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Naunyn-Schmiedeberg's Archives of Pharmacology

David Brinkman, Jiang H Wang, Henry P Redmond
Morphine has been used in the treatment of pain for centuries. It is commonly used by oncology in terminal cancer cases and by surgery perioperatively for oncology surgery. Its extra-analgesic effects on cancer have been described extensively but conflicting results abound. It has been shown to have varying effects on tumour progression, cell proliferation, tumour invasion, angiogenesis, immune function, and metastatic potential. In vivo studies on the effects of morphine and the mu-opioid receptor on tumours are discussed below...
September 20, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Nadezhda Levanova, Marcus Steinemann, Kira E Böhmer, Silvia Schneider, Yury Belyi, Andreas Schlosser, Klaus Aktories, Thomas Jank
Legionella pneumophila glucosyltransferase SetA, which is introduced into target cells by a type IV secretion system, affects the intracellular traffic of host cells. Here, we characterized the enzyme activity of the Legionella effector. We report that Asp118 and Arg121 of SetA are essential for glucohydrolase and glucotransferase activities. Exchange of Trp36 to alanine reduced the enzyme activity of SetA. All three amino acids were crucial for the cytotoxic effects of SetA in yeast. We observed that phosphatidylinositol-3-phosphate (PI3P) increased the glucosyltransferase activity of SetA severalfold, while the glucohydrolase activity was not affected...
September 17, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Aline Stamford S G Gatis-Carrazzoni, Fernanda Virgínia Barreto Mota, Tonny Cley Campos Leite, Tatiane Bezerra de Oliveira, Sandra Cabral da Silva, Isla Vanessa Alves Bastos, Maria Bernadete de Souza Maia, Pedro Silvino Pereira, Pedro Paulo Marcelino Neto, Earl Celestino de Oliveira Chagas, Tania Maria Sarmento Silva, Márcia Silva do Nascimento, Teresinha Gonçalves da Silva
Some species of the genus Miconia are used in Brazilian folk medicine as analgesic and anti-inflammatory; however, several species of this genus are still poorly studied. Therefore, the aims of this study were to investigate the phytochemistry characterization by UPLC-DAD-QTOF-MS/MS, acute toxicity, anti-inflammatory and antinociceptive properties of Miconia minutiflora (Bonpl.) DC. The methanol extract of M. minutiflora (Mm-MeOH) was subjected to ultra-high-performance liquid chromatography (UPLC-DAD-QTOF-MS/MS) for the identification of the main phytocompounds...
September 13, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Aly M Abdelrahman, Yousuf Al Suleimani, Asem Shalaby, Mohammed Ashique, Priyadarsini Manoj, Abderrahim Nemmar, Badreldin H Ali
Canagliflozin is a sodium glucose co-transporter 2 (SGLT2) inhibitor that is currently available for the management of type 2 diabetes mellitus. The present study investigated the effect of canagliflozin on cisplatin (CP)-induced nephrotoxicity in mice. The animals were divided into four groups (n = 6). The first and second groups received normal saline (control) and intraperitoneal (i.p.) cisplatin (20 mg/kg) on day 7, respectively. The third and fourth groups were given a single intraperitoneal (i.p...
September 11, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Enas S Nabih, Omnyah A El-Kharashi
Many pathways are involved in the association between biliary obstruction and liver injury. We investigated the intervention influence and effect of rosuvastatin (Rvs) on the high mobility group protein 1 (HMGB1)/toll-like receptor-4 (TLR4) axis and microRNA-21 (miR-21) in cholestatic liver injury. This model was performed by ligating common bile duct of Wistar rats. Saline and Rvs were orally administrated by gastric gavages. Liver and blood samples were collected and subjected to molecular and biochemical evaluation...
September 10, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Wencke Johannsen, Bernhard Frings, Stefan Herzig, Jan Matthes
Medical students' prescribing competencies are insufficient. So far, surveys focused on final-year students. Knowledge and confidence seem important, but their development during medical studies are unclear. This study investigated whether students perceived deficits in pharmacological knowledge change during medical studies. Alumni were included to look for changes occurring after graduation. Medical students at different stages of their studies were invited to fill in paper-and-pencil (6th-, 8th-, 9th- and 10th-term students) or online questionnaires (final-year students and alumni) regarding their self-assessed deficits in pharmacology...
September 7, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Feng Zhou, Fang Rao, You-Qing Deng, Hui Yang, Su-Juan Kuang, Fei-Long Wu, Shu-Lin Wu, Yu-Mei Xue, Xiao-Mu Wu, Chun-Yu Deng
Statins are widely used in the treatment of hypercholesterolemia. Studies have demonstrated that statins could maintain vascular contractile function through inhibiting the transformation of vascular smooth muscle cells (VSMCs) from the contractile phenotype to the synthetic phenotype. However, the underlying mechanisms have not been fully elucidated. The effect of atorvastatin on the thoracic aorta of Sprague-Dawley rats cultured in serum-free conditions in vitro was evaluated. Aortic constriction was induced by high potassium, phenylephrine, and CaCl2 ...
September 4, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Monira M Rageh, Reem H El-Gebaly, Marwa M Afifi
Silver nanoparticles (AgNPs) have a wide range of industrial and biomedical applications. The aim of the present study was to determine the cytotoxic and genotoxic effects of AgNPs on Ehrlich carcinoma-bearing mice. AgNPs were characterized by ultraviolet-visible absorption spectroscopy, dynamic light scattering, and transmission electron microscopy (TEM). Furthermore, the cytotoxicity and genotoxicity of AgNPs were evaluated using a series of assays: superoxide dismutase (SOD) enzyme activity, malondialdehyde (MDA) levels, DNA damage (comet assay), and histopathological examination of tissues and tumor size in Ehrlich carcinoma-bearing mice...
September 3, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Pengyu Zhang, Jixia Wang, Ying Zhao, Xiuli Zhang, Lala Qu, Chaoran Wang, Jiatao Feng, Anhui Wang, Weijia Zhou, Yanfang Liu, Tao Hou, Han Zhou, Zhiwei Wang, Xinmiao Liang
Label-free cell phenotypic assays were performed to establish a β2 -adrenoceptor (β2 -AR) target model in A431 cells and a β1 -AR target model in transfected HEK293-β1 cells, using known β2 -AR and β1 -AR agonists and antagonists. A list of natural compounds was screened on the target models, among which seven new compounds were found to be antagonistically active against β2 -AR. After receptor specificity evaluations on hydroxyl carboxylic acid receptor-2 (ΗΧΑ-2), histamine receptor (H1 R), and β1 -adrenoceptor (β1 -AR), six out of the seven compounds, including nuciferine, epiberberine, harmaline, harmine, palmatine, and columbamine, exhibited specific antagonistic activity against β2 -AR...
August 28, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Fatma M Abdallah, Maged W Helmy, Mohamed A Katary, Asser I Ghoneim
Hepatocellular carcinoma (HCC) is still a leading cancer killer in the community. Molecular targeted therapy with celecoxib (CXB) has shown promising antitumor effects; however, its use may be limited due to serious side effects. Curcumin (CUR) has also shown beneficial effects against HCC. Then, it was aimed to investigate the effects of adding CUR to CXB on HCC HepG2 cells. HepG2 cells were treated with CXB and/or CUR at increasing concentrations to investigate synergistic drug interactions, as calculated combination index (CI)...
August 28, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Maristella Adami, Cristina Micheloni, Daniela Grandi, Holger Stark
The anti-inflammatory effects of histamine H4 receptor (H4R) antagonists opened new therapeutic options for the treatment of inflammatory/allergic diseases, but the role of H4R in inflammation is far from being solved. Aim of the present study was to investigate the role of structurally related H4R ligands of the aminopyrimidine class with different efficacies and functionalities (neutral antagonist ST-994, partial agonist ST-1006, inverse agonist ST-1012, and partial inverse agonist ST-1124) on croton oil-induced ear edema and pruritus in mice...
August 25, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Yun Zhang, Song Zhang, Zonghong Liu, Xinbo Zhao, Yue Yuan, Li Sheng, Yue Li
Rheumatoid arthritis (RA) causes atrial remodeling that induces the occurrence and maintenance of atrial fibrillation (AF). In this study, we explored the influence of RA on atrial fibrillation and the potential therapeutic effects of resveratrol in a rat model. The following three groups of female Wistar rats (8 weeks old) were used in this study: control, collagen-induced arthritis (CIA), and resveratrol. Rats in the CIA and resveratrol groups were injected twice with type II collagen in Freund's incomplete adjuvant...
August 22, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Xiuli Fang, Yajun Liu, Jing Lu, Huiqi Hong, Jing Yuan, Yuhong Zhang, Panxia Wang, Peiqing Liu, Jiantao Ye
Protocatechuic aldehyde (PCA) is a natural compound found in the Chinese herb Salvia miltiorrhiza. It has been shown to possess multiple biological activities and to protect the cardiovascular system against oxidative stress, inflammation, and atherosclerosis. However, the potential effects of PCA on cardiac hypertrophy remain to be investigated. In this study, we showed that isoproterenol treatment (ISO, 10 μM for 24 h) induced significant hypertrophy in cultured neonatal rat cardiomyocytes, as manifested by enlargement of cell surface area (1...
August 21, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Aleksandra Szopa, Ewa Poleszak, Karolina Bogatko, Elżbieta Wyska, Sylwia Wośko, Urszula Doboszewska, Katarzyna Świąder, Aleksandra Wlaź, Jarosław Dudka, Andrzej Wróbel, Piotr Wlaź, Anna Serefko
The main goal of the present study was to evaluate the influence of the adenosine A1 receptor (A1R) antagonist - DPCPX - on depressive-like behavior in mice, as well as the effect of DPCPX on the activity of imipramine, escitalopram, and reboxetine, each at non-effective doses. The influence of DPCPX on behavior and its influence on the activity of selected antidepressants was evaluated in the forced swim test (FST) and the tail suspension test (TST) in mice. Locomotor activity was measured to verify and exclude false-positive data obtained in the FST and TST...
August 9, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Noha A T Abbas, Amal El Salem, Mohammed M Awad
Chronic kidney disease (CKD) is a global healthcare problem; however until now, there is no effective treatment that can stop its progression. In this study, we aimed to investigate the effect of empagliflozin, a sodium-glucose linked transporter-2 inhibitor (SGLT2 I) in a model of unilateral ureteric obstruction (UUO) in rats, as a model of progressive renal interstitial fibrosis in vivo and the possibility of inclusion of klotho protein. Rats were randomly divided into five groups: group 1: control group, group 2: UUO untreated group, group 3: prophylactic SGLT2 I treatment before UUO, group 4: immediate SGLT2 I treatment after UUO, and group 5: delayed SGLT2 I treatment (this group received distilled water 1 week after UUO then empagliflozin for 2 weeks)...
August 8, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Adjia Hamadjida, Stephen G Nuara, Dominique Bédard, Imane Frouni, Cynthia Kwan, Jim C Gourdon, Philippe Huot
Nefazodone is an anti-depressant that interacts with a wealth of pharmacological targets, including some that may exert anti-dyskinetic and anti-psychotic effects in Parkinson's disease (PD), notably serotonin 1A and 2A receptors. In this study, we sought to determine the effect of nefazodone on L-3,4-dihydroxyphenylalanine (L-DOPA)-induced dyskinesia and psychosis-like behaviours (PLBs) in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned primate. Six common marmosets developed parkinsonism following administration of MPTP, after which they were treated chronically with L-DOPA to induce stable dyskinesia and PLBs...
August 7, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Hebatalla I Ahmed, Somaia A Abdel-Sattar, Heba S Zaky
There are increasing evidences supporting the involvement of oxidative stress and neuroinflammation in schizophrenia. Vinpocetine, a nootropic phosphodiesterase-1 inhibitor, was proven to possess anti-oxidant and anti-inflammatory potentials. This research aimed to reveal the likely protective features of vinpocetine against ketamine-induced schizophrenia-like deficits in rats. Additionally, the probable mechanisms contributing to this neuroprotection were also elucidated. Vinpocetine was given (20 mg/kg, i...
August 6, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Kazuhiko Mizukami, Hiroaki Kamada, Hiroyuki Yoshida, Ikuko Ishii, Eisuke Nozawa, Koichi Wada, Tohru Ugawa
We determined the pharmacologic profile of ASP7657, trans-4-[({[1-(quinolin-2-ylmethyl)-5-(trifluoromethyl)-1H-indol-7 yl] carbonyl} amino) methyl] cyclohexanecarboxylic acid methanesulfonate (1:1), a newly synthesized selective E-type prostaglandin (EP)4 receptor antagonist using several in vitro and in vivo experiments. ASP7657 exhibited high affinity for rat and human EP4 receptors, with Ki values of 6.02 nM and 2.21 nM, respectively. In addition, ASP7657 potently inhibited the PGE2 -induced cyclic adenosine monophosphate (cAMP) increase in Chinese hamster ovary (CHO) cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0...
August 3, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Ting Li, Ke Xu, Delu Che, Zhuangzhuang Huang, Nabila Jahan, Sicen Wang
This study was designed to investigate the vasorelaxant effects and underlying mechanism of isocorynoxeine (ICN), one of the indole alkaloids from Uncaria hooks, on isolated mesenteric arteries in vitro. The myograph system was applied for isometric tension recording in the vascular rings. ICN relaxed both endothelium-intact and endothelium-denuded rat vascular rings precontracted with phenylephrine or KCl in a dose-dependent manner. Propranolol, tetraethylammonium, BaCl2 , and glibenclamide had no influence on the vasodilator effect of ICN on phenylephrine-primed vascular rings, while 4-aminopyridine decreased the maximum relaxation...
August 2, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Nihan Çarçak, Melis Yavuz, Tuğba Eryiğit Karamahmutoğlu, Akif Hakan Kurt, Meral Urhan Küçük, Filiz Yılmaz Onat, Kansu Büyükafsar
Rho/Rho-kinase (ROCK) signaling contributes to neuroinflammation, epileptogenesis, and seizures in convulsive-type epilepsies. However, this pathway has not been investigated in absence epilepsy. We investigated RhoA activity in genetic absence epilepsy rats from Strasburg (GAERS) and the effects of ROCK inhibitors Y-27632 and fasudil on spike-and-wave discharges (SWDs) of GAERS. ROCK level and activity were measured by Western blot analysis in the brain areas involved in absence seizures (i.e., cortex and thalamus) and hippocampus...
August 2, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
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