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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/27919660/a-comparison-of-vasodilation-mode-among-selexipag-ns-304-2-4-5-6-diphenylpyrazin-2-yl-isopropyl-amino-butoxy-n-methylsulfonyl-acetamide-its-active-metabolite-mre-269-and-various-prostacyclin-receptor-agonists-in-rat-porcine-and-human-pulmonary-arteries
#1
Chiaki Fuchikami, Kohji Murakami, Koyuki Tajima, Junko Homan, Keiji Kosugi, Kazuya Kuramoto, Michiko Oka, Keiichi Kuwano
Selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N- (methylsulfonyl)acetamide]) is a novel, orally available non-prostanoid prostacyclin receptor (IP receptor) agonist that has recently been approved for the treatment of pulmonary arterial hypertension (PAH). We examined the effect of the active metabolite of selexipag, MRE-269, and IP receptor agonists that are currently available as PAH therapeutic drugs on the relaxation of rat, porcine and human pulmonary artery. cAMP formation in human pulmonary artery smooth muscle cells was induced by all test compounds (MRE-269, epoprostenol, iloprost, treprostinil and beraprost sodium) and suppressed by IP receptor antagonists (CAY10441 and 2-[4-(1H-indol-4-yloxymethyl)-benzyloxycarbonylamino]-3-phenyl-propionic acid)...
December 2, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916557/histone-acetylation-and-histone-deacetylation-in-neuropathic-pain-an-unresolved-puzzle
#2
REVIEW
Ravneet Kaur Khangura, Anjana Bali, Amteshwar Singh Jaggi, Nirmal Singh
Chronic pain is broadly classified into somatic, visceral or neuropathic pain depending upon the location and extent of pain perception. Evidences from different animal studies suggest that inflammatory or neuropathic pain is associated with altered acetylation and deacetylation of histone proteins, which result in abnormal transcription of nociceptive processing genes. There have been a number of studies indicating that nerve injury up-regulates histone deacetylase enzymes, which leads to increased histone deacetylation and induce chronic pain...
December 2, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916559/rhinacanthin-c-enhances-doxorubicin-cytotoxicity-via-inhibiting-the-functions-of-p-glycoprotein-and-mrp2-in-breast-cancer-cells
#3
Tassarut Chaisit, Pongpun Siripong, Suree Jianmongkol
Rhinacanthin-C is a major bioactive naphthoquinone ester found in Rhinacanthus nasutus Kurz (Acanthaceae). This compound has potential therapeutic value as an anticancer and antiviral agent. In this study, we investigated an enhancement effect of rhinacanthin-C on doxorubicin cytotoxicity in human breast cancer cell lines and the involvement of the ABC drug efflux transporters. The cytotoxicity was determined by an MTT assay. Combination between doxorubicin and rhinacanthin-C at their non-cytotoxic concentrations when giving each compound alone significantly reduced cell viability in MCF-7 and MCF-7/DOX resistant cells...
December 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916558/role-of-carvacrol-in-cardioprotection-against-myocardial-ischemia-reperfusion-injury-in-rats-through-activation-of-mapk-erk-and-akt-enos-signaling-pathways
#4
Yunping Chen, Lina Ba, Wei Huang, Yan Liu, Hao Pan, E Mingyao, Pilong Shi, Ye Wang, Shuzhi Li, Hanping Qi, Hongli Sun, Yonggang Cao
Carvacrol (CAR) is a compound isolated from some essential oils, many studies have demonstrated its therapeutic potential on different diseases. This study aims to evaluate the protective effect of CAR against myocardial ischemia/reperfusion (I/R) injury in rats. Male adult rats underwent ligation of the left anterior descending coronary artery (LAD) in I/R models. Rats were treated with CAR after LAD. The levels of I/R- induced infarct size, cardiomyocyte apoptosis and cardiac functional impairment were examined...
December 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916556/micrornas-mediated-epithelial-mesenchymal-transition-in-fibrotic-diseases
#5
REVIEW
Xiao-Zhou Zou, Ting Liu, Zhi-Cheng Gong, Chang-Ping Hu, Zheng Zhang
MicroRNAs (miRNAs), a large family of small and highly conserved non-coding RNAs, regulate gene expression through translational repression or mRNA degradation. Aberrant expression of miRNAs underlies a spectrum of diseases including organ fibrosis. Recent evidence suggests that miRNAs contribute to organ fibrosis through mediating epithelial-mesenchymal transition (EMT). Alleviation of EMT has been proposed as a promising strategy against fibrotic diseases given the key role of EMT in fibrosis. miRNAs impact the expression of specific ligands, receptors, and signaling pathways, thus modulating EMT and consequently influencing fibrosis...
December 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916555/adx71943-and-adx71441-novel-positive-allosteric-modulators-of-the-gabab-receptor-with-distinct-central-peripheral-profiles-show-efficacy-in-the-monosodium-iodoacetate-model-of-chronic-osteoarthritis-pain-in-the-rat
#6
Mikhail Kalinichev, Tansy Donovan-Rodriguez, Françoise Girard, Hasnaá Haddouk, Isabelle Royer-Urios, Manfred Schneider, Simon T Bate, Cheryl Marker, James D Pomonis, Sonia Poli
We tested novel positive allosteric modulators (PAMs) of the γ-aminobutyric acid receptor B (GABAB), ADX71943 and ADX71441in the monosodium iodoacetate model of chronic osteoarthritis pain in rats with the objective to delineate the role of peripheral versus central GABAB receptor populations in modulation of chronic pain. Anesthetized Sprague-Dawley rats received an injection of monosodium iodoacetate into the knee and were tested for hyperalgesia starting post-MIA day 14. Effects of compounds on ipsilateral joint compression threshold were evaluated on post-MIA day 14 (after acute treatment), as well as after repeated, daily treatment on days 21 and 28 (ADX71943 only) and were compared to those of celecoxib (30mg/kg, p...
December 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27916554/activating-akt-to-inhibit-jnk-by-troxerutin-antagonizes-radiation-induced-pten-activation
#7
Ping Xu, Wen-Bo Zhang, Xin-Hua Cai, Pei-Yong Qiu, Ming-Hua Hao, Dan-Dan Lu
Radiotherapy is one of the most effective non-surgical treatments for many tumors. However, radiation damage remains a major negative consequence of radiotherapy. At present, radio-protective effect of troxerutin has been confimed, but the mechanism of this radioprotection has not been elucidated. Here, this study showed that troxerutin protected thymus tissue of irradiated mice, and its radio-protective effect on thymocytes was significant in the range of 0.625-10μg/ml. Troxerutin significantly inhibited apoptosis of irradiated thymocytes at the concentration of 10μg/ml...
December 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27915044/a-novel-aldosterone-synthase-inhibitor-ameliorates-mortality-in-pressure-overload-mice-with-heart-failure
#8
Shinji Furuzono, Masaki Meguro, Satoru Miyauchi, Shinichi Inoue, Tsuyoshi Homma, Keisuke Yamada, Yoh-Ichi Tagawa, Futoshi Nara, Takahiro Nagayama
It has been elucidated that mineralocorticoid receptor antagonists reduce mortality in patients with congestive heart failure and post-acute myocardial infarction. A direct inhibition of aldosterone synthase (CYP11B2) is also expected to have therapeutic benefits equal in quality to mineralocorticoid receptor antagonists in terms of reducing mineralocorticoid receptor signaling. Therefore, we have screened our chemical libraries and identified a novel and potent aldosterone synthase inhibitor, 2,2,2-trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-y}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol (compound 1), by lead optimization...
November 30, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27915043/involvement-of-bdnf-trkb-signaling-in-the-effect-of-diphenyl-diselenide-on-motor-function-in-a-parkinson-s-disease-rat-model
#9
Tuane Bazanella Sampaio, Simone Pinton, Juliana Trevisan da Rocha, Bibiana Mozzaquatro Gai, Cristina Wayne Nogueira
Parkinson's disease is a progressive neurodegenerative disorder characterized by degeneration of nigrostriatal dopaminergic neurons. Diphenyl diselenide [(PhSe)2] is a compound with pharmacological proprieties, such as antidepressant and neuroprotective. Therefore, this study investigated whether (PhSe)2 reverses motor impairment and neurochemical alterations in a model of Parkinson's disease induced by 6-hydroxydopamine (6-OHDA) in rats. For this, male Wistar rats received 20μg/3μl of 6-OHDA or vehicle into the right striatum...
November 30, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27915042/non-coding-rnas-and-berberine-a-new-mechanism-of-its-anti-diabetic-activities
#10
REVIEW
Wenguang Chang
Type 2 Diabetes (T2D) is a metabolic disease with high mortality and morbidity. Non-coding RNAs, including small and long non-coding RNAs, are a novel class of functional RNA molecules that regulate multiple biological functions through diverse mechanisms. Studies in the last decade have demonstrated that non-coding RNAs may represent compelling therapeutic targets and play important roles in regulating the course of insulin resistance and T2D. Berberine, a plant-based alkaloid, has shown promise as an anti-hyperglycaemic, anti-hyperlipidaemic agent against T2D...
November 30, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27915041/garlic-active-constituent-s-allyl-cysteine-protects-against-lipopolysaccharide-induced-cognitive-deficits-in-the-rat-possible-involved-mechanisms
#11
Mahboubeh Zarezadeh, Tourandokht Baluchnejadmojarad, Zahra Kiasalari, Siamak Afshin-Majd, Mehrdad Roghani
Neuroinflammation is known as a risk factor for cognitive deficit and dementia and its incidence increased with aging. S-allyl cysteine (SAC) is the active and main component of aged garlic extract with anti-inflammatory, neuroprotective, and nootropic potential. In this study, the protective effect of SAC against lipopolysaccharide (LPS)-induced cognitive deficit in the rat was investigated. For induction of learning and memory impairment and neuroinflammation, LPS was intraperitoneally injected at a dose of 167 μg/kg for 7 days and SAC was administered p...
November 30, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27913104/d-ala2-gip-glu-pal-is-neuroprotective-in-a-chronic-parkinson-s-disease-mouse-model-and-increases-bndf-expression-while-reducing-neuroinflammation-and-lipid-peroxidation
#12
Yanwei Li, WeiZhen Liu, Lin Li, Christian Hölscher
Type 2 diabetes mellitus (T2DM) is a risk factor for Parkinson's disease (PD). Therefore, treatment to improve insulin resistance in T2DM may be useful for PD patients. Glucose dependent insulinotropic polypeptide (GIP) is a member of the incretin hormone family that can promote insulin release and improve insulin resistance. Several GIP analogues have been developed as potential treatments for T2DM. We had shown previously that D-Ala2-GIP-glu-PAL, a novel long-acting GIP analogue, can play a neuroprotective role in the PD mouse model induced by acute MPTP injection...
November 29, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27908790/mpp-inhibits-mglur1-5-mediated-long-term-depression-in-mouse-hippocampus-by-calpain-activation
#13
Junyao Li, Hui Chen, Shengbing Wu, Yuefa Cheng, Qinglin Li, Jing Wang, Guoqi Zhu
Neurotoxins are harmful to nervous system and cause either neuronal cell death or impairment of synaptic activity, which contributes to Parkinson's disease or other neuronal disorders. Hippocampal synaptic plasticity was proposed as a cellular model for memory processing. In this study, we reported a novel effect of neurotoxin, 1-methyl-4-phenylpyridinium (MPP(+)), on metabotropic glutamate receptor 1/5 agonist, 3,5-dihydroxyphenylglycine (DHPG)-induced hippocampal synaptic plasticity, and MPP(+) incubation blocked DHPG-induced hippocampal long-term depression (LTD) in Schaffer collateral-CA1 synapses...
November 28, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894811/critical-role-of-toll-like-receptors-in-pathophysiology-of-allergic-asthma
#14
Seyyed Shamsadin Athari, Seyyede Masoume Athari, Fateme Beyzay, Masoud Movassaghi, Esmaeil Mortaz, Mehdi Taghavi
Allergic asthma is an airway disease, characterized by reversible bronchoconstriction, chronic inflammation of the airway, and thickness of smooth muscle in the respiratory tract. Asthma is orchestrated by an excessive Th2-adaptive immune response, in which innate immunity plays a key role. Recently TLRs have received more and more attention as they are central to orchestrate the innate immune responses. TLRs are localized as integral membrane or intracellular glycoproteins with those on the cell surface sensing microbial antigens and the ones, localized in intracellular vesicles, sensing microbial nucleic acid species...
November 26, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894814/tanshinone-iia-induced-cell-death-via-mir30b-p53-ptpn11-shp2-signaling-pathway-in-human-hepatocellular-carcinoma-cells
#15
Xuanqi Ren, Cui Wang, Binbin Xie, Linfeng Hu, Hui Chai, Lei Ding, Lihua Tang, Yongliang Xia, Xiaobing Dou
Tanshinone IIA, a multi-pharmaceutical compound from traditional Chinese herb, has been reported to have anti-hepatocarcinomic (HCC) properties through cell death induction. Apart from the typical p53-dependent pathway, mechanisms of the anti-carcinogenic role of Tanshinone remain scarce. In an effort to explore the mechanism behind Tanshinone IIA, we detected the upstream of the p53 and the potential novel pathway. Tanshinone IIA dose-dependently initiated HepG2 cell apoptosis and cell cycle arrest at the G1 checkpoint...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894813/salicylic-acid-retention-impairs-aspirin-reactivity-in-type-2-diabetes
#16
Haowen Zhang, Hao Xie, Xiao Zheng, Yingying Chai, Zhiyuan Tang, Hanyu Chen, Feiyan Li, Heier Christoph, Jiandong Chen, Weixin Sun, Hui Ye, Shiguang Wang, Haiping Hao, Xiaohu Chen
High on-aspirin platelet reactivity (HAPR) has been associated with compromised aspirin efficacy in patients with diabetes suffering from acute cardiovascular events, but the key mechanisms remain elusive. The objective of this study was to uncover the potential link between pathogenic accumulation of salicylic acid (SA), the major metabolite of aspirin, and HAPR in diabetic state. Aspirin failed to inhibit platelet CD62P expression and thromboxane (TX) B2/6-keto-prostaglandin(PG)F1α ratio in a type 2 diabetes mellitus (T2DM) mice model, particularly in the female, which were unanimously accompanied by significantly higher plasma SA concentrations...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894812/enhanced-legumain-recognition-and-nir-controlled-released-of-cisplatin-indocyanine-nanosphere-against-gastric-carcinoma
#17
Tianyi Shi, Lianshuai Gu, Yu Sun, Senlin Wang, Chaoqun You, Xiangyang Zhang, Jin Zhu, Baiwang Sun
Cisplatin-therapy has faced limitations in the gastric cancer therapy. To settle the bottleneck, enhanced specificity and controlled-release property are choosen. We synthesize cisplatin and indocyanine green (ICG) loaded PLGA-(DSPE-PEG2000) nanoparticles, which is abbreviated as CINPs. And we conjugate the Gly-Cys-Gly-Ala-Ala-Asn-Leu (GCGAANL) heptapeptide upon the surface of CINPs, the product is abbreviated as ACINPs. ACINPs with nearly 110nm exhibit good monodispersity and size stability. The EE (efficiency of encapsulation) and LE (loading of encapsulation) of cisplatin loaded into ACINPs are optimized as 29...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894810/na-ca-2-exchanger-1-inhibition-abolishes-ischemic-tolerance-induced-by-ischemic-preconditioning-in-different-cardiac-models
#18
Pasqualina Castaldo, Maria Loredana Macrì, Vincenzo Lariccia, Alessandra Matteucci, Marta Maiolino, Santo Gratteri, Salvatore Amoroso, Simona Magi
Ca(2+)-handling disturbances play an important role in the genesis of myocardial ischemia/reperfusion (I/R) injury. Ischemic preconditioning (IPC) is a powerful strategy to induce tolerance against subsequent ischemic episodes. IPC signaling pathways may be triggered by Ca(2+) ion. Since Na(+)/Ca(2+) exchanger 1 (NCX1) participates in modulating intracellular Ca(2+) homeostasis, here we further defined its role in I/R and investigated its potential involvement in IPC-induced cardioprotection. In isolated ventricular cardiomyocytes, perfused rat heart and H9c2 cardiomyoblasts, I/R produced a significant cell injury, assessed by measuring extracellular lactate dehydrogenase (LDH) and, for the whole heart, also by estimating myocardial infarct size area...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894809/cyclic-amp-camp-confers-drug-resistance-against-dna-damaging-agents-via-pkaia-in-cml-cells
#19
Ling-Yi Xiao, Wai-Ming Kan
Cyclic adenosine monophosphate (cAMP) regulates many vital functions such as metabolism, proliferation, differentiation and death. Depending on cell types and stimulators, cAMP could either promote or attenuate cell death. cAMP signal can be transduced by protein kinase A (PKA) and/or exchange protein directly activated by cAMP (EPAC). In CML cells, cAMP may suppress their proliferation and enhance their differentiation. However, the role of cAMP on DNA damaging agent toxicity and the mechanism involved has not been studied...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27894808/protective-effect-of-betulinic-acid-on-early-atherosclerosis-in-diabetic-apolipoprotein-e-gene-knockout-mice
#20
Jung Joo Yoon, Yun Jung Lee, Byung Hyuk Han, Eun Sik Choi, Min Chul Kho, Ji Hun Park, You Mee Ahn, Hye Yoom Kim, Dae Gill Kang, Ho Sub Lee
Atherosclerosis, a chronic and progressive disease, is a leading cause of endothelial dysfunction, diabetes mellitus, hypertension, and hypercholesterolemia. Betulinic acid (BA), a pentacyclic triterpene, has been reported to have a variety of biological effects, including anti-inflammatory and immunomodulatory properties. This study was designed to determine whether BA could prevent atherosclerosis in diabetic apolipoprotein-E gene knockout (ApoE KO) mice. The mice were treated with BA for 12 weeks to examine its beneficial effects on atherosclerosis in ApoE KO mice...
November 25, 2016: European Journal of Pharmacology
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