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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/28223126/targeted-inhibition-of-hdac8-increases-the-doxorubicin-sensitivity-of-neuroblastoma-cells-via-up-regulation-of-mir-137
#1
Gang Zhao, Guoliang Wang, Hongmin Bai, Tiandong Li, Fanghe Gong, Huan Yang, Jinchong Wen, Weimin Wang
Histone deacetylases (HDACs) have been suggested to be potential therapeutic targets for cancer treatment. Recent studies revealed that HDAC8 expression was associated with poor prognostic markers and poor overall survival rate of neuroblastoma (NB). Our present study revealed that among the four members of class I HDACs, HDAC8 is significantly over expressed in NB cells as compared with the normal fibroblast 3T3 cells or primary normal human astrocytes (NHA) cells. Targeted inhibition of HDAC8 by its specific siRNA (si-HDAC8) can inhibit the in vitro growth of NB cells...
February 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219711/oxidative-stress-inactivates-ecto-5-nucleotidase-by-inhibiting-protein-kinase-c-in-rat-hearts-in-vivo
#2
Toshio Obata, Michiko Nakashima
Examined in the present study, allopurinol are xanthine oxidase inhibitors for use in rat hearts in vivo dialysis technology and ventricular myocardial intersitial adenosine production can increase. The microdialysis probe was implanted in the left ventricular myocardium of anesthetized rat hearts and the tissue in the vicinity of the dialysis was perfused with Tyrode's solution containing adenosine 5'-monophosphate (AMP) through the dialysis probe at a rate of 1.0ml/min to assess the activity of ecto-5'-nucleotidase...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219710/unique-effect-of-4-hydroxyestradiol-and-its-methylation-metabolites-on-lipid-and-cholesterol-profiles-in-ovariectomized-female-rats
#3
Pan Wang, Bao-Ting Zhu
Animal studies have shown that endogenous estrogens such as 17β-estradiol (E2) can modulate lipid profiles in vivo, and this effect is generally thought to be mediated by the estrogen receptors (ERs). The present study sought to test a hypothesis that some of the endogenous estrogen metabolites that have very weak estrogenic activity may exert some of their modulating effects on lipid metabolism in an ER-independent manner. Using ovariectomized female rats as an in vivo model, we found that 4-hydroxyestradiol (4-OH-E2) has a markedly stronger effect in reducing the adipocyte size and serum cholesterol level in rats compared to E2, despite the weaker estrogenic activity of 4-OH-E2...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219709/cordycepin-diminishes-thymic-stromal-lymphopoietin-induced-interleukin-13-production
#4
Myoung-Schook Yoou, Kyoung Wan Yoon, Youngjin Choi, Hyung-Min Kim, Hyun-Ja Jeong
Atopic dermatitis (AD) is known to aggravate by thymic stromal lymphopoietin (TSLP) and TSLP is also known to up-regulate mast cell proliferation via production of interleukin (IL)-13. Thus, we investigated whether cordycepin could regulate mast cell proliferation induced by TSLP in human mast cell line, HMC-1 cell. Cordycepin significantly diminished the production and mRNA of IL-13 through the down-regulation of phosphorylated-signal transducer and activation of transcription 6 in the TSLP-stimulated HMC-1 cells...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219708/novel-technique-to-determine-the-pka-of-clonidine-at-prejunctional-%C3%AE-2-adrenoceptors-in-cardiac-and-vascular-sympathetic-transmission
#5
James A Angus, Pravin Rajasekaran, Christine E Wright
Analytical pharmacology draws heavily on the concept of equilibrium of agonist and silent antagonist concentrations competing at a specific receptor site. This condition breaks down in nerve transmission when transmitter release is inhibited by prejunctional α2-adrenoceptors activated by an agonist such as clonidine. We have developed a method that allows the agonist dissociation constant KA of clonidine to be determined in a robust isolated right atrial assay of mouse, rat and guinea pig. By applying low numbers of field pulses 1-4 to prevent autoinhibitory feedback, clonidine shifted the nerve pulse stimulation-tachycardia curves to the right...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28219707/22-azidosalvinorin-a-exhibits-antidepressant-like-effect-in-mice
#6
James Oluwagbamigbe Fajemiroye, Polepally Reddy Prabhakar, Carlos Luiz da Cunha, Elson Alves Costa, Jordan K Zjawiony
The increasing cases of depression has made the searches for new drugs and understanding of the underligning neurobiology of this psychiatric disorder a necessity. Here, we modified the structure of salvinorin A (a known halucinogen) and investigated antidepressant-like activity of its four derivatives; 22-methylsulfanylsalvinorin A(SA1), 2-O-cinnamoylsalvinorin B (CSB), 22-azidosalvinorin A (SA2), and 2-O-(4(')-azidophenylsulfonyl)salvinorin B (SA3). Prior to behavioural tests (Irwin test, open field test - OFT, forced swimming test - FST and tail suspension test - TST), SA1 was prepared by reacting salvinorin B and methylthioacetic acid with 89% yield; CSB was obtained from the reaction of salvinorin B and cinnamic acid with 92% yield; SA2 was obtained from the reaction of salvinorin B and azidoacetic acid with 81% yield; and SA3 was prepared by reacting salvinorin B with 4-azidophenylsulfonyl chloride with 80% yield...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216053/hypoglycemic-drugs-induce-antioxidant-aldehyde-dehydrogenase-activity-and-remain-high-in-patients-with-glycemic-control-in-type-2-diabetes
#7
Alejandra Picazo, Angélica S Jiménez-Osorio, Porfirio Zúñiga-Mejía, José Pedraza-Chaverri, Adriana Monroy, M Eunice Rodríguez-Arellano, Diana Barrera-Oviedo
The antioxidant system results essential to control and prevent lipid peroxidation due to stress damage in type 2 diabetes. An example is aldehyde dehydrogenase (ALDH), an enzyme that is involved in the detoxification of aldehydes formed during lipid peroxidation. This study was conducted to evaluate ALDH activity and to determine their association with hypoglycemic treatment in type 2 diabetes patients. The study population consisted of 422 Mexican subjects: a control group and type 2 diabetes patients. Type 2 diabetes patients were re-classified as those with or without hypoglycemic treatment and those with or without glycemic control (according to glycated hemoglobin (HbA1c))...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216052/interaction-among-herg-channel-blockers-is-a-potential-mechanism-of-death-in-caffeine-overdose
#8
Jifeng Zheng, Wei Zhao, Kai Xu, Qingmao Chen, Yingying Chen, Yueliang Shen, Liping Xiao, Liqin Jiang, Yuan Chen
Caffeine overdose death is due to cardiac arrest, but its mechanism has not been explored in detail. In this study, our data showed that caffeine significantly prolonged the heart rate-corrected QT interval (QTc) of rabbits in vivo (P < 0.05; n = 7). Caffeine was also found to be a hERG channel blocker with an IC50 of 5.04mM (n=5). Although these two findings likely link caffeine overdose death with hERG channel blockade, the amount of caffeine consumption needed to reach the IC50 is very high. Further study demonstrated that addition another hERG blocker could lower the consumption of caffeine significantly, no matter whether two hERG blockers share the same binding sites...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216051/morin-activates-the-nrf2-are-pathway-and-reduces-oxidative-stress-induced-dna-damage-in-pancreatic-beta-cells
#9
Pachamuthu Vanitha, S Senthil Kumar, Sireesh Dornadula, S Anantha Kumar, Palanisamy Rajaguru, Kunka Mohanram Ramkumar
Oxidative stress is an important factor contributing to the pathogenesis of diabetes and its complications. In our earlier study, we demonstrated the antidiabetic efficacy of morin by regulating key enzymes of carbohydrate metabolism in diabetic rats. The present study was designed to assess the antigenotoxic potential of morin in pancreatic β-cells, using the COMET assay. To explore its potential mechanisms of action, three genotoxic agents, H2O2 which induces DNA damage by the generation of reactive oxygen species, streptozotocin (STZ) by RNS and Methyl methanesulfonate (MMS) by DNA alkylation was used...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216050/vancomycin-induces-reactive-oxygen-species-dependent-apoptosis-via-mitochondrial-cardiolipin-peroxidation-in-renal-tubular-epithelial-cells
#10
Yuya Sakamoto, Takahisa Yano, Yuki Hanada, Aki Takeshita, Fumika Inagaki, Satohiro Masuda, Naoya Matsunaga, Satoru Koyanagi, Shigehiro Ohdo
Vancomycin (VCM) is a first-line antibiotic for serious infections caused by methicillin-resistant Staphylococcus aureus. However, nephrotoxicity is one of the most complaint in VCM therapy. We previously reported that VCM induced apoptosis in a porcine proximal tubular epithelial cell line (LLC-PK1), in which mitochondrial complex I may generate superoxide, leading to cell death. In the present study, VCM caused production of mitochondrial reactive oxygen species and peroxidation of the mitochondrial phospholipid cardiolipin that was reversed by administration of the mitochondrial uncoupler carbonyl cyanide-4-(trifluoromethoxy) phenylhydrazone (FCCP)...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216049/chronic-treatment-with-fluoxetine-modulates-vascular-adrenergic-responses-by-inhibition-of-pre-and-post-synaptic-mechanisms
#11
Camila A Pereira, Fernanda L Rodrigues, Silvia G Ruginsk, Camila Z Zanotto, José A Rodrigues, Diego A Duarte, Claudio M Costa-Neto, Leonardo B Resstel, Fernando S Carneiro, Rita C Tostes
Fluoxetine, a serotonin reuptake inhibitor (SSRI), has other effects in addition to blocking serotonin reuptake, including changes in the vasomotor tone. Whereas many studies focused on the acute effects of fluoxetine in the vasculature, its chronic effects are still limited. In the present study, we tested the hypothesis that chronic fluoxetine treatment modulates adrenergic vascular responses by interfering with post- and pre-synaptic mechanisms. Wistar rats were treated with vehicle (water) or chronic fluoxetine (10mg/kg/day) for 21 days...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216048/chloroquine-blocks-the-kir4-1-channels-by-an-open-pore-blocking-mechanism
#12
Leticia G Marmolejo-Murillo, Iván A Aréchiga-Figueroa, Eloy G Moreno-Galindo, Ricardo A Navarro-Polanco, Aldo A Rodríguez-Menchaca, Meng Cui, José A Sánchez-Chapula, Tania Ferrer
Kir4.1 channels have been implicated in various physiological processes, mainly in the K(+) homeostasis of the central nervous system and in the control of glial function and neuronal excitability. Even though, pharmacological research of these channels is very limited. Chloroquine (CQ) is an amino quinolone derivative known to inhibit Kir2.1 and Kir6.2 channels with different action mechanism and binding site. Here, we employed patch-clamp methods, mutagenesis analysis, and molecular modeling to characterize the molecular pharmacology of Kir4...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28216047/serotonin-2a-homodimers-are-needed-for-signalling-via-both-phospholipase-a2-and-phospholipase-c-in-transfected-cho-cells
#13
Alba Iglesias, Marta Cimadevila, María Isabel Cadavid, María Isabel Loza, José Brea
Different ligands differentially activate phospholipase A2 (PLA2) and phospholipase C (PLC) signalling pathways that are coupled to the serotonin 2A (5-HT2A) receptor, a class-A G-protein coupled receptor (GPCR). The serotonin 5-HT2A receptor has been shown to be expressed as a homodimer displaying some ligands negative cooperativity between protomers in the PLA2 signalling pathway. We hypothesized that the homodimeric complex is the minimum functional unit required for activation of the PLA2 and PLC pathways by the serotonin 5-HT2A receptor...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28213289/quercetin-and-pioglitazone-synergistically-reverse-endothelial-dysfunction-in-isolated-aorta-from-fructose-streptozotocin-f-stz-induced-diabetic-rats
#14
Thubasni Kunasegaran, Mohd Rais Mustafa, Francis I Achike, Dharmani Devi Murugan
Pioglitazone is an anti-diabetic drug with potential to cause adverse effects following prolonged use. This study, therefore, investigated the effects of combination treatment of a subliminal concentration of pioglitazone and quercetin, a potent antioxidant, on vascular reactivity of aorta isolated from fructose-streptozotocin (F-STZ)-induced diabetic rats. Relaxation to acetylcholine and sodium nitroprusside, and contraction to phenylephrine were tested in organ bath chambers following pre-incubation with vehicle (DMSO; 0...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28213290/zd0947-a-sulphonylurea-receptor-modulator-detects-functional-sulphonylurea-receptor-subunits-in-murine-vascular-smooth-muscle-atp-sensitive-k-channels
#15
Tadashi Yamamoto, Kohei Takahara, Keiichiro Uchida, Noriyoshi Teramoto
In order to identify functional sulphonylurea receptor (SUR.x) subunits of native ATP-sensitive K(+) channels (KATP channels) in mouse portal vein, the effects of ZD0947, a SUR.x modulator, were investigated on spontaneous portal vein contractions, macroscopic membrane currents and unitary currents recorded (using patch-clamp techniques) in freshly dispersed mouse portal vein myocytes. Spontaneous contractions in mouse portal vein were reversibly reduced by ZD0947 in a concentration-dependent manner (Ki = 293nM)...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28213288/inhibition-of-estrogen-related-receptor-%C3%AE-attenuates-vascular-smooth-muscle-cell-proliferation-and-migration-by-regulating-rhoa-p27-kip1-and-%C3%AE-catenin-wnt4-signaling-pathway
#16
Qunyi Li, Lei Zhu, Liudi Zhang, Haifei Chen, Yingfeng Zhu, Yongli Du, Wanxian Zhong, Mingkang Zhong, Xiaojin Shi
RhoA/p27(Kip1) and β-Catenin/Wnt4 signaling processes play central roles in proliferation and migration in vascular smooth muscle cells (VSMCs). ERRα, a member of orphan nuclear receptors, is a potent prognostic factor in breast, ovarian, colon and other types of tumors. However, biological significance of ERRα in VSMCs as well as the molecular mechanisms remains largely unknown. Therefore, the present study was designed to investigate whether ERRα is involved in the proliferation and migration of VSMCs in vitro and neointimal formation in vivo...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28213287/butein-induction-of-ho-1-by-p38-mapk-nrf2-pathway-in-adipocytes-attenuates-high-fat-diet-induced-adipose-hypertrophy-in-mice
#17
Zheng Wang, Sun-O Ka, Youngyi Lee, Byung-Hyun Park, Eun Ju Bae
Adipose tissue inflammation and oxidative stress are key components in the development of obesity and insulin resistance. Heme oxygenase (HO)-1 in adipocytes protects against obesity and adipose dysfunction. In this study, we report the identification of butein, a flavonoid chalcone, as a novel inducer of HO-1 expression in adipocytes in vitro and in vivo. Butein upregulated HO-1 mRNA and protein expression in 3T3-L1 adipocytes, accompanied by Kelch-Like ECH-Associated Protein (Keap) 1 degradation and increase in the nuclear level of nuclear factor erythroid 2-related factor 2 (Nrf2)...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28202393/role-of-a1-and-a2a-adenosine-receptor-agonists-in-adipose-tissue-inflammation-induced-by-obesity-in-mice
#18
Caroline Candida DeOliveira, Cintia Rabelo E Paiva Caria, Erica Martins Ferreira Gotardo, Marcelo Lima Ribeiro, Alessandra Gambero
Adenosine receptors are expressed in adipose tissue and control physiological and pathological events such as lipolysis and inflammation. The aim of this study was to evaluate the activity of N(6)-cyclopentyladenosine (CPA), a potent and selective A1 adenosine receptor agonist; 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxyamidoadenosine hydrochloride (CGS-21680), an A2A adenosine receptor agonist; and 5'-N-ethylcarboxamidoadenosine (NECA), a potent non-selective adenosine receptor agonist on adipose tissue inflammatory alterations induced by obesity in mice...
February 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28192100/disease-modifying-anti-rheumatic-activity-of-the-alkaloid-montanine-on-experimental-arthritis-and-fibroblast-like-synoviocytes
#19
Mirian Farinon, Vanessa S Clarimundo, Graziele P R Pedrazza, Pércio S Gulko, José A S Zuanazzi, Ricardo M Xavier, Patricia G de Oliveira
Montanine is an alkaloid isolated from Rhodophiala bifida bulb with potential anti-arthritic activity. In this context, we evaluated whether montanine has a disease modifying anti-rheumatic activity in two arthritis models and its effect in vitro on lymphocyte proliferation and on invasiveness of fibroblast-like synoviocytes (FLS). Antigen-induced arthritis (AIA) was performed in Balb/C mice with methylated bovine serum albumin, and nociception and leukocytes migration into the knee joint were evaluated. Collagen-induced arthritis (CIA) was performed in DBA/1J mice, and arthritis development and severity were assessed by clinical and histological scoring and articular nociception...
February 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28192099/role-of-interleukin-10-in-the-neuroprotective-effect-of-the-angiotensin-type-2-receptor-agonist-compound-21-after-ischemia-reperfusion-injury
#20
Abdelrahman Y Fouda, Bindu Pillai, Krishnan M Dhandapani, Adviye Ergul, Susan C Fagan
INTRODUCTION: We and others have shown that the angiotensin type 2 (AT2) receptor agonist, compound 21 (C21), provides neuroprotection and enhances recovery in rodent stroke models yet the mechanism involved is not known. Moreover, C21 treatment is associated with an anti-inflammatory response. Here we tested the hypothesis that C21 mediates neuroprotection by upregulating the neuroprotective and anti-inflammatory cytokine, interleukin (IL)-10. METHODS: Wistar rats were subjected to 3h-middle cerebral artery suture occlusion and treated at reperfusion with C21 (0...
February 10, 2017: European Journal of Pharmacology
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