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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/28315678/protective-effect-of-co-administration-of-curcumin-and-sildenafil-in-alcohol-induced-neuropathy-in-rats
#1
Maninder Kaur, Amarjeet Singh, Bimlesh Kumar, Sachin Kumar Singh, Amit Bhatia, Monica Gulati, T Prakash, Palak Bawa, Adil Hussain Malik
Neuropathic pain associated with chronic alcohol consumption is a medico-socioeconomical problem that affects both central and peripheral nervous system and has no satisfactory treatment till date. The present study was designed to investigate the protective effect of co-administration of curcumin and sildenafil on alcohol induced neuropathic pain in rats. In order to carry out this, ethanol (35% v/v, 10g/kg, p.o.) was administered for 10 weeks to induce neuropathic pain. Curcumin (30 and 60mg/kg, i.p.) and sildenafil (5 and 10mg/kg, i...
March 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315677/rimonabant-a-selective-cannabinoid1-receptor-antagonist-protects-against-light-induced-retinal-degeneration-in-vitro-and-in-vivo
#2
Tomoyo Imamura, Kazuhiro Tsuruma, Yuki Inoue, Tomohiro Otsuka, Yuta Ohno, Shiho Ogami, Shinsaku Yamane, Masamitsu Shimazawa, Hideaki Hara
The endocannabinoid system is involved in some neurodegenerative diseases such as Alzheimer's disease. An endogenous constellation of proteins related to cannabinoid1 receptor signaling, including free fatty acids, diacylglycerol lipase, and N-acylethanolamine-hydrolyzing acid amidase, are localized in the murine retina. Moreover, the expression levels of endogenous agonists of cannabinoid receptors are changed in the vitreous fluid. However, the role of the endocannabinoid system in the retina, particularly in the light-induced photoreceptor degeneration, remains unknown...
March 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315345/inositol-hexaphosphate-suppresses-colorectal-cancer-cell-proliferation-via-the-akt-gsk-3%C3%AE-%C3%AE-catenin-signaling-cascade-in-a-1-2-dimethylhydrazine-induced-rat-model
#3
Wenyang Yu, Cuiping Liu, Xin Li, Fuguo Yang, Lixue Cheng, Chang Liu, Yang Song
Colorectal cancer (CRC) is common worldwide, and most treatments for CRC have undesirable side effects. Many researchers have demonstrated that inositol hexaphosphate (IP6) has potent anticarcinogenic activity against CRC and no apparent toxicity to normal cells. However, the underlying mechanism is still unclear. In this study, we investigated the anticancer and anti-proliferative properties of IP6 in CRC and its possible mechanisms during this chemopreventive process. We examined the expression of genes related to the PI3K/Akt and Wnt pathways at the transcriptional and translational levels in a DMH-induced rat CRC model following IP6 administration...
March 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315346/inhibition-of-osteoporosis-by-the-%C3%AE-v%C3%AE-3-integrin-antagonist-of-rhodostomin-variants
#4
Tzu-Hung Lin, Rong-Sen Yang, Huang-Ju Tu, Houng-Chi Liou, Yen-Ming Lin, Woie-Jer Chuang, Wen-Mei Fu
Integrins are heterodimeric cell surface receptors that mediate cell-cell and cell-matrix interaction. The vitronectin and osteopontin receptor αvβ3 integrin has increased expression levels and is implicated in the adhesion, activation, and migration of osteoclasts on the bone surface as well as osteoclast polarization. αvβ3 integrin plays an important role in osteoclast differentiation and resorption. In addition, Arg-Gly-Asp (RGD)-containing peptides, small molecular inhibitors, and antibodies to αvβ3 integrin have been shown to inhibit bone resorption in vitro and in vivo...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315344/further-analysis-of-the-inhibition-by-agmatine-on-the-cardiac-sympathetic-outflow-role-of-the-%C3%AE-2-adrenoceptor-subtypes
#5
Luis Cobos-Puc, Hilda Aguayo-Morales, Janeth Ventura-Sobrevilla, Diana Luque-Contreras, Miguel Chin-Chan
This study has investigated the role of the α2-adrenoceptor subtypes involved in the inhibition of the cardiac sympathetic outflow induced by intravenous (i.v) infusions of agmatine. Therefore, we analysed the effect of an i.v. bolus injections of the selective antagonists BRL 44408 (300μg/kg; α2A), imiloxan (3000μg/kg; α2B), and JP-1302 (300μg/kg; α2C) given separately, and their combinations: BRL 44408 plus Imiloxan, JP 1302 plus imiloxan, BRL 44408 plus JP-1302, BRL 44408 plus imiloxan plus JP-1302 on the cardiac sympatho-inhibition of agmatine...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315343/inhibition-of-agonist-induced-smooth-muscle-contraction-by-picotamide-in-the-male-human-lower-urinary-tract-outflow-region
#6
Martin Hennenberg, Alexander Tamalunas, Yiming Wang, Patrick Keller, Melanie Schott, Frank Strittmatter, Annika Herlemann, Qingfeng Yu, Beata Rutz, Anna Ciotkowska, Christian G Stief, Christian Gratzke
Male lower urinary tract symptoms (LUTS) due to bladder outlet obstruction are characterized by abnormal smooth muscle contractions in the lower urinary tract. Alpha1-adrenoceptor antagonists may induce smooth muscle relaxation in the outflow region and represent the current goldstandard of medical treatment. However, results may be unsatisfactory or inadequate. Apart from α1-adrenoceptor agonists, smooth muscle contraction in the outflow region may be induced by thromboxane A2 (TXA2), endothelins, or muscarinic receptor agonists...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315342/ethanol-induced-erectile-dysfunction-and-increased-expression-of-pro-inflammatory-proteins-in-the-rat-cavernosal-smooth-muscle-are-mediated-by-nadph-oxidase-derived-reactive-oxygen-species
#7
Letícia N Leite, Gabriel T do Vale, Janaina A Simplicio, Bruno S De Martinis, Fernando S Carneiro, Carlos R Tirapelli
Ethanol consumption is associated with an increased risk of erectile dysfunction (ED), but the molecular mechanisms through which ethanol causes ED remain elusive. Reactive oxygen species are described as mediators of ethanol-induced cell toxicity/damage in distinctive tissues. The enzyme NADPH oxidase is the main source of reactive oxygen species in the endothelium and vascular smooth muscle cells and ethanol is described to increase NADPH oxidase activation and reactive oxygen species generation. This study evaluated the contribution of NADPH oxidase-derived reactive oxygen species to ethanol-induced ED, endothelial dysfunction and production of pro-inflammatory and redox-sensitive proteins in the rat cavernosal smooth muscle (CSM)...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315341/low-doses-of-tizanidine-synergize-the-anti-nociceptive-and-anti-inflammatory-effects-of-ketorolac-or-naproxen-while-reducing-of-side-effects
#8
Selene I Patiño-Camacho, Myrna Déciga-Campos, Karla Beltrán-Villalobos, Dalia A Castro-Vidal, Rosa M Montiel-Ruiz, Francisco J Flores-Murrieta
The aim of the present study was to determine whether tizanidine, an alpha2-adrenoceptor agonist, is able to increase the anti-inflammatory and anti-nociceptive effects of naproxen and ketorolac with a low incidence of gastric injury and spontaneous activity in rats. The anti-inflammatory effect was assayed in a carrageenan test, and oral administration of tizanidine (ED40 = 0.94 ± 0.2mg/kg), naproxen (ED40 = 3.18 ± 0.4mg/kg), and ketorolac (ED40 = 16.4 ± 1.9mg/kg) showed a dose-dependent effect on inflammation...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315340/in-vivo-pharmacological-profile-of-s-38093-a-novel-histamine-h3-receptor-inverse-agonist
#9
Fany Panayi, Aurore Sors, Lionel Bert, Brigitte Martin, Gaelle Rollin-Jego, Rodolphe Billiras, Isabelle Carrié, Karine Albinet, Laurence Danober, Nathalie Rogez, Jean-Yves Thomas, Luigi Pira, Valérie Bertaina-Anglade, Pierre Lestage
S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive and arousal properties. In intracerebral microdialysis studies performed in rats, S 38093 dose-dependently increased histamine extracellular levels in the prefrontal cortex and facilitated cholinergic transmission in the prefrontal cortex and hippocampus of rats after acute and chronic administration (10mg/kg i.p.). Acute oral administration of S 38093 at 0...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28300593/functional-estimation-of-endothelin-1-receptor-antagonism-by-bosentan-macitentan-and-ambrisentan-in-human-pulmonary-and-radial-arteries-in-vitro
#10
James A Angus, Paul F Soeding, Richard J A Hughes, Christine E Wright
BACKGROUND: Endothelin receptor antagonists are approved for pulmonary arterial hypertension. Development of selective ETA-receptor antagonists over mixed or dual receptor antagonists has depended on a range of receptor binding assays, second messenger assays and functional blood vessel assays. This study compared the 3 clinically-approved endothelin receptor antagonists in assays of human isolated pulmonary and radial arteries in vitro. METHODS: Human isolated pulmonary (i...
March 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28300592/new-peptide-inhibitors-modulate-the-self-assembly-of-islet-amyloid-polypeptide-residues-11-20-in-vitro
#11
Yexuan Mao, Lanlan Yu, Ran Yang, Chuanguo Ma, Lingbo Qu, Peter de B Harrington
The structural transition and misfolding of human islet amyloid polypeptide may cause a common metabolic disease Type 2 diabetes mellitus. Seventeen peptides have been synthesized, possessing different lengths, compositions, and peptide conformation. In this study, the mechanism of these peptides on inhibiting the formation of hIAPP11-20 amyloid fibrils was investigated using a conventional ThT fluorescence assay and microscale thermophoresis. The results showed that short peptides AT, SA, RF, KS, KT and KN, and cyclic peptides cyclic-KS, cyclic-KT and cyclic-KN displayed considerable inhibitory effect on hIAPP11-20 fibril formation and a strong affinity for hIAPP11-20...
March 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28300591/mir-455-inhibits-breast-cancer-cell-proliferation-through-targeting-cdk14
#12
Bing Wang, Aimei Zou, Liqiang Ma, Xiong Chen, Lie Wang, Ximing Zeng, Ting Tan
Breast cancer is the most frequently occurring cancer in women worldwide, microRNAs (miRNAs) play critical role in the initiation and progression of breast cancer. Here, we studied the effect of miR-455 on cell proliferation of breast cancer, and found that miR-455 was downregulated in breast cancer tissues and cells. Its overexpression inhibited cell proliferation, whereas its knockdown promoted cell proliferation of breast cancer. We found a Cdc2-related protein kinase CDK14 was the target of miR-455, when the 3(')UTR of CDK14 was cloned into luciferase reporter vector and transfected into cells, miR-455 mimic could inhibit the luciferase activity in a dose-dependent manner, miR-455 inhibitor increased the luciferase activity, but the mutant miR-455 mimic couldn't change the luciferase activity, suggesting miR-455 directly bound to the 3(')UTR of CDK14...
March 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28286125/n-propyl-gallate-suppresses-lipopolysaccharide-induced-inducible-nitric-oxide-synthase-activation-through-protein-kinase-c%C3%AE-mediated-up-regulation-of-heme-oxygenase-1-in-raw264-7-macrophages
#13
Wookwang Jeon, Seong Ji Park, Byung-Chul Kim
n-Propyl gallate is a synthetic phenolic antioxidant with potential anti-inflammatory effects. However, the underlying mechanism remains largely unknown. In the present study, we showed that n-propyl gallate increases the expression and activity of the heme oxygenase-1 (HO-1), a stress-inducible protein with potent anti-inflammatory activity, in RAW264.7 macrophages. The inhibition of the HO-1 activity by treatment with zinc (II) protoporphyrin IX (ZnPP) or by knockdown of the HO-1 expression with small interference RNA significantly reversed the inhibitory effect of n-Propyl gallate on activations of nuclear factor-κB (NF-κB) and inducible nitric oxide synthase (iNOS) induced by lipopolysaccharide (LPS)...
March 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28286124/pharmacological-evidence-for-systemic-and-peripheral-antinociceptive-activities-of-pioglitazone-in-the-rat-formalin-test-role-of-ppar%C3%AE-and-nitric-oxide
#14
Mohammad Taghi Mansouri, Bahareh Naghizadeh, Behnam Ghorbanzadeh, Hossein Rajabi, Marzieh Pashmforoush
Nitric oxide (NO) is involved in numerous physiological processes of the central and peripheral nervous system. This study aimed to evaluate the involvement of PPARγ and NO pathway in the systemic and peripheral antinociceptive effect pioglitazone (Pio) using formalin test in rats. After allocation, rats were injected with 2.5% formalin solution and the flinching behaviors were recorded for 5min (phase 1) and 15-60min (phase 2). pioglitazone was administered intraperitoneally (i.p.) at doses (10-50mg/kg) and intraplantarly (i...
March 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28286123/the-enhancement-of-txa2-receptors-mediated-contractile-response-in-intrarenal-artery-dysfunction-in-type-2-diabetic-mice
#15
Su-Juan Kuang, Jie-Sheng Qian, Hui Yang, Fang Rao, Xiao-Yan Chen, Meng-Zhen Zhang, Zhi-Xin Shan, Qiu-Xiong Lin, Yu-Mei Xue, Shu-Lin Wu, Li Jiang, Chun-Bo Chen, Chun-Yu Deng
Thromboxane A2 (TXA2) has been implicated in the pathogenesis of diabetic vascular complications, although the underlying mechanism remains unclear. The present study investigated the alterations in TXA2 receptor signal transduction in type 2 diabetic renal arteries. The contraction of renal arterial rings in control (db/m+) mice and type 2 diabetic (db/db) mice was measured by a Multi Myograph System. Intracellular calcium concentration ([Ca(2+)]i) in vascular smooth muscle cells was measured by Fluo-4/AM dye and confocal laser scanning microscopy...
March 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28284753/effects-of-nebulised-magnesium-sulphate-on-inflammation-and-function-of-the-guinea-pig-airway
#16
Dawn L Turner, William R Ford, Emma J Kidd, Kenneth J Broadley, Colin Powell
Magnesium sulphate is a potential treatment for acute severe asthma. However, the mechanisms and dose-response relationships are poorly understood. The first objective of this study was to examine whether inhaled magnesium sulphate exerts bronchodilator activity measured as bronchoprotection against histamine-induced bronchoconstriction in conscious guinea-pigs alone and combined with salbutamol. Secondly, we examined whether inhaled magnesium sulphate inhibits airways inflammation and function in models of neutrophilic and eosinophilic lung inflammation induced, respectively, by inhaled lipopolysaccharide or the inhaled antigen, ovalbumin (OVA)...
March 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28284752/troxerutin-exerts-neuroprotection-in-6-hydroxydopamine-lesion-rat-model-of-parkinson-s-disease-possible-involvement-of-pi3k-er%C3%AE-signaling
#17
Tourandokht Baluchnejadmojarad, Nida Jamali-Raeufy, Sedigheh Zabihnejad, Nafiseh Rabiee, Mehrdad Roghani
Parkinson's disease (PD) is a neurodegenerative disease with progressive loss of mesencephalic dopaminergic neurons of the substantia nigra and with multiple incapacitating motor and non-motor symptoms. Troxerutin is a natural bioflavonoid with nephro- and hepato-protective, antioxidant, and anti-inflammatory properties. In this study, we evaluated its possible neuroprotective effect in 6-hydroxydopamine (6-OHDA) rat model of PD. Intrastriatal 6-OHDA-lesioned rats were pretreated with troxerutin at a dose of 150mg/kg/day for 1 week...
March 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28283388/psoralidin-a-prenylated-coumestan-as-a-novel-anti-osteoporosis-candidate-to-enhance-bone-formation-of-osteoblasts-and-decrease-bone-resorption-of-osteoclasts
#18
Yuankun Zhai, Yingying Li, Yanping Wang, Jiawei Cui, Kun Feng, Xijian Kong, Li Chen
Traditional Chinese medicines (TCM) have been proven to prevent osteoporosis, but their clinical applications are not widely recognized due to their complicated ingredients. Psoralidin, a prenylated coumestan, has been reported to prevent bone loss of ovariectomized rats, but detailed mechanisms are still not clear. In current study, we found that both psoralidin and coumestrol promoted osteoblast proliferation and differentiation, as evidenced by improvements in cell proliferation and alkaline phosphatase activity; increased formation of ALP colonies and calcified nodules; enhanced secretion of collagen-I, BMP-2, osteocalcin and osteopontin; and stimulation of the expression of IGF-1, β-catenin, Runx-2, Osterix, and OPG, as well as the mRNA ratio of OPG/RANKL, while significantly decreasing the expression of RANKL...
March 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28274625/apd668-a-g-protein-coupled-receptor-119-agonist-improves-fat-tolerance-and-attenuates-fatty-liver-in-high-trans-fat-diet-induced-steatohepatitis-model-in-c57bl-6-mice
#19
Umakant Ashok Bahirat, Rekha Raghuveer Shenoy, Rajan Naresh Goel, Kumar V S Nemmani
G-protein coupled receptor 119 (GPR119) receptor is a rhodopsin-like, class A Gαs-coupled receptor, predominantly expressed in pancreatic islet cells and intestinal entero-endocrine cells. GPR119 has been emerged as a novel therapeutic target for the treatment of dyslipidemia in type 2 diabetes. In this study, we investigated the effect of APD668, a GPR119 agonist alone and in combination with linagliptin, a DPPIV inhibitor on oral fat tolerance test. Our findings demonstrate that APD668, a GPR119 agonist inhibits the intestinal triglyceride absorption after acute fat load in mice...
March 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28263754/licocoumarone-isolated-from-glycyrrhiza-uralensis-selectively-alters-lps-induced-inflammatory-responses-in-raw-264-7-macrophages
#20
Lehao Wu, Yunpeng Fan, Chao Fan, Yang Yu, Lei Sun, Yu Jin, Yan Zhang, Richard D Ye
The effects of licocoumarone (LC) isolated from Glycyrrhiza uralensis were studied in LPS-stimulated RAW 264.7 macrophages. Our study demonstrated that LC dose-dependently attenuated LPS-induced NO production by down-regulating iNOS expression. Additionally, the treatment with LC inhibited LPS-induced expression of cytokines including IL-1β, IL-6 and IL-10, but not TNF-α, at both mRNA and protein levels. Similar suppressive effects of LC were observed on LPS-stimulated murine peritoneal macrophages as well...
March 2, 2017: European Journal of Pharmacology
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