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Naunyn-Schmiedeberg's Archives of Pharmacology

Atilla Topcu, Filiz Mercantepe, Sema Rakici, Levent Tumkaya, Huseyin Avni Uydu, Tolga Mercantepe
According to data issued by the International Agency for Research on Cancer in 2012, the estimated number of new cases of all types of cancer worldwide was estimated to exceed 10 million, and 6 million of whom receive radiotherapy. Radiotherapy is the treatment of cancer using ionizing radiation. Our study investigated the effects of x-radiation resulting from radiotherapy (RT) on the testis at the molecular level, and prospectively considered the potential protective characteristics of antioxidants against testicular damage resulting from x-radiation...
November 13, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Hichem Moulahoum, Belkacem Mohamed Amine Boumaza, Meriem Ferrat, Abdelkader Bounaama, Bahia Djerdjouri
Arsenic trioxide (As2 O3 ) is a trending subject in recent therapy approaches despite its described toxicity. In this work, we have investigated the use of arsenic trioxide in a murine model of chemically induced inflammatory bowel disease "colitis." Male mice were randomly separated into four different groups. Controls received vehicle, arsenic group had a daily injection of As2 O3 (2.5 mg/kg, i.p.) for 2 days. Colitis was induced through intra-rectal instillation of 4% (v/v) solution of acetic acid in the second day...
November 10, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Xiangli Meng, Yuxiang Yuan, Fengjuan Shen, Chengqiu Li
Cardiomyocyte infarction could lead to high morbidity and mortality worldwide. Recent studies demonstrated that Heme oxygenase-1 (HO-1) could exert cardiac protective effect and arouse attention. However, the detailed mechanism is still unclear. Our study provided evidences of the protective effect of HO-1 overexpression on cardiomyocytes against hypoxia/reoxygenation (H/R). We divided the treatment into four groups: the control group, H/R group, H/R+HO-1 group, and H/R+Null group. Immunofluorescent study was utilized to label the BrdU-positive and LC3-positive cells...
November 10, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Izabela Zakrocka, Katarzyna M Targowska-Duda, Artur Wnorowski, Tomasz Kocki, Krzysztof Jóźwiak, Waldemar A Turski
Glutamate (GLU) mainly through N-methyl-D-aspartate (NMDA) receptors plays pivotal role in kidney function regulation. Kynurenic acid (KYNA), a GLU receptors antagonist, is synthesized from kynurenine by kynurenine aminotransferases (KATs). Previously, it was shown that angiotensin II type 1 receptor blockers (ARBs) decrease KYNA production in rat brain in vitro. The aim of this study was to examine the influence of six ARBs: candesartan, irbesartan, losartan, olmesartan, telmisartan, and valsartan on KYNA production on rat kidney in vitro...
October 29, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Katharina Olbrisch, Tobias Kisch, Julia Thern, Evelyn Kramme, Jan Rupp, Tobias Graf, Sebastian G Wicha, Peter Mailänder, Walter Raasch
Infections are a major problem in patients with burn diseases. Mortality is high despite antibiotic therapy as studies are controversial concerning drug underdosing. The aims of this prospective, observational study were to monitor plasma concentrations of piperacillin during standard piperacillin/tazobactam treatment in 20 burn patients and 16 controls from the intensive care unit (ICU) and to optimize doses by in silico analyses. Piperacillin/tazobactam (4/0.5 g, tid) was administered over 0.5 h. Blood samples were taken at 1, 4, and 7...
October 27, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Elif Cadirci, Rustem Anil Ugan, Busra Dincer, Betul Gundogdu, Irfan Cinar, Erol Akpinar, Zekai Halici
Sepsis is a life-threatening organ dysfunction condition response resulting in acute lung injury. Urotensin II (UII), an endogenous vasoactive peptide, is widely distributed in pulmonary, cardiovascular, central nervous, renal and metabolic systems, and especially in inflammatory regions. This study aimed to investigate whether urotensin II (UII) and UII receptor (UTR) antagonists play a role in the inflammatory response to sepsis-induced lung damage and they are possible therapeutic targets. In the study, 78 male Balb-c mice were used...
October 24, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Tolulope Eniola Omolekulo, Olugbenga Samuel Michael, Lawrence Aderemi Olatunji
Combined oral contraceptive (COC) treatment has been shown to be associated with glucose deregulation and increased triglyceride levels, but the mechanisms are elusive. Soluble dipeptidyl peptidase-4 (sDPP-4) and adenosine deaminase (ADA) are involved in the initiation and/or progression of cardiometabolic disorders. We therefore, hypothesized that increased DPP-4 and ADA activities are involved in glucose deregulation and hepatic triglyceride accumulation induced by COC treatment. This study also investigated whether short-chain fatty acid, acetate, would protect against COC-induced dysmetabolic effects...
October 2, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Kehinde Samuel Olaniyi, Lawrence Aderemi Olatunji
Fructose (FRU) intake has increased dramatically in recent decades with a corresponding increased incidence of insulin resistance (IR), particularly in young adults. The use of oral ethinylestradiol-levonorgestrel (EEL) formulation is also common among young women worldwide. The present study aimed at determining the effect of EEL on high fructose-induced cardiac triglyceride (TG) and glycogen accumulation. The study also investigated the possible involvement of pyruvate dehydrogenase kinase-4 (PDK-4) in EEL and/or high fructose metabolic effects on the heart...
October 1, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Lina Jin, Xue Fu, Shuangshuang Yao, Jian Yang, Guang Ning, Zhiguo Zhang
The purpose of this study was to explore the protective effect of protopanaxatriol (PPT) on acute liver injury induced by concanavalin A (ConA). In this study, mice were randomly separated into four groups. The first group received PBS (i.v.). The second group was given PPT (50 mg/kg body weight, i.p.) for 3 days before PBS (i.v.) injection. The third group received ConA (15 mg/kg body weight, i.v.). The fourth group was administered PPT (50 mg/kg body weight, i.p.) for 3 days before ConA (i.v.) injection...
September 30, 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
Max Kenedy Felix Dos Santos, Elaine C Gavioli, Lorena Santa Rosa, Vanessa de Paula Soares-Rachetti, Bruno Lobão-Soares
Caffeine is the most consumed psychoactive substance in the world; in general, it is not associated to potentially harmful effects. Nevertheless, few studies were performed attempting to investigate the caffeine addiction. The present review was mainly aimed to answer the following question: is caffeine an abuse drug? To adress this point, the effects of caffeine in preclinical and clinical studies were summarized and critically analyzed taking account the abuse disorders described in the Diagnostic and Statistical Manual of Mental Disorders (DSM-V)...
December 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...
December 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...
December 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)...
December 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...
December 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
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