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Pharmacological Reports: PR

Maksym V Kopanitsa, Gemma Gou, Nurudeen O Afinowi, Àlex Bayés, Seth G N Grant, Noboru H Komiyama
BACKGROUND: Synaptic Ras-GTPase-activating protein 1 (SYNGAP1) is an abundant brain-specific protein localized at the postsynaptic density of mammalian excitatory synapses. SYNGAP1 functions as a crucial regulator of downstream intracellular signaling triggered by N-methyl-d-aspartate receptor activation. One of the most important signaling pathways regulated by SYNGAP1 is the Ras-Raf-MEK-ERK pathway. SYNGAP1 deficiency is associated with hyperphosphorylation of MEK and ERK kinases and with altered synaptic function in Syngap1+/- mice...
June 22, 2018: Pharmacological Reports: PR
Sayed Aliul Hasan Abdi, Mohd Amir Afjal, Abul Kalam Najmi, Sheikh Raisuddin
BACKGROUND: The aim of this study was to evaluate the modulatory effect of S-allyl cysteine against cyclophosphamide-induced changes in uroplakin IIIa, CCL11 and TNF-α. METHODS: Mice were treated with cyclophosphamide (200 mg/kg × 7 d, ip). S-allyl cysteine (150 mg/kg × 7d, ip), and comparator compound mesna (40 mg/kg × 7d, ip) were administered 1 h before and 4 h after each cyclophosphamide dose. The urinary bladder was analysed for mRNA and protein changes in uroplakin IIIa, CCL11 and TNF-α and histopathological findings...
June 21, 2018: Pharmacological Reports: PR
Bożena Gabryel, Anna Bielecka, Jacek Bernacki, Krzysztof Łabuzek, Zbigniew S Herman
No abstract text is available yet for this article.
June 14, 2018: Pharmacological Reports: PR
Anil Kumar, Ruchika Mittal
Studies demonstrates the major involvement of inflammatory and apoptotic pathway in the pathophysiology of diabetic nephropathy. The cross talk between inflammatory and apoptotic pathway suggests Txnip as a molecular connexion in progression of disease state. Txnip modulates inflammatory pathway (via ROS production and NLRP3 inflammasome activity) and apoptotic pathway (via mTOR pathway). The key contribution of Txnip in both the pathways, reflects, its crucial role in diabetic nephropathy. In the present review, we have first provided an overview of diabetic nephropathy and Txnip system, followed by the mechanistic insight of Txnip in the progression of diabetic nephropathy...
June 2018: Pharmacological Reports: PR
Juan Du, Wenpeng Dong, Huifeng Li, Bo Li, Xiaodan Liu, Qinghui Kong, Wei Sun, Tingli Sun, Peilong Ma, Yan Cui, Ping Kang
BACKGROUND: Development of novel therapeutic strategies that specifically target diabetic kidney disease (DKD) is urgently needed. METHODS: Male KKAy mice were divided randomly into three equal groups - KK, KI, and KF; Male C57BL/6 mice were the control group. All KKAy mice were fed a high-fat diet. From the 16th week, the KI group was given IFN-γ, and the KF group was assigned to be treated with fludarabine. C57BL/6 mice were always fed a normal mouse diet. Every 4 weeks, body weight, random blood sugar, urine albumin and urea of all mice were measured...
June 2018: Pharmacological Reports: PR
Iwona Kamińska, Julia K Bar
BACKGROUND: The association between p53 protein phosphorylated at serine 15 (Ser15), serine 20 (Ser20) and ovarian tumor cell sensitivity after chemotherapy was analyzed in order to define the influence of p53 activation on tumor cell sensitivity to chemotherapy. METHODS: The study was performed on ovarian cancer cell line (OvBH-1), colon adenocarcinoma metastasis to ovary (SW626) and on cells isolated from ascitic fluids from patients with ovarian cancer: with (p53+) or without (p53-) p53 nuclear protein accumulation...
June 2018: Pharmacological Reports: PR
Meysam Amidfar, Yong-Ku Kim, Ove Wiborg
BACKGROUND: Previous clinical and preclinical studies have indicated that the N-methyl-d-aspartate (NMDA) receptor antagonist, memantine, has neuroprotective properties as well as antidepressant effects. The present study was designed to examine behavioral and molecular effects of memantine administration in rats subjected to the repeated unpredictable stress (RUS) paradigm. METHODS: Rats were split into four groups at random including control+saline, control+memantine, stressed+saline and stressed+memantine...
June 2018: Pharmacological Reports: PR
Monu Yadav, Milind Parle, Deepak Kumar Jindal, Sameer Dhingra
BACKGROUND: Stigmasterol, a naturally occurring phytoestrogen has been reported to possess many pharmacological activities. The aim of the present study was to screen the effect of stigmasterol against ketamine-induced mice model of psychosis. METHODS: The behavioural studies included an assessment of locomotor activity, stereotypic behaviours, immobility duration, step down latency and effects on catalepsy. Biochemical estimations involved the estimations of GABA, dopamine, GSH, MDA, TNF-α, total protein content and AChE activity...
June 2018: Pharmacological Reports: PR
Zülbiye Yılmaz, Esra Betül Kalaz, A Fatih Aydın, Vakur Olgaç, Semra Doğru-Abbasoğlu, Müjdat Uysal, Necla Koçak-Toker
BACKGROUND: Methylglyoxal (MG) is a highly reactive dicarbonyl compound. It is produced by processes like glycolysis, glucose autooxidation, lipid peroxidation, and protein glycation. It is a major precursor of advanced glycation end products (AGE). It also exacerbates oxidative stress in the organism. Although there are some in vitro studies investigating the effect of resveratrol (RES) as an antioxidant and antiglycating agent on MG-induced toxicity, in vivo effect of RES is unknown...
June 2018: Pharmacological Reports: PR
Mina Taati, Esmaeal Tamaddonfard
BACKGROUND: Oxytocin plays an important role in supraspinal modulation of pain. In the present study, we investigated the effects of ventrolateral orbital cortex (VLOC) microinjection of oxytocin on neuropathic pain after blockade of opioid receptors in this area and ventrolateral periaqueductal gray (vlPAG). METHODS: Neuropathic pain was induced by complete transcection of preoneal and tibial branches of sciatic nerve. The VLOC and vlPAG were unilaterally (contralateral to the sciatic nerve-injured side) and bilaterally implanted with guide cannulas, respectively...
June 2018: Pharmacological Reports: PR
Ching-Hsia Hung, Ja-Ping Shieh, Chong-Chi Chiu, Jhi-Joung Wang, Yu-Wen Chen
BACKGROUND: We aimed to evaluate the effect of doxylamine, a first generation antihistamine, as a local analgesic agent by comparing its effect to bupivacaine. METHODS: After blocking the cutaneous trunci muscle reflex (CTMR) by subcutaneous injection of doxylamine, we assessed doxylamine's cutaneous analgesic effect in rats. The dose-related effect and duration of doxylamine on infiltrative cutaneous analgesia were compared with that of bupivacaine. RESULTS: We demonstrated that doxylamine, as well as the local anesthetic bupivacaine produced the cutaneous analgesic effects in a dose-related fashion...
June 2018: Pharmacological Reports: PR
Li Tang, Jie-Ran Luo, Dai-Tian Li, Rui Ge, Yun-Long Ma, Fei Xu, Tai-Gang Liang, Shu-Rong Ban, Qing-Shan Li
BACKGROUND: Great attention has been paid to the development of novel anti-inflammatory drugs to overcome the adverse reactions of traditional drugs. Recently, a new compound 4-o-methyl-benzenesulfonyl benzoxazolone (MBB) we have prepared attracted our attention for its promising anti-inflammatory activity and low toxicity. The present study aimed to further investigate the anti-inflammatory effects of MBB both in vivo and in vitro in order to determine its potential as a novel NSAIDs lead compound...
June 2018: 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...
June 2018: Pharmacological Reports: PR
Madhu Kaundal, Rahul Deshmukh, Mohd Akhtar
BACKGROUND: The purpose of the study was to explore the therapeutic potential of Betulinic acid (BA) in streptozotocin (STZ) induced memory damage in experimental rats. METHODS: STZ (3mg/kg bilaterally) as intracerebroventrical (icv) route was administered on day 1 and 3 in rats. Donepezil (5mg/kg/day po), used as standard, and BA (5, 10 and 15mg/kg/day po) were administered after 1h of 1st STZ infusion up to 21days. Object recognition task (ORT) for non-spatial, Morris water maze (MWM) for spatial and locomotor activity were performed to evaluate behavioral changes in rats...
June 2018: Pharmacological Reports: PR
Ewa A Ogłodek, Marek J Just, Anna D Grzesińska, Aleksander Araszkiewicz, Adam R Szromek
Patients with schizophrenia are predisposed toward developing cardiovascular disease. Although neuroleptics affect the cardiovascular system, it is also important to consider the consequences of the disease itself such as lower physical activity due to living on disability pension, inadequate nutrition, and/or nicotine addiction, being more common among patients with schizophrenia versus the general population. All these factors combined lead to an increased risk of death caused by cardiovascular conditions in schizophrenic patients...
June 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
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