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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
Grzegorz Kreiner
Neurodegenerative diseases are currently a major challenge in elderly care due to demographic changes and dramatic increases in the aging population worldwide. This review is focused on the most promising research discovering ways to attenuate neural loss or enhance neuroprotection and unraveling the basis of neurodegeneration using transgenic mouse models. With the recent introduction of the powerful and relatively simple gene-editing tool CRISPR-Cas9, we have entered a new era in genetic engineering that will certainly lead to a variety of new transgenic models in the near future...
September 16, 2018: Pharmacological Reports: PR
Bartłomiej Rospond, Anna Sadakierska-Chudy, Grzegorz Kazek, Mirosław Krośniak, Beata Bystrowska, Małgorzata Filip
BACKGROUND: Obesity has reached global epidemic proportions and is associated with serious medical comorbidities and economic consequences. In this preclinical study, we characterized how the palatable diet changed food intake pattern, caloric intake, metabolic profile and hormone levels. We also evaluated the expression of dopamine D2 receptors in the rat striatum. METHODS: Male Wistar rats were fed with either high-fat or high-sucrose diet for 5 weeks according to different feeding regimes: ad libitum access or scheduled for a 2-h period each day without caloric restriction during the remainder of the day...
September 10, 2018: Pharmacological Reports: PR
An-Kuo Chou, Chong-Chi Chiu, Yu-Wen Chen, Jhi-Joung Wang, Ching-Hsia Hung
BACKGROUND: Pramoxine has been shown to produce spinal anesthesia, while cutaneous analgesia (peripheral) of pramoxine is not established. The experimental goal was to examine cutaneous antinociception produced by a local anesthetic (LA) pramoxine and compare this result with that of another well-known LA lidocaine. METHODS: Cutaneous antinociception was evaluated by blockade of pinprick- induced cutaneous trunci muscle reflex (CTMR) on the skin of rat's back. After the dose-related curves were constructed, the quality and duration of drug's (lidocaine and pramoxine) cutaneous antinociception were compared...
September 10, 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
Meizhi Wang, Hui Gao, Haijun Qu, Jing Li, Kaili Liu, Zhiwu Han
BACKGROUND: The most frequent type of renal cell carcinoma is called clear-cell renal cell carcinoma (ccRCC) which is associated with a poor prognosis. It has been observed that miR-137 is aberrantly expressed in many different kinds of human malignancies including ccRCC. This research aims to examine the role of miR-137 in ccRCC. METHODS: Quantitative RT-PCR (qRT-PCR) was applied to measure miR-137 expression in ccRCC and adjacent noncancerous tissue. Gene expression was determined by western blot...
October 2018: Pharmacological Reports: PR
Mostafa Mahmoud Hamdy, Mohamed Mostafa Elbadr, Ahmed Barakat
BACKGROUND: Morphine - the main pillar of nociceptive pain management - systemic use is associated with development of tolerance and dependence. Tolerance and dependence lay a heavy burden in clinical pain management settings. An added weight to this dilemma is that effective, safe, and tolerable solution to this problem is still beyond reach. Antidepressants were reported as possible alleviators of opioid tolerance and dependence. One of the increasingly used antidepressant in clinical practice is bupropion given its high safety and tolerability profile...
October 2018: Pharmacological Reports: PR
Agnieszka Matuszewska, Beata Nowak, Diana Jędrzejuk, Marcin Landwójtowicz, Ewa Sadanowicz, Tomasz Sozański, Joanna Kwiatkowska, Małgorzata Pieśniewska, Marek Bolanowski, Adam Szeląg
BACKGROUND: Histamine regulates function of osteoclasts and osteoblasts, however data regarding the influence of histamine H2 receptors antagonists on bone tissue are ambiguous. Factors that influence growing skeleton may have an important impact on the peak bone mass and future risk of fractures. The aim of our study was the assessment of influence of ranitidine, on growing bones. METHODS: The experiment was carried out on young male Wistar rats divided into two groups receiving either ranitidine (10mg/kg ip) or vehicle...
October 2018: Pharmacological Reports: PR
Dasiel O Borroto-Escuela, Alexander O Tarakanov, Ismel Brito, Kjell Fuxe
The existence of mGluR, NMDAR, AMPAR and putative KAR heteroreceptor complexes in synaptic and extrasynaptic regions of brain glutamate synapses represents a major integrative mechanism. Our aim in the current article is to analyze if the formation of the different types glutamate hetereceptor complexes involves the contribution of triplet amino acid homologies (protriplets) in a postulated receptor interface based on the triplet puzzle theory. Seven main sets (lists) of receptor pairs in databases were used containing various sets (lists) of human receptor heteromers and nonheteromers obtained from the available scientific publications including the publically available GPCR-hetnet database...
October 2018: Pharmacological Reports: PR
Ji Won Lim, Ji Hoon Ha, Yoon Ju Jeong, Soo Nam Park
BACKGROUND: In mammals, UV radiation induces melanin synthesis in melanocyte for protecting their skin through the stimulation of α-melanocyte stimulating hormone (α-MSH) from keratinocytes. In this study, the inhibitory effects of dehydroglyasperin C (DGC), an useful component of Glycyrrhiza uralensis (G. uralensis), was investigated on melanogenesis induced by α-melanocyte stimulating hormone (α-MSH) and its mechanisms. METHODS: Melanogenesis suppression effect of DGC on α-MSH induced B16F1 melanoma cells...
October 2018: Pharmacological Reports: PR
Yan Wang, Mengzhen Niu, Sha Yin, Fei Zhang, Ruizan Shi
BACKGROUND: To evaluate the protective effect of nebivolol against kidney damage and elucidate the underlying mechanism in a two-kidney, one-clip (2K1C) rat model. METHODS: 2K1C rats were obtained by clipping left renal artery of male Wistar rats and were considered hypertensive when systolic blood pressure (SBP) was ≥160mmHg 4 weeks after surgery. The 2K1C hypertensive rats were divided into untreated, nebivolol (10mg/kg, ig), and atenolol (80mg/kg, ig) treatment groups...
October 2018: Pharmacological Reports: PR
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