33,897 results match your criteria European journal of pharmacology[Journal]


Proteomic analysis of flavokawain C-induced cell death in HCT 116 colon carcinoma cell line.

Eur J Pharmacol 2019 Apr 20. Epub 2019 Apr 20.

Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia; University of Malaya Centre for Proteomics Research (UMCPR), University of Malaya, 50603, Kuala Lumpur, Malaysia. Electronic address:

Flavokawain C (FKC), a naturally occurring chalcone, has previously been shown to inhibit the growth of colon carcinoma HCT 116 cells through induction of apoptosis and cell cycle arrest. However, the possible underlying mechanisms of cell death as a response to FKC treatment remains unclear. In this study, we performed proteomic analysis of HCT 116 cells treated with FKC to identify proteins that change in abundance. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193026
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http://dx.doi.org/10.1016/j.ejphar.2019.04.032DOI Listing
April 2019
1 Read

Alpha 2 adrenoceptor agonist guanabenz directly inhibits hyperpolarization-activated, cyclic nucleotide-modulated (HCN) channels in mesencephalic trigeminal nucleus neurons.

Eur J Pharmacol 2019 Apr 19. Epub 2019 Apr 19.

Department of Brain and Cognitive Sciences, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea; Department of Neurobiology & Physiology, School of Dentistry, Seoul National University, Seoul, Republic of Korea. Electronic address:

Alpha 2 (α-) adrenoceptor agonists, such as clonidine or dexmedetomidine, have been found to inhibit hyperpolarization-activated, cyclic nucleotide-modulated (HCN) channels, not only by reducing intracellular cyclic AMP levels but also by directly blocking HCN channels. In this study, we examined the inhibitory effect of guanabenz, a centrally acting α-adrenoceptor agonist with high specificity for α-subtype, on HCN channels in mesencephalic trigeminal nucleus (MTN) neurons which robustly express HCN channels and have been suggested to coexpress α-adrenoceptors. By performing whole-cell patch-clamp recording on MTN neurons in brainstem slices, hyperpolarization-activated inward current (I) was examined during guanabenz treatment. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.036DOI Listing
April 2019
7 Reads

Propofol improves colonic but impairs hepatic mitochondrial function in tissue homogenates from healthy rats.

Eur J Pharmacol 2019 Apr 19. Epub 2019 Apr 19.

Department of Anaesthesiology, University of Duesseldorf, Moorenstrasse 5, 40225, Duesseldorf, Germany. Electronic address:

Evidence suggests that propofol infusion syndrome (PRIS) is caused by an altered mitochondrial function. The aim of this study was to examine the effects of propofol and the vehicle MCT on mitochondrial function in hepatic and colonic tissue. Mitochondrial oxygen consumption was determined in colon and liver homogenates after incubation with buffer (control), propofol (50, 75, 100, 500 μM) or the carrier substances DMSO and MCT. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.031DOI Listing

Diabetic retinopathy: Focus on NADPH oxidase and its potential as therapeutic target.

Eur J Pharmacol 2019 Apr 19. Epub 2019 Apr 19.

Department of Ophthalmology, Xiangya Hospital, Central South University, Changsha, 410008, China. Electronic address:

Diabetic retinopathy is a common complication of diabetes that affects the retina due to a sustained high blood sugar level. Recent studies have demonstrated that high glucose-driven oxidative stress plays an important role in the microvascular complications of retina in diabetes. Oxidative stress occurs due to the excess of reactive oxygen species, which causes oxidative damage to retina, leading to the leak of tiny blood vessels, or acts as signaling molecules to trigger neovascularization, resulting in new fragile vessels. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.038DOI Listing

Dual actions of norathyriol as a new candidate hypouricaemic agent: uricosuric effects and xanthine oxidase inhibition.

Eur J Pharmacol 2019 Apr 19. Epub 2019 Apr 19.

Biomedical Engineering Research Center, Kunming Medical University, Kunming, 650500, China. Electronic address:

Hyperuricaemia, which results from the overproduction and underexcretion of uric acid, has been linked with chronic renal dysfunction, cardiovascular diseases, diabetes and metabolic syndrome. However, available clinical drugs cannot simultaneously target the production and excretion of uric acid. Norathyriol, a natural xanthone, was expected to have the dual actions. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.034DOI Listing
April 2019
1 Read

Dihydroartemisinin represses esophageal cancer glycolysis by down-regulating pyruvate kinase M2.

Eur J Pharmacol 2019 Apr 17. Epub 2019 Apr 17.

Department of Gastrointestinal Oncology, Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, 150081, PR China. Electronic address:

Esophageal cancer, especially esophageal squamous cell carcinoma (ESCC) threatens so many lives in China every year. Traditional treatment of ESCC has usually been disappointing. The development of novel therapy is worth investigation. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193024
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http://dx.doi.org/10.1016/j.ejphar.2019.04.018DOI Listing
April 2019
2 Reads

Isoliquiritigenin suppresses the proliferation and induced apoptosis via miR-32/LATS2/Wnt in nasopharyngeal carcinoma.

Eur J Pharmacol 2019 Apr 17. Epub 2019 Apr 17.

Department of Radiation Oncology, Jiangsu Cancer Hospital, Jiangsu Institute of Cancer Research, The Affiliated Cancer Hospital of Nanjing Medical University, Nanjing, 210009, China. Electronic address:

Nasopharyngeal Carcinoma is limited by the various severe side-effects and surgery is rarely performed. Iosliquiritigenin has a series of biological activities, such as antiviral, anti-free radical and antitumor. However, the role and underlying mechanism of isoliquiritigenin in nasopharyngeal carcinoma have not been understood yet. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.033DOI Listing

Tetramethylpyrazine attenuates blood-brain barrier disruption in ischemia/reperfusion injury through the JAK/STAT signaling pathway.

Eur J Pharmacol 2019 Apr 17. Epub 2019 Apr 17.

Department of Neurosurgery, Renmin Hospital of Wuhan University, Wuhan, Hubei, 430060, PR China. Electronic address:

Tetramethylpyrazine (TMP) has been studied in depth and is widely used in the treatment of many kinds of diseases in China. However, whether it has neuroprotec-tive effects on cerebral ischemia remains unclear. An ischemia/reperfusion (I/R) injury animal model was established via middle cerebral artery occlusion in this study. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.028DOI Listing

Tanshinone IIA protects hypoxia-induced injury by preventing microRNA-28 up-regulation in PC-12 cells.

Eur J Pharmacol 2019 Apr 16. Epub 2019 Apr 16.

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

Cerebral ischemia is the second leading cause of death and disability worldwide. Despite the neuroprotective role of Tanshinone IIA has been widely reported, the molecular mechanisms involving miRNAs remains unclear. We aimed to figure out a novel regulatory mechanism of Tanshinone IIA associated with miRNAs. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.030DOI Listing

Ginsenoside Rg1 attenuates hepatic insulin resistance induced by high-fat and high-sugar by inhibiting inflammation.

Eur J Pharmacol 2019 Apr 16. Epub 2019 Apr 16.

Department of Biochemistry and Molecular Biology, School of Basic Medicine, Kunming Medical University, Kunming, Yunnan, 650500, PR China; Yunnan Province Key Laboratory for Nutrition and Food Safety in Universities, PR China. Electronic address:

Ginsenoside Rg1 is the active ingredient of Chinese herbal medicine ginseng and sanqi, which has remarkable effects on anti-inflammation and anti-diabetes. In this study, we explored the molecular mechanism of ginsenoside Rg1 against diabetes in rat subjected to insulin resistance induced by high-fat and high-sugar (HFHS). Biochemical analysis revealed that ginsenoside Rg1 significantly decreased the serum levels of alanine transaminase, aspartate transaminase, alkaline phosphatase, total cholesterol, triglyceride, low-density lipoprotein and increased the serum levels of high-density lipoprotein, which indicated ginsenoside Rg1 improved the extent of hepatic steatosis. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.027DOI Listing
April 2019
2.532 Impact Factor

Geniposide protects against hypoxia/reperfusion-induced blood-brain barrier impairment by increasing tight junction protein expression and decreasing inflammation, oxidative stress, and apoptosis in an in vitro system.

Eur J Pharmacol 2019 Apr 14. Epub 2019 Apr 14.

School of Traditional Chinese Medicine Department, Beijing University of Chinese Medicine, Beijing, 100029, China. Electronic address:

The blood-brain barrier (BBB) is involved in the pathogeneses of ischemic stroke (IS). Geniposide (GEN), an iridoid glycoside isolated from Gardenia jasminoides Ellis, has been used for the treatment of IS. However, the effects of GEN on the BBB are poorly understood. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.021DOI Listing

Artesunate protects against surgery-induced knee arthrofibrosis by activating Beclin-1-mediated autophagy via inhibition of mTOR signaling.

Eur J Pharmacol 2019 Apr 14;854:149-158. Epub 2019 Apr 14.

Department of Orthopedics, Orthopedic Institute, Northern Jiangsu People's Hospital Affiliated to Yangzhou University, Yangzhou, Jiangsu 225001, China. Electronic address:

Intraarticular fibrosis following knee surgery is a troublesome complication and remains a challenging problem for clinicians. Artesunate (ART), a classical anti-malarial drug extracted from the Chinese medicinal herb Artemisia annua L, has been associated with some fibrosis-related diseases. However, its effect and underlying mechanism on knee arthrofibrosis are still obscure. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193024
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http://dx.doi.org/10.1016/j.ejphar.2019.04.017DOI Listing
April 2019
10 Reads

Carvedilol and thyroid hormones co-administration mitigates oxidative stress and improves cardiac function after acute myocardial infarction.

Eur J Pharmacol 2019 Apr 13;854:159-166. Epub 2019 Apr 13.

Laboratory of Cardiovascular Physiology and Reactive Oxygen Species, Physiology Department, Institute of Basic Health Science, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil. Electronic address:

After acute myocardial infarction (AMI), reactive oxygen species and oxidative stress have important roles in the progression to heart failure. As a therapeutic alternative, thyroid hormones (TH) revealed cardioprotective effects after AMI, including decreasing oxidative stress. Carvedilol beta-blocker, already used in the clinical treatment of AMI, also mitigate cardiac pathological remodelling. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.024DOI Listing
April 2019
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(-)-Myrtenol accelerates healing of acetic acid-induced gastric ulcers in rats and in human gastric adenocarcinoma cells.

Eur J Pharmacol 2019 Apr 13;854:139-148. Epub 2019 Apr 13.

Department of Physiology and Pharmacology, Faculty of Medicine, Federal University of Ceará, Fortaleza, Ceará, Brazil.

The gastroprotective property of (-)-myrtenol, a monoterpenoid, has been demonstrated previously against acute gastric ulceration induced by ethanol. However, the healing property of (-)-myrtenol in a chronic gastric ulcer model remains to be verified. This study evaluated its healing efficacy and the mechanism involved using the rat model of chronic gastric ulcer induced by serosal injection of 80% acetic acid in vivo, and human gastric adenocarcinoma cells (AGS) in vitro. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.025DOI Listing
April 2019
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Inhibition of salt appetite in sodium-depleted rats by carvacrol: Involvement of noradrenergic and serotonergic pathways.

Eur J Pharmacol 2019 Apr 13;854:119-127. Epub 2019 Apr 13.

Department of Physiology, Health Sciences Institute, Federal University of Bahia, 40110-100, Salvador, Bahia, Brazil.

Carvacrol, a monoterpene phenol present in the essential oil of oregano, possesses several biological properties, such as antioxidant, anti-inflammatory, anxiolytic, anticonvulsive and antinociceptive. In vitro studies have shown that carvacrol inhibits serotonin, noradrenaline and dopamine transporters and the enzymes monoamine oxidase-A and B. Different brain functions are controlled by monoamines, including cardiovascular control, thirst and sodium appetite. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.026DOI Listing

Long non-coding RNA FENDRR attenuates the stemness of non-small cell lung cancer cells via decreasing multidrug resistance gene 1 (MDR1) expression through competitively binding with RNA binding protein HuR.

Eur J Pharmacol 2019 Apr 11;853:345-352. Epub 2019 Apr 11.

Department of Radiology, The First Hospital of Jilin University, Changchun, Jilin, 130021, China. Electronic address:

The roles of long non-coding RNA (lncRNA) FENDRR in non-small cell lung cancer (NSCLC) cells progression have never been revealed. As cancer stem cells (CSCs) act important roles in tumor progression, here, we focused on FENDRR roles in NSCLC cell stemness. We found that lncRNA FENDRR expression was significantly decreased in lung cancer tissues and cells, especially in NSCLC cells. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.022DOI Listing
April 2019
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In vitro anti-glioblastoma activity of L-valine derived boroxazolidones.

Eur J Pharmacol 2019 Apr 11;854:194-200. Epub 2019 Apr 11.

Molecular Signaling Lab, Faculty of Medicine and Health Technology, Tampere University and BioMediTech, P.O. Box 553, 33101 Tampere, Finland. Electronic address:

In the present study, a series of L-valine derived boroxazolidones, previously synthesized and reported to have residual activity in a human epithelial cell line, have been evaluated in vitro for their anti-glioblastoma activity. A boroxazolidone derivative containing 2,4-difluorophenyl moieties (6) was found to have higher cytotoxicity than the standard drug, Temozolomide (TMZ). Compound 6 was found to exhibit dose-dependent growth inhibitory effects with an IC of 49 μM and 53 μM for LN229 and SNB19 cells, respectively. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.020DOI Listing

Inhibition of miR-140-3p or miR-155-5p by antagomir treatment sensitize chordoma cells to chemotherapy drug treatment by increasing PTEN expression.

Eur J Pharmacol 2019 Apr 10. Epub 2019 Apr 10.

Department of Orthopedics, China-Japan Union Hospital, Jilin University, Changchun, 130033, PR China.

Previous researches suggested microRNA-140-3p (miR-140-3p) and miR-155-5p as cancer promotor in chordoma. We aimed to investigate the mechanisms of these two miRNAs in chordoma cells. Patient-derived chordoma cell lines were established in vitro. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.034DOI Listing

Short chain fatty acid butyrate uptake reduces expressions of prostanoid EP receptors and their mediation of cyclooxygenase-2 induction in HCA-7 human colon cancer cells.

Eur J Pharmacol 2019 Apr 10;853:308-315. Epub 2019 Apr 10.

Department of Pharmacology for Life Sciences, Graduate School of Pharmaceutical Sciences & Graduate School of Biomedical Sciences, Tokushima University, Tokushima, 770-8505, Japan. Electronic address:

Microbiota produce short chain fatty acids (SCFAs), which are known to maintain gut homeostasis, by the fermentation of dietary fiber in the human colon. Among SCFAs, butyrate has been considered as the most physiologically effective SCFA in colorectal epithelial cells for growth and differentiation. Here we show that the E-type prostanoid 4 (EP) receptor expression level is regulated by different concentrations of butyrate, but not by other SCFAs, in human colon cancer HCA-7 cells, through sodium-coupled monocarboxylate transporter-1 (SMCT-1)-mediated uptake followed by the activation of histone acetyltransferase: cAMP response element binding protein-binding protein/p300. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.014DOI Listing
April 2019
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Antihypertensive and cardioprotective effects of new compound 1-(β-phenylethyl)-4-amino-1,2,4-triazolium bromide (Hypertril).

Eur J Pharmacol 2019 Apr 10;853:336-344. Epub 2019 Apr 10.

Department of Pharmacology, Bogomolets National Medical University, Tarasa Shevchenko Blvd, 13, Kyiv, 01601, Ukraine.

Despite the success which was achieved in the treatment of arterial hypertension, the problem remains actual. At the departments of pharmaceutical chemistry and pharmacology of the Zaporozhye State Medical Institute (Ukraine), our research team isolated the compound 1-(β-phenylethyl)-4-amino-1,2,4-triazolium bromide (Hypertril) as derivative of 4-amino-1,2,4-triazole. The objectives of this investigation were the study of cardioprotective and antihypertensive activities of this new compound Hypertril and we used the Spontaneously hypertensive rats (SHR) as an experimental model. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.013DOI Listing
April 2019
1 Read

Neuroprotection of cordycepin in NMDA-induced excitotoxicity by modulating adenosine A receptors.

Eur J Pharmacol 2019 Apr 10;853:325-335. Epub 2019 Apr 10.

School of Life Science, PR China. Electronic address:

Cerebral ischemia impairs physiological form of synaptic plasticity such as long-term potentiation (LTP). Clinical symptoms of cognitive dysfunction resulting from cerebral ischemia are associated with neuron loss and synaptic function impairment in hippocampus. It has been widely reported that cordycepin displays neuroprotective effect on ameliorating cognitive dysfunction induced by cerebral ischemia. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193024
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http://dx.doi.org/10.1016/j.ejphar.2019.04.015DOI Listing
April 2019
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Comparison of the antinociceptive profiles of morphine and oxycodone in two models of inflammatory and osteoarthritic pain in rat.

Eur J Pharmacol 2019 Apr 10;854:109-118. Epub 2019 Apr 10.

Área de Farmacología y Nutrición - Unidad Asociada I+D+i Al Instituto de Química Médica (CSIC), Grupo de Excelencia Investigadora URJC-Banco de Santander-Grupo Multidisciplinar de Investigación y Tratamiento Del Dolor (i+Dol), Dpto. Ciencias Básicas de La Salud, Facultad de Ciencias de La Salud, Universidad Rey Juan Carlos, Avda. Atenas, S/n. 28922 Alcorcón, Madrid, Spain. Electronic address:

Oxycodone and morphine are two opioid drugs commonly used for the treatment of moderate to severe pain. However, their use in the management of noncancer pain remains a controversial issue and, in this respect, the evidence on their effectiveness and safety, particularly in osteoarthritis, is being questioned. In order to analyse their analgesic profile, two different pain models in rats were used: the formalin-induced inflammatory pain and the monosodium iodoacetate (MIA)-induced knee osteoarthritic pain. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.011DOI Listing
April 2019
1 Read

C1q/TNF-related protein-9 attenuates retinal inflammation and protects blood-retinal barrier in db/db mice.

Eur J Pharmacol 2019 Apr 10;853:289-298. Epub 2019 Apr 10.

Department of Cardiology, Renmin Hospital of Wuhan University, Wuhan, 430060, PR China; Cardiovascular Research Institute, Wuhan University, Wuhan, 430060, PR China; Hubei Key Laboratory of Cardiology, Wuhan, 430060, PR China. Electronic address:

C1q/TNF-related protein-9(CTRP9) is an adipose cytokine, a closest adiponectin paralog, which has anti-inflammatory, antioxidant, vasodilation and anti-atherosclerosis effects. In addition, it can increase insulin sensitivity, decrease blood glucose level and inhibit the apoptosis of endothelial cells. However, it remains unclear whether CTRP9 has beneficial effects on diabetic retinopathy (DR). Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.012DOI Listing
April 2019
1 Read
2.532 Impact Factor

Immune-endocrine interactions related to a high risk of infections in chronic metabolic diseases: The role of PPAR gamma.

Eur J Pharmacol 2019 Apr 8. Epub 2019 Apr 8.

Laboratório de Inflamação, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz (FIOCRUZ), Avenida Brasil, 4365, Rio de Janeiro, RJ, Brazil. Electronic address:

Diverse disturbances in immune-endocrine circuitries are involved in the development and aggravation of several chronic metabolic diseases (CMDs), including obesity, diabetes, and metabolic syndrome. The chronic inflammatory syndrome observed in CMDs culminates in dysregulated immune responses with low microbial killing efficiency, by means low host innate immune response, and loss of ability to eliminate the pathogens, which results in a high prevalence of infectious diseases, including pneumonia, tuberculosis, and sepsis. Herein, we review evidence pointing out PPARγ as a putative player in immune-endocrine disturbances related to increased risk of infections in CMDs. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.008DOI Listing
April 2019
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A 3D bioprinted hydrogel mesh loaded with all-trans retinoic acid for treatment of glioblastoma.

Eur J Pharmacol 2019 Apr 8;854:201-212. Epub 2019 Apr 8.

Laboratory for Innovations in Microengineering (LiME), Department of Mechanical Engineering, University of Victoria, Victoria, BC V8P 5C2, Canada; Centre for Advanced Materials and Related Technologies (CAMTEC), University of Victoria, Victoria, BC, V8P 5C2, Canada; Centre for Biomedical Research (CBR), University of Victoria, Victoria, BC, V8P 5C2, Canada. Electronic address:

Treatment of glioblastoma (GBM), as the most lethal type of brain tumor, still remains a major challenge despite the various therapeutic approaches developed over the recent decades. GBM is considered as one of the most therapy-resistant human tumors. Treatment with temozolomide (TMZ) chemotherapy and radiotherapy in GBM patients has led to 30% of two-year survival rate (American Brain Tumor Association), representing a demanding field to develop more effective therapeutic strategies. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.007DOI Listing
April 2019
8 Reads
2.532 Impact Factor

Baicalein improves glucose metabolism in insulin resistant HepG2 cells.

Eur J Pharmacol 2019 Apr 7;854:187-193. Epub 2019 Apr 7.

Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, Beijing, 100005, China.

Insulin resistance (IR) is the primary pathogenesis of Type 2 diabetes mellitus (T2DM). Scutellaria baicalensis Georgi is a traditional Chinese herbal medicine, often used in the clinical treatment of T2DM. Baicalein which is considered to have anti-IR effects is one of its active ingredients. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193023
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http://dx.doi.org/10.1016/j.ejphar.2019.04.005DOI Listing
April 2019
6 Reads

Pharmacology of JNJ-28583113: A novel TRPM2 antagonist.

Eur J Pharmacol 2019 Apr 6;853:299-307. Epub 2019 Apr 6.

Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, CA, 92121, USA.

Transient receptor potential melastatin type 2 (TRPM2) is a cation channel activated by free intracellular ADP-ribose and reactive oxygen species. TRPM2 signaling has been linked to the pathophysiology of CNS disorders such as neuropathic pain, bipolar disorder and Alzheimer's disease. In this manuscript, we describe the discovery of JNJ-28583113, a potent brain penetrant TRPM2 antagonist. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.043DOI Listing
April 2019
2 Reads

trans-Chalcone modulates Leishmania amazonensis infection in vitro by Nrf2 overexpression affecting iron availability.

Eur J Pharmacol 2019 Apr 6;853:275-288. Epub 2019 Apr 6.

Department of Pathological Sciences, Center of Biological Sciences, State University of Londrina, Rod. Celso Garcia Cid PR445 Km 380, 86057-970, Londrina, Paraná, Brazil.

Leishmania parasites infect macrophages causing a wide spectrum of human diseases encompassing from cutaneous to visceral forms. The drugs currently used in leishmaniasis treatment are highly toxic and associated with acquired resistance. Seeking novel therapeutic targets, we conducted a comprehensive in vitro study to investigate the action of trans-chalcone (TC) against Leishmania amazonensis promastigote and amastigote forms. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193021
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http://dx.doi.org/10.1016/j.ejphar.2019.03.049DOI Listing
April 2019
2 Reads

The effect of medicinal plants on multiple drug resistance through autophagy: A review of in vitro studies.

Eur J Pharmacol 2019 Jun 6;852:244-253. Epub 2019 Apr 6.

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:

Multiple drug resistance (MDR) often occurs after prolonged chemotherapy, leading to refractory tumor and cancer recurrence. Autophagy as a primarily process during starvation or stress has a bipolar nature in cancer. It can cause MDR to become more difficult or make resistant cancer cells more susceptible to chemotherapeutic agents. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.001DOI Listing

The effects of probiotic and synbiotic supplementation on inflammatory markers among patients with diabetes: A systematic review and meta-analysis of randomized controlled trials.

Eur J Pharmacol 2019 Jun 6;852:254-264. Epub 2019 Apr 6.

Research Center for Biochemistry and Nutrition in Metabolic Diseases, Kashan University of Medical Sciences, Kashan, I.R, Iran. Electronic address:

This systematic review and meta-analysis of randomized controlled trials (RCTs) was performed to evaluate the effect of probiotic and symbiotic supplementation on inflammatory markers among patients with diabetes. Clinical trials were searched using Cochrane Library, EMBASE, PubMed, and Web of Science online databases for relevant trials published until April 2018. Two independent investigators evaluated study eligibility, extracted data, and assessed risk of bias of included clinical trials. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.003DOI Listing
June 2019
1 Read

Delta-opioid receptor antagonist naltrindole reduces oxycodone addiction and constipation in mice.

Eur J Pharmacol 2019 Jun 6;852:265-273. Epub 2019 Apr 6.

Department of Pharmacology, National Defense Medical Center, Taipei City, 11490, Taiwan, ROC; Center for Neuropsychiatric Research, National Health Research Institutes, Zhunan, Miaoli County, 35053, Taiwan, ROC. Electronic address:

Oxycodone, a widely prescribed and very potent oral opioid analgesic agent, is highly addictive and has many side effects, including troublesome constipation. Our studies in mice indicated that pretreatment of naltrindole did not significantly affect the analgesic efficacy of oxycodone but attenuated the tolerance and withdrawal induced by chronic oxycodone administration. Naltrindole also attenuated the oxycodone-induced rewarding and re-instatement behaviors, as shown by the conditioned place preference test. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.009DOI Listing
June 2019
1 Read

Comparison of the effects of synthetic and plant-derived mTOR regulators on healthy human ovarian cells.

Eur J Pharmacol 2019 Apr 5;854:70-78. Epub 2019 Apr 5.

King Saud University, Department of Zoology, College of Science, Riyadh, 11451, Saudi Arabia.

The aim of the present in vitro study was to compare the effects of synthetic and plant-derived mTOR regulators on healthy human ovarian cells. We compared the effect of two synthetic mammalian mTOR blockers MC2141 and MC2183 with that of natural/plant-derived mTOR blocker rapamycin and mTOR activator resveratrol on cultured human ovarian granulosa cells. We evaluated the accumulation of markers for the mTOR system (sirtuin 1; SIRT 1), proliferation (PCNA), and apoptosis (caspase 3) along with the expression of the transcription factor p53 by quantitative immunocytochemistry. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.048DOI Listing
April 2019
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Glabridin resensitizes p-glycoprotein-overexpressing multidrug-resistant cancer cells to conventional chemotherapeutic agents.

Eur J Pharmacol 2019 Jun 5;852:231-243. Epub 2019 Apr 5.

Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China. Electronic address:

Multidrug resistance (MDR) remains an obstacle to chemotherapy related with the overexpression of several efflux membrane proteins, and p-glycoprotein (P-gp) is the most studied among them. Thus, continuous investigational efforts are necessary to find valuable MDR reversal agents, and the flavonoid compound glabridin (GBD) seems to be a promising candidate. This study aimed to investigate the potential of GBD against MDR and explore the possible mechanisms. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.002DOI Listing
June 2019
3 Reads

Sinomenine facilitates the efficacy of gabapentin or ligustrazine hydrochloride in animal models of neuropathic pain.

Eur J Pharmacol 2019 Apr 4;854:101-108. Epub 2019 Apr 4.

Department of Physiology and Pharmacology, Karolinska Institutet, 17177, Stockholm, Sweden. Electronic address:

Management of chronic pain is restricted by the lack of effective tools. This study evaluated the efficacies of sinomenine combined gabapentin or ligustrazine hydrochloride in treating peripheral and central chronic neuropathic pain. The study was conducted in mice with photochemically induced sciatic nerve injury, and in rats with photochemically induced spinal cord injury. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.061DOI Listing

Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels.

Eur J Pharmacol 2019 Apr 5;854:92-100. Epub 2019 Apr 5.

Department of Physiology, College of Medicine, The Catholic University of Korea, Seoul, 06591, South Korea. Electronic address:

Cariprazine is a novel atypical antipsychotic drug that is widely used for the treatment of schizophrenia and bipolar mania/mixed disorder. We used the whole-cell patch-clamp technique to investigate the effects of cariprazine on hERG channels that are stably expressed in HEK cells. Cariprazine inhibited the hERG 1A and hERG 1A/3. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.006DOI Listing
April 2019
7 Reads

Molecular targets for tivantinib (ARQ 197) and vasculogenic mimicry in human melanoma cells.

Eur J Pharmacol 2019 Apr 4;853:316-324. Epub 2019 Apr 4.

Comparative Oncology, Radiobiology and Epigenetics Laboratory, College of Veterinary Medicine, University of Missouri, Columbia, MO, 65211, USA.

Tivantinib (TivB) was reported previously to target MET and microtubule assembly in different cells resulting in cytotoxicity. However, its other cellular targets remain unknown, especially the proteins involved in focal adhesion and cytoskeletal organization. We studied the effect of TivB on vinculin a focal adhesion protein, and RhoC, a GTPase which promote the reorganization of cytoskeleton. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.010DOI Listing
April 2019
1 Read

Knockdown of HOXB8 inhibits tumor growth and metastasis by the inactivation of Wnt/β-catenin signaling pathway in osteosarcoma.

Eur J Pharmacol 2019 Apr 5;854:22-27. Epub 2019 Apr 5.

Institute of Chronic Diseases Risk Assessment Henan University, Kaifeng, 475000, Henan Province, China. Electronic address:

Homeobox B8 (HOXB8) is a member of HOX family and was reported to be dysregulated in human cancers. However, its expression pattern and function in human osteosarcoma (OS) remain unknown. The aim of the current study is to examine its expression and biological roles in human OS cells. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.04.004DOI Listing

Geniposide alleviates hypoxia-induced injury by down-regulation of lncRNA THRIL in rat cardiomyocytes derived H9c2 cells.

Eur J Pharmacol 2019 Apr 3;854:28-38. Epub 2019 Apr 3.

Department of Cardiac Surgery, Jining No.1 People's Hospital, Jining, 272011, Shandong, China. Electronic address:

Geniposide (GEN) is an iridoid glycoside extracts from Gardenia jasminoides Ellis with antioxidant and anti-inflammarory properties. The objective of this study was to explore the effects of GEN on a cell model of myocardial infarction (MI). After transfection, hypoxia-stimulated H9c2 cells were treated with GEN. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.058DOI Listing
April 2019
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A synthetic peptide disturbing GluN2A/SHP1 interaction in dorsal root ganglion attenuated pathological pain.

Eur J Pharmacol 2019 Apr 2;854:62-69. Epub 2019 Apr 2.

Department of Molecular Pharmacology, School of Pharmacy, Lanzhou University, Lanzhou, Gansu, 730000, PR China. Electronic address:

Src Homology 2 domain-containing protein tyrosine phosphatase 1 (SHP1) interacts specifically with GluN2A subunit of N-methyl-D-aspartate (NMDA) subtype of glutamate receptors in spinal cord dorsal horn. This molecular interaction is involved in the development of GluN2A-dependent spinal sensitization of nociceptive behaviors. Intrathecal application of a GluN2A-derived polypeptide (short for pep-GluN2A) has been shown to disturb spinal GluN2A/SHP1 interaction and inhibit inflammatory pain. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193022
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http://dx.doi.org/10.1016/j.ejphar.2019.03.060DOI Listing
April 2019
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MicroRNA-301b promotes the proliferation and invasion of glioma cells through enhancing activation of Wnt/β-catenin signaling via targeting Glypican-5.

Eur J Pharmacol 2019 Apr 3;854:39-47. Epub 2019 Apr 3.

Department of Emergency Medicine, The Second Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi, 710004, PR China. Electronic address:

Accumulating evidence has suggested that Glypican-5 (GPC5) is a tumor suppressor gene in many types of cancers. However, whether GPC5 is involved in glioma remains unknown. This study was designed to explore the expression, biological function and regulatory mechanism of GPC5 in glioma. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.057DOI Listing

A CRTH2 antagonist, CT-133, suppresses NF-κB signalling to relieve lipopolysaccharide-induced acute lung injury.

Eur J Pharmacol 2019 Apr 3;854:79-91. Epub 2019 Apr 3.

Department of Critical Care Medicine and Orthopedics, The First Affiliated Hospital, Zhejiang University, School of Medicine, Hangzhou City, 310009, China. Electronic address:

Acute lung injury (ALI) and acute respiratory distress syndrome are life-threatening conditions that still have no definite pharmacotherapy. Hence, we investigate the potential effectiveness and underlying mechanism of CT-133, a newly developed selective antagonist of prostaglandin D2 receptor 2 (DP2) or of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2), against lipopolysaccharide (LPS)-induced ALI. CT-133 (10 or 30 mg/kg) or dexamethasone (1 mg/kg, positive control) were intragastrically administered 1 h before and 12 h after intratracheal LPS instillation, and primary neutrophils and macrophages and RAW264. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.053DOI Listing
April 2019
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Asymmetric dimethylarginine: An crucial regulator in tissue fibrosis.

Eur J Pharmacol 2019 Apr 3;854:54-61. Epub 2019 Apr 3.

Department of Pharmacology, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, 410078, China; Provincial Key Laboratory of Cardiovascular Research, Central South University, Changsha, 410078, China. Electronic address:

Fibrosis is a reparative process with very few therapeutic options to prevent its progression to organ dysfunction. Chronic fibrotic diseases contribute to an estimated 45% of all death in the industrialized world. Asymmetric dimethylarginine (ADMA), an endothelial nitric oxide synthase inhibitor, plays a crucial role in the pathogenesis of various cardiovascular diseases associated with endothelial dysfunction. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.055DOI Listing
April 2019
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Identification and biochemical analyses of selective CB agonists.

Eur J Pharmacol 2019 Apr 3;854:1-8. Epub 2019 Apr 3.

Department of Pharmaceutical Sciences, University of Connecticut, 69 N Eagleville Rd, Storrs, CT, 06269, USA. Electronic address:

Cannabinoid CB and CB receptors are activated by Δ-tetrahydrocannabinol, a psychoactive component of marijuana. The cannabinoid CB receptor is primarily located in the brain and is responsible for the psychoactive side effects, whereas the cannabinoid CB receptor is located in immune cells and is an attractive target for immune-related maladies. We identify small molecules that selectively bind to the cannabinoid CB receptor and can be further developed into therapeutics. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.054DOI Listing
April 2019
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Schisandrin B prevents ulcerative colitis and colitis-associated-cancer by activating focal adhesion kinase and influence on gut microbiota in an in vivo and in vitro model.

Eur J Pharmacol 2019 Apr 3;854:9-21. Epub 2019 Apr 3.

Center for New Drug Safety Evaluation and Research, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 211198, China. Electronic address:

Colitis-associated cancer (CAC) has a close relationship with ulcerative colitis (UC). Therapeutic effect of Schisandrin B (SchB) on UC and CAC remains largely unknown. We investigated the preventative effect of SchB on the dextran sulphate sodium (DSS) model of UC and azoxymethane (AOM)/DSS model of CAC. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193022
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http://dx.doi.org/10.1016/j.ejphar.2019.03.059DOI Listing
April 2019
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Nobiletin suppresses oxidative stress and apoptosis in H9c2 cardiomyocytes following hypoxia/reoxygenation injury.

Eur J Pharmacol 2019 Apr 3;854:48-53. Epub 2019 Apr 3.

Department of Cardiology, Huaihe Hospital of Henan University, Kaifeng, 475000, Henan Province, China.

Nobiletin (3',4',5,6,7,8-hexamethoxyflavone), a dietary polymethoxylated flavonoid found in Citrus fruits, was reported to exhibit protective activity against ischemia/reperfusion (I/R). However, the role of nobiletin in myocardial I/R injury remains unclear. This study was designed to examine the cardioprotective effect of nobiletin from myocardial hypoxia/reoxygenation (H/R) injury in vitro, and to explore the potential molecular mechanisms. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.056DOI Listing
April 2019
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Methotrexate disposition, anti-folate activity and efficacy in the collagen-induced arthritis mouse model.

Eur J Pharmacol 2019 Apr 2;853:264-274. Epub 2019 Apr 2.

Department of Pharmacy Practice, University of Kansas Medical Center, Kansas City, KS, USA. Electronic address:

Methotrexate (MTX) efficacy in autoimmune arthritis is variable and unpredictable resulting in the need for the identification of biomarkers to guide drug therapy. This study utilizes the collagen-induced arthritis mouse model to investigate erythrocyte MTX disposition and anti-folate activity as biochemical markers of efficacy in autoimmune arthritis. Following induction of arthritis, DBA/1J mice were treated with once-weekly subcutaneous MTX at varying doses over a period of 40 days. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.052DOI Listing
April 2019
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SENP2 suppresses NF-κB activation and sensitizes breast cancer cells to doxorubicin.

Eur J Pharmacol 2019 Mar 30;854:179-186. Epub 2019 Mar 30.

Molecular Biology Laboratory, The First Affiliated Hospital of Henan University of Science and Technology, China. Electronic address:

Doxorubicin is a chemotherapeutic agent commonly used to treat breast cancer. However, breast cancer often develops drug resistance, leading to disease recurrence and poor prognosis. Delineating the mechanisms underlying drug resistance is imperative for overcoming the challenge of treating doxorubicin-resistant breast cancer. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00142999193021
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http://dx.doi.org/10.1016/j.ejphar.2019.03.051DOI Listing
March 2019
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Dioscin inhibits intimal hyperplasia in rat carotid artery balloon injury model through inhibition of the MAPK-FoxM1 pathway.

Eur J Pharmacol 2019 Mar 30;854:213-223. Epub 2019 Mar 30.

Department of Pharmacology, Tianjin Key Laboratory of Inflammation Biology, School of Basic Medical Sciences, Tianjin Medical University, Tianjin, 300070, People's Republic of China. Electronic address:

Vascular smooth muscle cell (VSMC) proliferation and migration are crucial events in the pathological course of atherosclerosis and restenosis after percutaneous coronary intervention (PCI). Dioscin has been shown to exhibit powerful cardiovascular protective effects and potent therapeutic potential in cancer owing to the inhibition of cell proliferation and migration. However, its effects on arterial wall hypertrophy-related diseases caused by VSMC proliferation and migration remain unclear. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.050DOI Listing
March 2019
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Niclosamide ethanolamine induces trachea relaxation and inhibits proliferation and migration of trachea smooth muscle cells.

Eur J Pharmacol 2019 Mar 29;853:229-235. Epub 2019 Mar 29.

Department of Pharmacology (the State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Research, Ministry of Education), College of Pharmacy, Harbin Medical University; Translational Medicine Research and Cooperation Center of Northern China, Heilongjiang Academy of Medical Sciences, Harbin Medical University, PR China. Electronic address:

Our previous study found that the anthelmintic drug niclosamide relaxed the constricted arteries and inhibited proliferation and migration of vascular smooth muscle cells. Here, we investigated the effect of niclosamide ethanolamine (NEN) on trachea function and the proliferation and migration of trachea smooth muscle cells. Isometric tension of trachea was recorded by multi-channel myograph system. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.047DOI Listing
March 2019
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Dehydroepiandrosterone sulfate improves visceral sensation and gut barrier in a rat model of irritable bowel syndrome.

Eur J Pharmacol 2019 Jun 29;852:198-206. Epub 2019 Mar 29.

Division of Gastroenterology and Hematology/Oncology, Department of Medicine, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido, 078-8510, Japan; Department of General Medicine, Asahikawa Medical University, Midorigaoka Higashi 2-1-1-1, Asahikawa, 078-8510, Japan. Electronic address:

Stress-induced altered visceral sensation and impaired gut barrier play an important role in the pathophysiology of irritable bowel syndrome (IBS). These responses were demonstrated to be peripheral corticotropin-releasing factor (CRF) dependent and also mediated via proinflammatory cytokine in animal IBS model. Dehydroepiandrosterone sulfate (DHEA-S) is known to have anti-inflammatory properties by suppressing proinflammatory cytokine release. Read More

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http://dx.doi.org/10.1016/j.ejphar.2019.03.037DOI Listing