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Pharmacological Reports: PR

Anita K Bakrania, Bhavesh C Variya, Snehal S Patel
BACKGROUND: Angiogenesis, the physiological process involving growth of new blood vessels from preexisting vessels, is essential for organ growth and repair. However, the imbalance in angiogenesis contributes to copious pathologies including cancer. Preceding the development of anti-angiogenic or proangiogenic agents, its evaluation is equally imperative; hence, precise and adequate models required. Valid mammalian models are expensive, time-consuming and not easy to set up, instigating legal and ethical aspects making it necessary to establish models with satisfactory activity and limited drawbacks...
April 17, 2018: Pharmacological Reports: PR
José Luis Cortes-Altamirano, Samuel Reyes-Long, Adriana Olmos-Hernández, Herlinda Bonilla-Jaime, Paul Carrillo-Mora, Cindy Bandala, Alfonso Alfaro-Rodriguez
BACKGROUND: Levetiracetam (LEV) is a novel anticonvulsant with proven antinociceptive properties. However, the antinociceptive and pronociceptive effect of this drug has not yet been fully elucidated in a tonic pain model. METHODS: Thirty-six male rats (Wistar) were randomized into six groups and underwent the formalin test as follows: rats in the control group were administered 50μL of 1% formalin in the paw; sham-group rats were administered 50μL of saline in the paw to mimick the application of formalin; the four experimental groups were administered LEV intragastrically (ig) (50, 100, 200 and 300mg/kg), and 40min later 50μL of 1% formalin was injected in the paw...
April 2018: Pharmacological Reports: PR
Magdalena A Zabielska, Jan Adamus, Robert Kowalski, Jerzy Gebicki, Ewa M Slominska, Zain Khalpey, Ryszard T Smolenski
BACKGROUND: Pyruvate improves contractility of normal, hypoxic, and post-ischemic myocardium. However, sodium overload is a major problem with its therapeutic application if sodium pyruvate is used. Development of alternative forms such as N-1-methylnicotinamide (MNA) pyruvate may help to overcome this problem. The aim of the study was to investigate the effect of MNA pyruvate in a murine model of cardiac ischemia. METHODS: Seven month old male ApoE-/- LDLr-/- mice that develop myocardial infarction when exposed to hypoxic stress, were used in this study...
April 2018: Pharmacological Reports: PR
Amrita A Chowdhury, Nitin B Gawali, Vipin D Bulani, Pankaj S Kothavade, Snehal N Mestry, Padmini S Deshpande, Archana R Juvekar
BACKGROUND: Alzheimer's disease (AD) is characterized by amyloid beta (Aβ) plaques, neurofibrillary tangles (NFTs) and cognitive impairment. Literature cites the role of advanced glycation end products (AGEs) in AD due to increased cytotoxicity via oxidative stress. d-galactose (d-gal) induced amnesia stimulates Aβ overproduction via increased oxidative stress and AGEs. Trigonelline (TRG), a naturally occurring alkaloid has been reported to have neuroprotective and antidiabetic properties...
April 2018: Pharmacological Reports: PR
Clarissa Vasconcelos de Oliveira, Viviane Nogueira Zorzi, Michele Rechia Fighera, Luiz Fernando Freire Royes, Ana Flávia Furian, Mauro Schneider Oliveira
BACKGROUND: The process by which a brain insult elicits epilepsy is termed epileptogenesis and it is characterized by numerous molecular and functional alterations. Statins are first-line drugs for hypercholesterolemia and related diseases, and display neuroprotective properties in clinical and experimental studies. Considering the importance in developing therapeutic strategies to prevent or modify epileptogenesis, we aimed the present study to test the hypothesis that atorvastatin modifies seizure susceptibility of mice after status epilepticus (SE)...
April 2018: Pharmacological Reports: PR
JinHong Jiang, WeiDong Jin, YaLi Peng, XueYa Liang, Shu Li, LiJuan Wei, ZhiPing Lei, LongFei Li, Min Chang
BACKGROUND: This study aimed to investigate the functional roles of Cortistatin-14 (CST-14) in the gastrointestinal (GI) motility. METHODS: For in vivo study, mice were randomly divided into control, ip injected CST-14 (0.1, 0.5, 1, 5, 10mg/kg)+control group, icv injected CST-14 (5μg)+control group, dextran sulfate sodium-induced colitis group, CST-14+colitis group, castor oil-induced diarrhea group, CST-14+diarrhea group. We carried out these experiments by quantitative real-time PCR, GI transit, bead expulsion and fecal pellet output...
April 2018: Pharmacological Reports: PR
Akiyoshi Saitoh, Hiromu Tominaga, Yasuhiro Ogawa, Yoko Irukayama-Tomobe, Mitsuhiko Yamada, Masashi Yanagisawa, Hiroshi Nagase
BACKGROUND: We previously reported that the novel selective delta opioid receptor (DOP) agonist KNT-127 did not cause convulsions in mice, whereas the prototype DOP agonist SNC80 did. Previous studies have reported that SNC80 caused electroencephalographic (EEG) disturbances in rodents. However, whether KNT-127 affects EEG responses is unknown. Therefore, the present study aimed to compare the effect of KNT-127 on EEG responses with that of SNC80 in mice. METHODS: For behavioral experiments, male C57BL6/J mice were injected intraperitoneally with either KNT-127 (30 mg/kg) or SNC80 (30 mg/kg) and monitored for convulsions and subsequent catalepsy-like behavior for 10 min immediately after drug treatment...
April 2018: Pharmacological Reports: PR
Michał Seweryn Karbownik, Paweł Gunerka, Paweł Turowski, Maciej Wieczorek, Edward Kowalczyk, Wojciech Łężak, Tadeusz Pietras
BACKGROUND: Catalytic subunit delta of phosphoinositide 3-kinase, p110δ, encoded by the PIK3CD gene, was recently proposed as a target for pharmacological treatment of schizophrenia. Current antipsychotic drugs were found to decrease the mRNA expression of PIK3CD, but the mechanism of this process is not known. The aim of the study was to elucidate the mechanism by which antipsychotic drugs affect the mRNA expression of PIK3CD. METHODS: The direct effect of haloperidol, clozapine, olanzapine, quetiapine and amisulpride on p110δ enzymatic activity was tested with a kinase assay, and the results were referenced against data on the mRNA expression of PIK3CD...
April 2018: Pharmacological Reports: PR
Aysu Hayriye Tezcan, Omur Ozturk, Sefer Ustebay, Yasemen Adali, Hatice Yagmurdur
BACKGROUND: The aim of the present study was to determine the therapeutic effects of medical ozone therapy on acute acetaminophen (APAP)-induced hepatotoxicity which were not clearly demonstrated in prior studies. METHOD: Twenty-four mice were randomly assigned into three equal groups: Group 1 (control), Group 2 (APAP) and Group 3 (APAP +ozone). Hepatotoxicity was induced by APAP given as a single dose of 300mg/kg intraperitoneally in Groups 2 and 3. Additionally, Group 3 received 20mcg/0...
April 2018: Pharmacological Reports: PR
Alina Sesarman, Lucia Tefas, Bianca Sylvester, Emilia Licarete, Valentin Rauca, Lavinia Luput, Laura Patras, Manuela Banciu, Alina Porfire
BACKGROUND: Emerging treatment options for colon cancer are needed to overcome the limitations regarding the side effects of current chemotherapeutics and drug resistance. The goal of this study was to assess the antitumor actions of PEGylated long-circulating liposomes (LCL) co-delivering curcumin (CURC) and doxorubicin (DOX) on murine colon carcinoma cells (C26). METHODS: The cytotoxicity of CURC and DOX, administered alone or in combination, either in free or LCL form, was evaluated with regard to antiproliferative effects on C26 cells and to protumor processes that might be affected...
April 2018: Pharmacological Reports: PR
Katarzyna Głombik, Aneta Stachowicz, Ewa Trojan, Joanna Ślusarczyk, Maciej Suski, Katarzyna Chamera, Katarzyna Kotarska, Rafał Olszanecki, Agnieszka Basta-Kaim
BACKGROUND: Alteration in the brain mitochondrial functions have been suggested to participate, as a relevant factor, in the development of mental disorders. Therefore, the brain mitochondria may be a crucial therapeutic target in the course of depression. METHODS: Our goal was to find out the impact of two antidepressant drugs with various mechanisms of action - imipramine and fluoxetine, on the frontal cortex mitochondria-enriched fraction in an animal model of depression based on the prenatal stress procedure...
April 2018: Pharmacological Reports: PR
Haydee Izurieta Munoz, Eric B Gonzales, Nathalie Sumien
BACKGROUND: The objective of this study was to evaluate creatine as an anti-nociceptive compound in an animal model of thermal and inflammatory pain. Creatine has the structural potential to interact with acid-sensing ion channels (ASIC), which have been involved in pain sensation modulation. The hypothesis evaluated in this study was that creatine will interact with ASICs leading to decreased nociception. METHODS: Male and female C57BL/6J mice were fed with either a control diet or the control diet supplemented with creatine (6...
April 2018: Pharmacological Reports: PR
Nathani Minaz, Rema Razdan, Lokesh Pathak
BACKGROUND: Well known risk factors for diabetic erectile dysfunction include impaired nitric oxide synthesis and endothelial dysfunction. We proposed to evaluate the efficacy of nitric oxide donor, molsidomine in rat model of diabetic erectile dysfunction. METHODS: Streptozotocin (52mg/kg, ip) induced diabetic male rats were treated with molsidomine (5 and 10mg/kg, po) for 8 weeks. The sexual behaviour of male rat in presence of the female rat in oestrous phase was observed at the end of study...
April 2018: Pharmacological Reports: PR
Rowaida Refaat, Dalia Sarhan, Metwali Kotb, Eman El-Abd, Emad El-Bassiouni
BACKGROUND: The present study aimed to investigate the possible post-irradiation protective effects of ectoine on CNS and testes of male mice. METHODS: The study included thirty male Swiss albino mice (20-22 gm). Mice were divided into five groups (six each); controls (injected intraperitoneally with 0.2ml saline), irradiated group 1 (received six Gy whole body x-irradiation single dose, injected with saline, and sacrificed after one day), irradiated group 2 (x-irradiated, injected with saline, and sacrificed after one week), ectoine group 1 (x-irradiated, injected with 200mg/kg ectoine, and sacrificed after one day), and ectoine group 2 (x-irradiated, injected daily with 200mg/kg ectoine, and sacrificed after one week)...
April 2018: Pharmacological Reports: PR
Paulino Barragán-Iglesias, Víctor Hugo Oidor-Chan, Emanuel Loeza-Alcocer, Jorge Baruch Pineda-Farias, Isabel Velazquez-Lagunas, Ana Belen Salinas-Abarca, Enrique Hong, Alicia Sánchez-Mendoza, Rodolfo Delgado-Lezama, Theodore J Price, Vinicio Granados-Soto
BACKGROUND: The purpose of this study was to evaluate the participation of satellite glial cells (SGC), microglia and astrocytes in a model of streptozotocin-induced diabetes initiated in neonatal rats (nSTZ) and to determine the pharmacological profile for pain relief. METHODS: nSTZ was used to induce experimental diabetes. Von Frey filaments were used to assess tactile allodynia. Drugs were given by systemic administration. Western blotting and immunohistochemistry were used to determine protein expression and cellular localization...
April 2018: Pharmacological Reports: PR
Krzysztof Łukawski, Marta Andres-Mach, Mirosław Czuczwar, Jarogniew J Łuszczki, Krzysztof Kruszyński, Stanisław J Czuczwar
The prevalence of epilepsy is estimated 5-10 per 1000 population and around 70% of patients with epilepsy can be sufficiently controlled by antiepileptic drugs (AEDs). Epileptogenesis is the process responsible for converting normal into an epileptic brain and mechanisms responsible include among others: inflammation, neurodegeneration, neurogenesis, neural reorganization and plasticity. Some AEDs may be antiepileptiogenic (diazepam, eslicarbazepine) but the correlation between neuroprotection and inhibition of epileptogenesis is not evident...
April 2018: Pharmacological Reports: PR
Patrycja Nowicka-Stążka, Ewa Langner, Waldemar Turski, Wojciech Rzeski, Jolanta Parada-Turska
BACKGROUND: Previously, we have demonstrated that kynurenic acid (KYNA), an endogenous metabolite of tryptophan formed along kynurenine pathway, is present in synovial fluid of rheumatoid arthritis (RA) and osteoarthritis (OA) patients. In this study, the goal was to investigate the presence of quinaldic acid (QUDA), a putative metabolite of KYNA, in synovial fluid of RA and OA patients. METHODS: The effect of QUDA on proliferation and motility of synovial fibroblasts and its interaction with KYNA were determined in vitro...
April 2018: Pharmacological Reports: PR
Jun Yin, Leixiang Han, Wei Cong
BACKGROUND: Long term use of glucocorticoids is one of the most common causes of secondary osteoporosis. Osteocyte, the most abundant cell type in bone, coordinates the function of osteoblast and osteoclast. This study evaluates the protective effect of alpinumisoflavone (AIF), a naturally occurring flavonoid compound, on dexamethasone (Dex)-induced apoptosis of osteocytes. METHODS: MLO-Y4 cell was used as a cell model. The effect of AIF on the cell viability was assessed by MTT assay...
April 2018: Pharmacological Reports: PR
Tsugunobu Andoh, Sikai Li, Daisuke Uta
BACKGROUND: Atopic dermatitis is a chronic and severe pruritic skin disease. Interlukin-31 (IL-31) has been recently demonstrated to be one of the key pruritogens in atopic dermatitis. However, the mechanisms underlying IL-31-induced itching remains unclear. In our previous study, we have shown that thromboxane (TX) A2 is involved in itch-associated responses in mice with atopy-like skin diseases. METHODS: IL-31 was given intradermally into the rostral back of ICR mice and the hind-paw scratching to the injection site were counted...
April 2018: Pharmacological Reports: PR
Ártur Krumberg Schüller, Diego Antonio Mena Canata, Fernanda Schäfer Hackenhaar, Vanessa Krüger Engers, Fernanda Maciel Heemann, Jordana Salete Putti, Tiago Boeira Salomon, Mara Silveira Benfato
BACKGROUND: Bilateral ovariectomy is an experimental model used to analyse the effects of menopause and develop strategies to mitigate the deleterious effects of this condition. Supplementation of the diet with antioxidants has been used to reduce potential oxidative stress caused by menopause. The purpose of the study was to analyse the effects of α-lipoic acid (LA), docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), dietary supplementation on oxidative stress in the livers of ovariectomized rats...
April 2018: Pharmacological Reports: PR
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