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Pharmacological Reports: PR

Aruna Rani, Vikky Rajulapati, Arun Goyal
BACKGROUND: PGs are involved in cellular communication and cancer biology. The role of CS in melanoma and fibrosarcoma cell lines was explored by using chondroitin AC lyase (PsPL8A). METHODS: The proliferation of mouse fibroblast L929, human melanoma (SK-Mel 28) and fibrosarcoma (HT-1080) cell lines after treatment with chondroitin AC lyase (PsPL8A) was studied by MTT assay. The mode of cell death was studied by Annexin-V FITC using flow cytometry and fluorescence microscopy...
October 25, 2018: Pharmacological Reports: PR
Michelle Richter, Selina J Moroniak, Hartmut Michel
BACKGROUND: The osmolyte and antioxidant taurine plays an important role in regulation of cellular volume, oxidative status and Ca2+ -homeostasis. Taurine uptake in human cells is regulated by the Na+ - and Cl- -dependent taurine transporter TauT. In order to gain deeper structural insights about the substrate binding pocket of TauT, a HEK293 cell line producing a GFP-TauT fusion protein was generated. METHODS: Transport activity was validated using cell-based [3 H]-taurine transport assays...
October 24, 2018: Pharmacological Reports: PR
Anna Czajkowska-Kośnik, Marta Szekalska, Katarzyna Winnicka
Skin application of pharmaceutical products is one of the methods used for drug administration. The problem of limited drug penetration via topical application makes searching for safe drug carriers that will provide an expected therapeutic effect of utmost importance. Research into safe drug carriers began with liposome structures, paving the way for work with nanocarriers, which currently play a large role as drug vehicles. Nanostructured lipid carriers (NLC) consist of blended solid and liquid lipids (oils) dispersed in an aqueous solution containing a surfactant...
October 11, 2018: Pharmacological Reports: PR
Naga K R Ghattamaneni, Sunil K Panchal, Lindsay Brown
BACKGROUND: Inflammatory bowel disease (IBD) is an important cause of chronic disability in humans. METHODS: We characterized a model of chronic IBD in young male Wistar rats by administering dextran sodium sulfate (DSS: 0%, 0.25%, 0.5%, or 1% in drinking water) for six weeks, with 0.5% DSS for twelve weeks, following DSS cessation or together with treatment with sulfasalazine for the last 6 weeks. We measured gastrointestinal characteristics including stool consistency, blood in stools, small intestine and colon length, intestinal transit and permeability, and gut microbiota, as well as extra-intestinal parameters including oral glucose tolerance, systolic blood pressure, fat and lean mass, and left ventricular stiffness...
October 11, 2018: Pharmacological Reports: PR
Matteo Micucci, Alberto Chiarini, Roberta Budriesi
BACKGROUND: Constitutive (agonist-independent) activity is a prerogative of many G protein-coupled receptors (GPCRs) including α1 -adrenoceptors (α1 -ARs). Inhibition of such an activity at α1 -AR subtypes by antagonists with negative efficacy is difficult to be adequately tested. METHODS: In the present experimental approach, we compared the activity of three calcium channel blockers (nifedipine, diltiazem and verapamil) and of three potent benzodioxane-based α1 -AR antagonists, differing for subtype selectivity and inverse agonist properties, in producing smooth muscle relaxation and negative inotropy under the same test conditions...
October 11, 2018: Pharmacological Reports: PR
Paulina Jaworska-Andryszewska, Janusz K Rybakowski
A contemporary model for the pathogenesis of mood disorders (bipolar and depressive disorders) involves gene-environmental interaction, with genetic predisposition, epigenetic regulation, and environmental effects. Among multiple environmental factors, the experience of childhood trauma can be connected with the pathogenesis, course and the treatment of mood disorders. Patients with mood disorders have the greater frequency of childhood trauma compared with the general population, and adverse childhood experiences can exert a negative impact on their clinical course...
October 11, 2018: Pharmacological Reports: PR
Ana Carla A Souza, Fabíula F Abreu, Lúcio R L Diniz, Renata Grespan, Josimari M DeSantana, Lucindo J Quintans-Júnior, Paula P Menezes, Adriano A S Araújo, Cristiane B Correa, Simone A Teixeira, Marcelo N Muscará, Soraia K P Costa, Enilton A Camargo
BACKGROUND: Skeletal muscle inflammation is strongly associated with pain and may impair regeneration and functional recovery after injury. Since anti-inflammatory and antinociceptive effects have been described for the inclusion complex of carvacrol and β-cyclodextrin (βCD-carvacrol), this study investigated the effects of βCD-carvacrol in a model of acute skeletal muscle inflammation. METHODS: Muscle injury was induced in male Wistar rats by injection of 3% carrageenan in the gastrocnemius muscle...
October 11, 2018: Pharmacological Reports: PR
Ewelina Rojewska, Katarzyna Ciapała, Joanna Mika
BACKGROUND: The G protein-coupled receptor 35 (GPR35), is considered important for nociceptive transmission, as suggested by accumulating evidence. This receptor was discovered in 1998; however, a lack of pharmacological tools prevented a complete understanding of its function and how to exploit it therapeutically. We studied the influence of CXCL17, kynurenic acid and zaprinast on nociceptive transmission in naïve and neuropathic mice. Additionally, we investigated the influence of kynurenic acid and zaprinast on morphine effectiveness in neuropathic pain...
October 6, 2018: Pharmacological Reports: PR
Fatemeh Delrobaei, Iman Fatemi, Ali Shamsizadeh, Mohammad Allahtavakoli
BACKGROUND: Menopause is associated with increased oxidative stress and memory impairment. Based on the antioxidant property of ascorbic acid (AA), It's effect on cognitive function, the serum level of the brain-derived neurotrophic factor (BDNF) and the activity of antioxidant enzymes within the brain in ovariectomized (OVX) mice was investigated. METHODS: AA (100, 300 and 500 mg/kg), was orally administrated per day in OVX mice for 30 days. Tactile learning and working memory were evaluated by the novel object recognition task and T-maze continuous alternation task, respectively...
October 3, 2018: Pharmacological Reports: PR
Wojciech Garczorz, Enrique Gallego-Colon, Agnieszka Kosowska, Krzysztof Siemianowicz, Agnieszka Kłych-Ratuszny, Michał Woźniak, Mohammad Reza F Aghdam, Tomasz Francuz, Mariola Dorecka
BACKGROUND: Diabetic retinopathy (DR) is one of the most common complications of diabetes and the leading cause of acquired blindness in adults. In diabetic patients hyperglycemia induces complex metabolic abnormalities affecting retinal homeostasis, and promotes retinal inflammation and angiogenesis. Incretin mimetic drugs such exenatide, are a relatively new group of drugs used in the treatment of diabetes. We investigated the potential direct effects of exenatide on human retinal pigment epithelium (HRPE)...
October 3, 2018: Pharmacological Reports: PR
Lan-Ying Shi, Li Zhang, Hui Li, Tao-Li Liu, Ji-Cai Lai, Zhi-Bing Wu, Jian Qin
BACKGROUND: Aging is one of the most important inevitable risk factors of Alzheimer disease (AD). Oxidative stress plays a critical role in the process of aging. Curcumin has been proposed to improve neural damage, especially neurodegenerative injury, through its antioxidant and anti-inflammatory properties. Therefore, we investigated the effects of curcumin on acrolein-induced AD-like pathologies in HT22 cells. METHODS: HT22 murine hippocampal neuronal cells were treated with 25μM acrolein for 24h with or without pre-treating with curcumin at the selected optimum concentration (5μg/mL) for 30min...
October 2018: Pharmacological Reports: PR
Marta Jóźwiak-Bębenista, Magdalena Jasińska-Stroschein, Edward Kowalczyk
BACKGROUND: Recent evidence suggests that the mitogen activated protein kinase (MAPK)-associated signaling pathway in the frontal cortical areas demonstrates abnormal activity in cases of schizophrenia. Moreover, schizophrenia patients often display alterations in the regional cellular energy metabolism and blood flow of the brain; these are shown to parallel changes in angiogenesis primarily mediated by vascular endothelial growth factor (VEGF). METHODS: The present study examines the differential effects of time-dependent treatment with haloperidol, olanzapine and amisulpride (20μM) on VEGF and MAPK mRNA expression and VEGF level, using the T98 cell line as an example of nerve cells...
October 2018: Pharmacological Reports: PR
Katarzyna Kamińska, Anna Górska, Karolina Noworyta-Sokołowska, Adam Wojtas, Zofia Rogóż, Krystyna Gołembiowska
BACKGROUND: Preclinical and clinical studies have suggested a beneficial effect of combination treatment with atypical antipsychotic drugs and antidepressants (ADs) in schizophrenia and in drug-resistant depression. METHODS: In the present study, we investigated the effect of chronic administration of risperidone and ADs (escitalopram or mirtazapine), given separately or jointly on the extracellular levels of dopamine (DA) and serotonin (5-HT) in the rat frontal cortex...
October 2018: Pharmacological Reports: PR
Sattar Ostadhadi, Saeed Shakiba, Abbas Norouzi-Javidan, Vahid Nikoui, Samira Zolfaghari, Mohsen Chamanara, Ahmad-Reza Dehpour
BACKGROUND: Considering the pivotal role of nitric oxide (NO) pathway in depressive disorders, the aim of the present study was to investigate the antidepressant-like effect of selegiline in mice forced swimming test (FST), and possible involvement of NO-cyclic guanosine monophosphate (cGMP) pathway in this action. METHODS: After assessment of locomotor activity in open-field test, mice were forced to swim individually and the immobility time of the last 4min was evaluated...
October 2018: Pharmacological Reports: PR
Joanna Motyl, Joanna B Strosznajder
Parkinson's disease (PD) is one of the most common serious neurodegenerative disorders in the world. The incidence of PD appears to be growing and this illness has an unknown pathogenesis. PD is characterized by selective loss of dopaminergic (DA) neurons in the substantia nigra (SN), with an enigmatic cause in most individuals. Current pharmacotherapies and surgery provide symptomatic relief but their effects against the progressive degeneration of neuronal cells are strongly limited if present at all. Therefore, uncovering novel molecular mechanisms of DA cell death and new potentially disease-modifying pharmacological targets is an important task for basic research...
October 2018: Pharmacological Reports: PR
Hosein Pasandi, Saman Abbaspoor, Mohammad Naser Shafei, Mahmoud Hosseini, Abolfazl Khajavirad
BACKGROUND: The pedunculopontine tegmental (PPT) nucleus is a heterogeneous nucleus with several functions including cardiovascular regulation. The presence of GABAA receptor has been shown in the PPT. Therefore, the cardiovascular effects of this receptor were examined. METHODS: Rats were divided into: Control; Muscimol; Bicuculline (BMI); Hexamethonium (Hexa)+BMI and Atropine+BMI groups. The femoral vein and artery were cannulated for drug administration and recording of cardiovascular parameters, respectively...
October 2018: Pharmacological Reports: PR
Faisal Imam, Naif O Al-Harbi, Mohammad Matar Al-Harbi, Mushtaq Ahmad Ansari, Abdullah F Al-Asmari, Mohd Nazam Ansari, Wael A Al-Anazi, Saleh Bahashwan, Mashal M Almutairi, Musaad Alshammari, Mohammad Rashid Khan, Abdulaziz Mohammed Alsaad, Moureq Rashed Alotaibi
BACKGROUND: Doxorubicin is an effective, potent and commonly used anthracycline-related anticancer drug; however, cardiotoxicity compromises its therapeutic potential. Apremilast, a novel phosphodiesterase type 4-inhibitor, reported to have anti-inflammatory effects and modulating many inflammatory mediators. METHODS: The present study investigated the influence of apremilast against doxorubicin-induced cardiotoxicity in male Wistar rats. A total, 24 animals were divided into four groups of six animal each...
October 2018: Pharmacological Reports: PR
Ilona Joniec-Maciejak, Adriana Wawer, Danuta Turzyńska, Alicja Sobolewska, Piotr Maciejak, Janusz Szyndler, Dagmara Mirowska-Guzel, Adam Płaźnik
BACKGROUND: Parkinson's disease (PD) is a progressive neurodegenerative process leading to the loss of dopaminergic neurons and their projections. 1-methyl-4-phenol-1,2,5,6-tetrahydropyridine (MPTP) toxicity is a well-recognized animal model of PD. It is suggested that the impairment of mitochondrial function in the substantia nigra plays an important role in both the onset and the progression of PD. Octanoic acid (C8), a fatty acid that is the main constituent of the medium-chain triglyceride ketogenic diet, increases the metabolic activity of mitochondria; hence, it seemed interesting to investigate whether C8 exhibits neuroprotective effects in the MPTP model of PD and whether it affects mitochondria function in the striatum...
October 2018: Pharmacological Reports: PR
Farzaneh Shakeri, Nama Mohamadian Roshan, Mahsa Kaveh, Naeima Eftekhar, Mohammad Hossein Boskabady
BACKGROUND: Curcumin has shown various pharmacological effects such as anti-inflammatory activities. In this study, the effects of curcumin on tracheal responsiveness and lung pathological features were evaluated in a rat model of asthma. METHODS: Tracheal responsiveness and lung pathological features were evaluated in control rats (C), ovalbumin (OVA)-sensitized rats (as an animal model of asthma; A), A rats treated with curcumin (Cu, 0.15, 0.30, and 0.60mg/ml) and dexamethasone (D, 1...
October 2018: Pharmacological Reports: PR
Anna Mróz, Izabela Ryska, Hanna Sominko, Anna Bejrowska, Zofia Mazerska
BACKGROUND: The compound 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes - UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. METHODS: UGT-mediated transformations with rat liver (RLM), human liver (HLM), and human intestine (HIM) microsomes and with 10 recombinant human isoenzymes were investigated...
October 2018: Pharmacological Reports: PR
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