Biomedical Sciences and Public Health, School of Medicine, University "Politecnica delle Marche", Via Tronto 10/A, 60126, Ancona, Italy.

Ticagrelor is a direct acting and reversibly binding P2Y 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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.067DOI Listing
February 2019
1 Read

Cytotoxic and multidrug resistance reversal activity of phenothiazine derivative is strongly enhanced by theobromine, a phytochemical from cocoa.

Eur J Pharmacol 2019 Feb 2;849:124-134. Epub 2019 Feb 2.

Department of Biophysics, Wroclaw Medical University, ul. Chalubinskiego 10, 50-368 Wroclaw, Poland.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.061DOI Listing
February 2019

Inhibition of microRNA-155 attenuates sympathetic neural remodeling following myocardial infarction via reducing M1 macrophage polarization and inflammatory responses in mice.

Eur J Pharmacol 2019 Feb 2. Epub 2019 Feb 2.

Department of Cardiovascular Medicine, Xiangya Hospital, Central South University, Changsha, Hunan, P.R. China, 410008; National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan, P.R. China, 410008; Institute of Hypertension, Central South University, Changsha, Hunan, China. Electronic address:

Inflammation plays an important role in sympathetic neural remodeling induced by myocardial infarction (MI). MiR-155 is a vital regulator of inflammatory responses, and macrophage-secreted miR-155 promotes cardiac fibrosis and hypertrophy. However, whether miR-155 influences MI-induced sympathetic neural remodeling is not clear. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.001DOI Listing
February 2019
3 Reads
2.532 Impact Factor

p38 mitogen activated protein kinase mediates cardiac Na/H exchanger inhibition induced by Sildenafil.

Eur J Pharmacol 2019 Feb 2;849:96-105. Epub 2019 Feb 2.

Centro de Investigaciones Cardiovasculares "Dr. Horacio E. Cingolani", Facultad de Ciencias Médicas, Universidad Nacional de La Plata, Calle 60 y 120, 1900 La Plata, Argentina. Electronic address:

Since the original description as potent antianginal compounds, phosphodiesterase 5A inhibitors have continuously increased their possible therapeutic applications. In the heart, Sildenafil was shown to protect against an ischemic insult by decreasing cardiac Na/H exchanger (NHE1) activity, action that was mediated by protein kinase G. p38 mitogen activated protein kinase (p38MAPK) activation was described in cardiac ischemia, but its precise role remains elusive. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.070DOI Listing
February 2019
5 Reads

Role of hydrogen sulfide in cognitive deficits: Evidences and mechanisms.

Eur J Pharmacol 2019 Feb 2;849:146-153. Epub 2019 Feb 2.

Department of Cardiology, China-Japan Union Hospital of Jilin University, Changchun 130033, Jilin Province, China. Electronic address:

Hydrogen sulfide (HS) is a gaseous molecule and is endogenously produced in the brain by cystathionine beta-synthase, 3-mercaptopyruvate-sulfurtransferase, cysteine aminotransferase and cystathionine γ-lyase. Physiologically, HS acts as a neuromodulator and regulates synaptic activity of neurons and glia to promote the development of long-term potentiation. A decrease in HS levels in the brain and plasma has been directly correlated with the degree of severity of Alzheimer disease in patients. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.072DOI Listing
February 2019
3 Reads

The effect of alpha-lipoic acid on inflammatory mediators: a systematic review and meta-analysis on randomized clinical trials.

Eur J Pharmacol 2019 Feb 2;849:115-123. Epub 2019 Feb 2.

Department of Basic Medical Sciences, Neyshabur University of Medical Sciences, Neyshabur, Iran. Electronic address:

Alpha-Lipoic Acid (ALA) is a natural antioxidant compound which is naturally found in plant sources. New evidence revealed that ALA can reduce inflammation. Our objective in this meta-analysis was to conduct a systematic review and meta-analysis on randomized controlled trials to indicate ALA effects on serum inflammatory mediators concentration such as tumor necrosis factor-alpha (TNF-α), c-reactive protein (CRP), and interleukin-6 (IL-6). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.065DOI Listing
February 2019

Inhibitory effect of immunosuppressive drug tacrolimus on voltage-gated K current in rabbit coronary arterial smooth muscle cells.

Eur J Pharmacol 2019 Feb 2;849:59-66. Epub 2019 Feb 2.

Department of Physiology, Kangwon National University School of Medicine, Chuncheon 24341, South Korea. Electronic address:

In the present study, we investigated the inhibitory effect of tacrolimus, a macrolide immunosuppressive drug that acts through calcineurin inhibition, on voltage-gated K (Kv) channels expressed in native smooth muscle cells isolated from the coronary arteries of rabbits. Tacrolimus reduced the amplitude of Kv currents in a dose-dependent manner with an IC value and Hill coefficient of 7.80 ± 3. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.069DOI Listing
February 2019
1 Read
2.532 Impact Factor

Harmine mitigates LPS-induced acute kidney injury through inhibition of the TLR4-NF-κB/NLRP3 inflammasome signalling pathway in mice.

Eur J Pharmacol 2019 Feb 1;849:160-169. Epub 2019 Feb 1.

School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, PR China.

Acute kidney injury is a common clinical condition associated with increased morbidity and mortality. It is essential to find effective drugs with low side effects in the treatment of acute kidney injury. Harmine is one of the major active components of Peganum harmala L. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.062DOI Listing
February 2019
1 Read
2.532 Impact Factor

Intraocular pressure-lowering effects of imidazo[1,2-a]- and pyrimido[1,2-a]benzimidazole compounds in rats with dexamethasone-induced ocular hypertension.

Eur J Pharmacol 2019 Feb 1;850:75-87. Epub 2019 Feb 1.

International Medical University, IMU Clinical School, Seremban, Malaysia.

Ocular hypertension is believed to be involved in the etiology of primary open-angle glaucoma. Although many pharmaceutical agents have been shown to be effective for the reduction of intraocular pressure (IOP), a significant opportunity to improve glaucoma treatments remains. Thus, the aims of the present study were: (1) to evaluate the IOP-lowering effect of four compounds RU-551, RU-555, RU-839 (pyrimido[1,2-a]benzimidazole), and RU-615 (imidazo[1,2-a]benzimidazole) on steroid-induced ocular hypertension in rats after single drop and chronic applications; and (2) to test in silico and in vitro conventional rho-associated kinase (ROCK) inhibitory activity of the selected compound. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00142999193008
Publisher Site
http://dx.doi.org/10.1016/j.ejphar.2019.01.059DOI Listing
February 2019
6 Reads

Natural compound methyl protodioscin protects rat brain from ischemia/reperfusion injury through regulation of Mul1/SOD2 pathway.

Eur J Pharmacol 2019 Feb 1;849:50-58. Epub 2019 Feb 1.

Department of Laboratory Medicine, The Third Xiangya Hospital of Central South University, Changsha 410013, China. Electronic address:

Methyl protodioscin (MPD) is reported to relieve angina pectoris and myocardial ischemia, and mitochondrial E3 ubiquitin ligase 1 (Mul1) plays a key role in maintaining mitochondrial functions. Bioinformatic analysis shows potential interactions between MPD and Mul1. This study aims to explore whether MPD could protect rat brain against ischemia/reperfusion (I/R) injury through regulation of Mul1/ superoxide dismutase 2 (SOD2) pathway. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.057DOI Listing
February 2019
1 Read

TAS-203, an oral phosphodiesterase 4 inhibitor, exerts anti-inflammatory activities in a rat airway inflammation model.

Eur J Pharmacol 2019 Feb 1;849:22-29. Epub 2019 Feb 1.

Discovery and Preclinical Research Division, Taiho Pharmaceutical Co. Ltd., 3 Okubo, Tsukuba, Ibaraki 300-2611, Japan.

Cyclic adenosine monophosphate (cAMP) is a key intracellular second messenger, which is degraded by phosphodiesterase 4 (PDE4). PDE4 suppresses cAMP levels, and thus stimulates the activity of inflammatory cells. Therefore, PDE4 has been considered as a therapeutic target for airway inflammatory diseases including asthma and chronic obstructive pulmonary disease (COPD). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.068DOI Listing
February 2019
2 Reads

miR-34a inhibits progression of neuroblastoma by targeting autophagy-related gene 5.

Eur J Pharmacol 2019 Feb 1;850:53-63. Epub 2019 Feb 1.

Neonatal Intensive Care Unit, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450000, China. Electronic address:

Neuroblastoma (NB) is a common pediatric malignancy with high mortality in childhood. Although many attentions have been gained, novel biomarkers for NB diagnosis and prognosis are still needed. microRNAs (miRNAs) played important roles in NB progression and miR-34a is a tumor suppressor in NB. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00142999193003
Publisher Site
http://dx.doi.org/10.1016/j.ejphar.2019.01.071DOI Listing
February 2019
3 Reads
2.532 Impact Factor

MEPO promotes neurogenesis and angiogenesis but suppresses gliogenesis in mice with acute ischemic stroke.

Eur J Pharmacol 2019 Feb 2;849:1-10. Epub 2019 Feb 2.

Institute of Cerebrovascular Disease Research and Department of Neurology, Xuanwu Hospital of Capital Medical University, Beijing, China; Beijing Geriatric Medical Research Center and Beijing Key Laboratory of Translational Medicine for Cerebrovascular Diseases, Beijing, China; Beijing Institute for Brain Disorders, Beijing, China. Electronic address:

Previously study has proved the non-erythropoietic mutant erythropoietin (MEPO) exerted neuroprotective effects against ischemic cerebral injury, with an efficacy similar to that of wild-type EPO. This study investigates its effects on neurogenesis, angiogenesis, and gliogenesis in cerebral ischemic mice. Male C57BL/6 mice were subjected to middle cerebral artery occlusion (MCAO) and reperfusion. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00142999193003
Publisher Site
http://dx.doi.org/10.1016/j.ejphar.2019.01.066DOI Listing
February 2019
3 Reads

IRS-1 targets TAZ to inhibit adipogenesis of rat bone marrow mesenchymal stem cells through PI3K-Akt and MEK-ERK pathways.

Eur J Pharmacol 2019 Feb 1;849:11-21. Epub 2019 Feb 1.

Department of Endocrinology, The Third Hospital of Hebei Medical University, 139 Ziqiang Road, Shijiazhuang 050051, Hebei Province, PR China; Key Orthopaedic Biomechanics Laboratory of Hebei Province, 139 Ziqiang Road, Shijiazhuang 050051, Hebei Province, PR China. Electronic address:

Gene modification of mesenchymal stem cells (MSCs) offers a promising approach for clinical stem cell therapy. Transcriptional co-activator with PDZ-binding motif (TAZ) plays a vital role in MSCs' differentiation. We aim to explore the interaction of insulin receptor substrate-1 (IRS-1) with TAZ to regulate MSCs' adipogenesis in this study. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.064DOI Listing
February 2019
1 Read

Phellodendrine chloride suppresses proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis.

Eur J Pharmacol 2019 Feb 1;850:23-34. Epub 2019 Feb 1.

State Key Laboratory of Natural Medicines, China Pharmaceutical University, 210009 Nanjing, Jiangsu, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, China Pharmaceutical University, 210009 Nanjing, Jiangsu, China. Electronic address:

Despite the massive efforts to develop the treatment of pancreatic cancers, no effective application exhibits satisfactory clinical outcome. Macropinocytosis plays a critical role for continuous proliferation of pancreatic ductal adenocarcinoma (PDAC). In this study, we generated a screening method and identified phellodendrine chloride (PC) as a potential macropinocytosis inhibitor. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.060DOI Listing
February 2019
1 Read

Stimulation of pulmonary vagal C-fibers by trans-4-methyl-β-nitrostyrene induces bradycardiac and depressor reflex in rats: Role of vanilloid TRPV receptors.

Eur J Pharmacol 2019 Feb 1;849:154-159. Epub 2019 Feb 1.

Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, CE, Brazil. Electronic address:

Previously, we showed that the synthetic nitroderivative trans-4-methyl-β-nitrostyrene (T4MeN) induced vasorelaxant effects in rat isolated aortic rings. Here, we investigated the mechanisms underlying the cardiovascular effects of T4MeN in normotensive rats. In pentobarbital-anesthetized rats, intravenous (i. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.063DOI Listing
February 2019

Mechanisms underlying the vasorelaxant effect of trans-4-methoxy-β-nitrostyrene in the rat mesenteric resistance arteries.

Eur J Pharmacol 2019 Feb 1. Epub 2019 Feb 1.

Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, CE, Brazil. Electronic address:

Mechanisms underlying the vasorelaxant effects of the synthetic nitro compound, trans-4-methoxy-β-nitrostyrene (T4MN) were studied in isolated small resistance arteries from spontaneously hypertensive rats (SHRs). T4MN caused vasorelaxation in endothelium-intact third-order branches of the mesenteric artery pre-contracted with noradrenaline (NA). This effect was unchanged by indomethacin and atropine but was significantly reduced by endothelium removal, L-NAME, LY294002, glybenclamide, TEA, apamin, TRAM 34, or by the association of apamin and TRAM 34. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.058DOI Listing
February 2019

Alleviation of mechanical stress-induced allodynia by improving blood flow in chronic constriction injury mice.

Eur J Pharmacol 2019 Feb 2;849:67-74. Epub 2019 Feb 2.

Department of Pharmacology, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka City, Japan. Electronic address:

Reduced blood flow in the skin is observed in patients with neuropathic pain and in animal models. The aim of the present study was to elucidate the relationship between reduced skin blood flow and neuropathic pain in mice with a chronic constriction injury (CCI). Noradrenaline-induced contraction was enhanced in isolated plantar arteries ipsilateral to the CCI surgery compared to the contralateral arteries. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.02.002DOI Listing
February 2019

Attenuating oxygen-glucose deprivation-caused autophagosome accumulation may be involved in sevoflurane postconditioning-induced protection in human neuron-like cells.

Eur J Pharmacol 2019 Jan 30;849:84-95. Epub 2019 Jan 30.

Department of Anesthesiology, University of Virginia, Charlottesville, VA 22901, USA. Electronic address:

Application of the commonly used volatile anesthetic sevoflurane after brain ischemia (sevoflurane postconditioning) attenuates ischemic brain injury. It is not known whether autophagy plays a role in this sevoflurane postconditioning-induced neuroprotection. Human SH-SY5Y cells were induced to become neuron-like cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.051DOI Listing
January 2019

LncRNA OR3A4 participates in the angiogenesis of hepatocellular carcinoma through modulating AGGF1/akt/mTOR pathway.

Eur J Pharmacol 2019 Jan 30;849:106-114. Epub 2019 Jan 30.

Department of Interventional and Vascular, the Fourth Affiliated Hospital of Harbin Medical University, Harbin, Heilongjiang 150001, China. Electronic address:

Hepatocellular carcinoma (HCC), as the commonest type in liver cancer, is in urgent need for better treatment target due to its high mortality and poor prognosis. The involvement of angiogenesis in HCC has been identified by multiple studies, but the underlying mechanism remains unclear. Long non-coding RNAs (LncRNAs) have been reported to regulate numerous cancers, including HCC. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.049DOI Listing
January 2019
2 Reads
2.532 Impact Factor

Mechanisms underlying vascular hypocontractility induced by ethanol withdrawal: Role of cyclooxygenase 2-derived prostacyclin.

Eur J Pharmacol 2019 Jan 30;847:103-112. Epub 2019 Jan 30.

Escola de Enfermagem de Ribeirão Preto - DEPCH/Faculdade de Ciências Farmacêuticas de Ribeirão Preto - DFQ, USP, Ribeirão Preto, SP, Brazil. Electronic address:

The effects on the vasculature produced by ethanol withdrawal include both vasodilatation and hypocontractility, although a detailed biochemical understanding of these processes is yet to be accomplished. Here, we sought to investigate some of the mechanisms underlying vascular hypocontractility induced by ethanol withdrawal. Male Wistar rats were treated with increasing doses of 3-9% ethanol (v/v) for 21 days and the impact of ethanol withdrawal on the vascular function was assessed 48 h after immediate ethanol suspension. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.055DOI Listing
January 2019

TRIM66 confers tumorigenicity of hepatocellular carcinoma cells by regulating GSK-3β-dependent Wnt/β-catenin signaling.

Eur J Pharmacol 2019 Jan 30. Epub 2019 Jan 30.

Department of Infectious Diseases, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an 710061, China.

Tripartite motif 66 (TRIM66) protein, a member of the tripartite motif (TRIM) protein superfamily, has emerged as an oncogenic protein that is closely related to carcinogenesis in multiple cancers. However, whether TRIM66 plays a role in the progression of hepatocellular carcinoma (HCC) remains unknown. This study was aimed to investigate TRIM66 expression and its potential biological function in HCC cell lines. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.054DOI Listing
January 2019

Beneficial effects of rosiglitazone, a peroxisome proliferator-activated receptor-γ agonist, in a mouse allergic asthma model is not associated with the recruitment or generation of Foxp3-expressing CD4 regulatory T cells.

Eur J Pharmacol 2019 Jan 30;848:30-38. Epub 2019 Jan 30.

Department of Pathological Anatomy, Faculty of Veterinary Medicine, University of Warmia and Mazury, Oczapowskiego Street 13, 10-719 Olsztyn, Poland.

The activation of peroxisome proliferator-activated receptor γ (PPAR-γ) has been shown to attenuate allergic airway inflammation (AAI). To gain better understanding of mechanisms underlying this effect, the impact of rosiglitazone (RSG), a PPAR-γ agonist, on CD4 effector (Teff) and Foxp3-expressing regulatory (Treg) T cells in a mouse model of allergic asthma was studied. Furthermore, we investigated whether the activation of PPAR-γ may directly affect IL-4, IL-10 and IL-17 production by CD4 T cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2019.01.053DOI Listing
January 2019