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Pharmacological Reports: PR

Elżbieta Lorenc-Koci, Anna Czarnecka, Kinga Kamińska, Joanna Knutelska, Małgorzata Zygmunt, Magdalena Dudek
BACKGROUND: Interaction between dopaminergic and nitrergic neurotransmission in the brain plays a crucial role in the control of motor function and in the regulation of blood pressure (BP). In Parkinson's disease (PD), dopaminergic denervation of the striatum leads to disturbances in the nitrergic system in the basal ganglia. Recently, it has been demonstrated that addition of a low dose of the nitric oxide donor molsidomine to l-DOPA therapy improves dopaminergic neurotransmission in the denervated nigrostriatal system and weakens dyskinesias in rodent models of the disease...
September 28, 2016: Pharmacological Reports: PR
Norbert Cibiček, Lenka Roubalová, Jiří Vrba, Martina Zatloukalová, Jiří Ehrmann, Jana Zapletalová, Rostislav Večeřa, Vladimír Křen, Jitka Ulrichová
BACKGROUND: Isoquercitrin (quercetin-3-O-β-d-glucopyranoside) is a flavonoid that exhibited antioxidant and anti-inflammatory activities in a number of in vitro and in vivo studies. Experimental evidence from rodent models of inflammatory bowel disease is, however, lacking. This study was designed to examine whether isoquercitrin effectively and dose-dependently attenuates acute dextran sulfate sodium (DSS)-induced rat colitis. METHODS: Wistar rats were divided into negative control group (exposed to vehicle only), positive control group (DSS-induced colitis plus vehicle), low isoquercitrin group (DSS pretreated with isoquercitrin 1mg/kg/day) and high isoquercitrin group (DSS with isoquercitrin 10mg/kg/day)...
September 19, 2016: Pharmacological Reports: PR
Xia Chen, Hua Guo, Fuxia Li, Di Fan
BACKGROUND: The present study is designed to explore the metastasis-inhibitory effect of physcion 8-O-β-glucopyranoside (PG) in human breast cancer, and the mechanisms underlying its role in tumor metastasis. METHODS: Both in vitro and in vivo studies were conducted. Cell migration and invasion were analyzed by transwell assay. The translocation of β-catenin from the nucleus to cytoplasm membrane was demonstrated by immunofluorescent staining. The expression of signaling molecules was determined by Western blot or qRT-PCR...
September 13, 2016: Pharmacological Reports: PR
Michał Holecki, Gabriela Handzlik-Orlik, Agnieszka Almgren-Rachtan, Jan Duława, Jerzy Chudek
BACKGROUND: Statins are used to reduce a cardiovascular risk. However, the effectiveness of the therapy in many cases remains unsatisfactory. Therefore, the aim of this study was to evaluate the influence of obesity and diabetes on the achievement of therapeutic goal in lipid-lowering therapy in patients with a various cardiovascular risk in the daily clinical practice. METHODS: This study was conducted on the basis of questionnaires obtained from 7018 patients (41...
September 13, 2016: Pharmacological Reports: PR
Katarzyna Kamińska, Karolina Noworyta-Sokołowska, Alexandra Jurczak, Anna Górska, Zofia Rogóż, Krystyna Gołembiowska
BACKGROUND: Schizophrenia is a psychiatric disorder characterized by positive and negative symptoms often accompanied by depression and cognitive deficits. Positive symptoms, like delusions and hallucinations are caused by an excess of dopamine (DA) signaling and are treated with the second generation antipsychotic drugs. Negative symptoms of schizophrenia are represented by social withdrawal, apathy and blunted emotional response. It was demonstrated that co-administration of risperidone and selective serotonin reuptake inhibitors alleviated depressive symptoms and cognitive dysfunction in animal models of schizophrenia...
September 11, 2016: Pharmacological Reports: PR
Ping Chen, Fei-Mi Li, Yu-Fu Zhou, Christopher Qian, Juan Li, Li-Rong Jiang, Zhong-Ming Qian
BACKGROUND: The antioxidant properties of alpha-lipoic acid (ALA) are associated with its ability to reduce iron in cells and tissues, which is partly due to its inhibiting effect on iron uptake from transferrin and its promoting effect on iron deposition into ferritin. However, the relevant mechanisms are unknown. METHODS: We therefore investigated the effects of ALA on the expression of transferrin receptor 1 (TfR1), divalent metal transporter 1 (DMT1), ferroportin 1 (Fpn1) and ferritin in BV-2 microglia cells...
September 11, 2016: Pharmacological Reports: PR
Halil Kara, Fatma Isli, Gokce Sevim Ozturk Fincan, Seniz Yildirim, Sevim Ercan, Yusuf Sarioglu
BACKGROUND: Hydrogen sulfide (H2S) is a gaseous signaling molecule that, similar to nitric oxide (NO), plays an important role as an inhibitor neurotransmitter in the digestive tract. This study aimed to investigate the effect of H2S and to identify neurogenic contraction responses dependent on the electrical field stimulation (EFS) in the isolated lower esophageal sphincters of rabbits. METHODS: An isolated lower esophageal sphincter was placed in an organ bath system and mechanical responses were recorded using a force transducer...
September 6, 2016: Pharmacological Reports: PR
Kamilla Blecharz-Klin, Ilona Joniec-Maciejak, Katarzyna Jawna-Zboińska, Justyna Pyrzanowska, Agnieszka Piechal, Adriana Wawer, Ewa Widy-Tyszkiewicz
BACKGROUND: The present study was designed to clarify the effect of prenatal and postnatal paracetamol administration on the neurotransmitter level and balance of amino acids in the cerebellum. METHODS: Biochemical analysis to determine the concentration of neurotransmitters in this brain structure was performed on two-month-old Wistar male rats previously exposed to paracetamol in doses of 5 (P5, n=10) or 15mg/kg (P15, n=10) throughout the entire prenatal period, lactation and until the completion of the second month of life, when the experiment was terminated...
September 6, 2016: Pharmacological Reports: PR
Joanna Gola, Barbara Strzałka-Mrozik, Celina Kruszniewska-Rajs, Adrian Janiszewski, Bartłomiej Skowronek, Mariusz Gagoś, Grzegorz Czernel, Urszula Mazurek
BACKGROUND: A new form of amphotericin B (AmB)- complex with copper (II) ions (AmB-Cu(2+)) - is less toxic to human renal cells. Cytokines, including Tumor Necrosis Factor (TNF), are responsible for nephrotoxicity observed in patients treated with AmB. Another problem during therapy is the occurrence of oxidized forms of AmB (AmB-ox) in patients' circulation. To elucidate the molecular mechanism responsible for the reduction of the toxicity of AmB-Cu(2+), we evaluated the expression of genes encoding TNF and its receptors alongside encoding proteins involved in TNF-induced signalization...
September 5, 2016: Pharmacological Reports: PR
Tomohiro Mori, Nozomu Abe, Kazutomo Saito, Hiroaki Toyama, Yasuhiro Endo, Yutaka Ejima, Masanori Yamauchi, Mariko Goto, Hajime Mushiake, Itsuro Kazama
BACKGROUND: Besides their anti-inflammatory properties, corticosteroid drugs exert anti-allergic effects. Exocytosis of mast cells is electrophysiologically detected as the increase in the whole-cell membrane capacitance (Cm). Therefore, the lack of such increase after exposure to the drugs suggests their mast cell-stabilizing effects. METHODS: We examined the effects of 1, 10, 100 and 200μM hydrocortisone or dexamethasone on the degranulation from rat peritoneal mast cells...
September 5, 2016: Pharmacological Reports: PR
Marzena Ułamek-Kozioł, Ryszard Pluta, Sławomir Januszewski, Janusz Kocki, Anna Bogucka-Kocka, Stanisław J Czuczwar
We review the Alzheimer-related expression of genes following brain ischemia as risk factors for late-onset of sporadic Alzheimer's disease and their role in Alzheimer's disease ischemia-reperfusion pathogenesis. More recent advances in understanding ischemic etiology of Alzheimer's disease have revealed dysregulation of Alzheimer-associated genes including amyloid protein precursor, β-secretase, presenilin 1 and 2, autophagy, mitophagy and apoptosis. We review the relationship between these genes dysregulated by brain ischemia and the cellular and neuropathological characteristics of Alzheimer's disease...
September 5, 2016: Pharmacological Reports: PR
Antonio Marcos Birocale, Ana Raquel Santos Medeiros, Leandro Dias Gonçalves Ruffoni, Liliam Takayama, José Martins de Oliveira, Keico Okino Nonaka, Rosa Maria Rodrigues Pereira, Nazaré Souza Bissoli
BACKGROUND: Telmisartan, an angiotensin AT1 receptor blocker, and treadmill running were compared for their effects on bone mineral density (BMD) and biomechanical properties of male spontaneously hypertensive rats (SHR). It was hypothesized that running (18m/min/60min/d) and telmisartan (5mg/kg/d) would have a positive effect on bone parameters. METHODS: Three-month-old male SHRs were divided into three groups: sedentary (S), telmisartan (T), and exercise (E). At the end of an 8-week protocol, femur and lumbar vertebrae were analyzed by dual-energy X-ray absorptiometry (DXA) for bone mineral density and by the three-point bending test for biomechanical properties...
September 5, 2016: Pharmacological Reports: PR
Artur Pałasz, Aleksandra Suszka-Świtek, Łukasz Filipczyk, Katarzyna Bogus, Ewa Rojczyk, John Worthington, Marek Krzystanek, Ryszard Wiaderkiewicz
BACKGROUND: Spexin (SPX) is a recently discovered neuropeptide that exhibits a large spectrum of central and peripheral regulatory activity, especially when considered as a potent anorexigenic factor. It has already been proven that antidepressants, including selective serotonin reuptake inhibitors (SSRI), can modulate peptidergic signaling in various brain structures. Despite these findings, there is so far no information regarding the influence of treatment with the SSRI antidepressant escitalopram on brain SPX expression...
September 3, 2016: Pharmacological Reports: PR
Elżbieta Płonka-Półtorak, Paweł Zagrodzki, Jadwiga Kryczyk-Kozioł, Tuomas Westermarck, Pekka Kaipainen, Markus Kaski, Faik Atroshi
BACKGROUND: We aimed to demonstrate the relationship between the valproate (VPA) treatment versus lipid and serum free fatty acids (FFAs) profiles to be the potential atherosclerosis risk factor in epileptic patients. METHODS: Fasting blood samples were taken from 21 adult VPA-treated patients and 21 controls. The profiles of lipids, FFAs, clinical parameters and body mass index (BMI) were evaluated. RESULTS: No significant differences between the study group and controls were found for any of the studied parameters...
September 3, 2016: Pharmacological Reports: PR
Zhi-Qin Liu, Xiao-Mei Song, Que-Ting Chen, Ting Liu, Ji-Tao Teng, Kun Zhou, Du-Qiang Luo
BACKGROUND: Metformin is a first-line drug for treating type 2 diabetes mellitus, yet its mechanism remains only partially understood and controversial. In this study we assessed a global gene expression profiling in liver of KKAy mice affected by metformin. This study aimed to identify the novel anti-diabetic mechanisms of metformin. METHODS: After KKAy mice were administered metformin for 5 weeks, the gene changes profile in the livers of KKAy mice were assessed by using the Agilent whole mice genome oligo microarray...
September 3, 2016: Pharmacological Reports: PR
Anna Gądek-Michalska, Joanna Tadeusz, Paulina Rachwalska, Jan Bugajski
BACKGROUND: The aim of this study was to compare the expression of interleukin-1β (IL-1β), neuronal nitric oxide synthase (nNOS) and inducible nitric oxide synthase (iNOS) in the prefrontal cortex (PFC), hippocampus (HIP) and hypothalamus (HT) during chronic crowding (CS) (psychosocial) and restraint (RS) (physico-psychological) stress. Adaptational changes of these stress mediators to a subsequent acute RS, in two models of chronic stress were investigated. METHODS: Rats were crowded (24 in one cage) or restrained in metal tubes for 10min twice a day for 3, 7, and 14 consecutive days and decapitated...
September 3, 2016: Pharmacological Reports: PR
Helena Shifrin, Dorit Moradov, Corina Bejar, Donna Schorer-Apelbaum, Marta Weinstock
BACKGROUND: In search of safer treatments for inflammatory bowel disease in subjects not responding to, or showing adverse effects to TNF-α antagonists, we tested three novel indoline carbamates in the 2,4-dinitrobenzene sulfonic acid (DNBS) model of colitis in rats. The compounds have anti-inflammatory activity in other disease models in mice. METHODS: AN827 (3-(2-(methoxy carbonyl) ethyl) indolin-4-ylethyl methyl) carbamate (0.1 or 1mg/kg), AN680 (3-(2-(methoxy carbonyl) ethyl) indolin-6-ylethyl methyl) carbamate (1...
August 31, 2016: Pharmacological Reports: PR
Wafaa A Hewedy, Dalia K Mostafa
BACKGROUND: Cyclosporine A (CsA)-induced nephrotoxicity is a challenging problem complicating its chronic use in a large array of autoimmune diseases, as well as in organ transplantation. A considerable body of evidence points to the involvement of nitric oxide (NO) and its endogenous synthesis inhibitor, asymmetric dimethylarginine (ADMA), in CsA-induced renal and cardiovascular adverse effects. In this study, the potential of the third generation β-blocker, nebivolol, to modify the NO/ADMA system is hypothesized to play a role in protection against CsA-induced renal injury and endothelial dysfunction...
August 31, 2016: Pharmacological Reports: PR
Angela M Shysh, Vasyl S Nagibin, Sergii P Kaplinskii, Victor E Dosenko
BACKGROUND: The goal of present investigation is to check the hypothesis that cardioprotective effect of polyunsaturated fatty acids (PUFAs) is mediated by influence on mRNA expression level of the FATP, IL-1ra and GJP43 through stimulation of PPARγ. METHODS: Animals obtained n-3 PUFAs orally during 4 weeks (0.1ml/100g b.w. per day) or during prenatal period. In experiments, isolated perfused hearts were subjected to 20-min regional ischemia and 40min reperfusion...
August 30, 2016: Pharmacological Reports: PR
Ana T G Guerrero, Larissa G Pinto, Fernando Q Cunha, Sérgio H Ferreira, Jose C Alves-Filho, Waldiceu A Verri, Thiago M Cunha
BACKGROUND: Toll-like receptors (TLRs) including TLR4 and their signal pathways contribute to the pathogenesis of arthritis. Herein, we evaluated the mechanisms underlying the hyperalgesic response caused by TLR4 activation in the tibio-tarsal joint in mice. METHODS: Joint inflammatory hyperalgesia was induced by intra-articular (ia) injection of LPS (lipopolysaccharide- TLR4 agonist) in C57BL/6, TLR4, TLR2, MyD88, TRIF, TNFR1/2 and IL-1R1 knockout ((-/-)) mice...
August 24, 2016: Pharmacological Reports: PR
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