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Naunyn-Schmiedeberg's Archives of Pharmacology

Kensuke Saeki, Shun-Ichi Yasuda, Masami Kato, Mayumi Kano, Yuki Domon, Naohisa Arakawa, Yutaka Kitano
Mirogabalin, a novel ligand for the α2 δ subunit of voltage-gated calcium channels, is under the development for the treatment of neuropathic pain. Mirogabalin specifically and potently binds to α2 δ subunits, and it shows analgesic effects in both peripheral and central neuropathic pain models in rats. To expand pharmacological findings on mirogabalin and provide additional information of its potential for chronic pain therapy, we examined the effects of mirogabalin in 2 experimental models of fibromyalgia, namely, the intermittent cold stress model (ICS model) and the unilateral intramuscular acidic saline injection model (Sluka model)...
February 15, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Martina Fragni, Diego Galli, Marco Nardini, Elisa Rossini, Sara Vezzoli, Matteo Zametta, Francesca Longhena, Arianna Bellucci, Elisa Roca, Maurizio Memo, Alfredo Berruti, Sandra Sigala
To study the capability of the CYP17A1 inhibitor abiraterone acetate (AER) to antagonize the androgen receptor (AR) activation in human prostate cancer (PCa) cell lines. T877A-AR-LNCaP, WT-AR-VCaP, AR-negative DU145, and PC3 PCa cell lines were used by MTT and cell count to study the ability of AER and enzalutamide (ENZ) to modify cell viability. The role of ARs in LNCaP was demonstrated through a gene-silencing experiment. The mechanism of AER cytotoxicity in LNCaP cells was studied, as well as the ability of AER to modulate AR gene expression...
February 15, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Gaopeng Guan, Jun Zhang, Shengyuan Liu, Wenyin Huang, Ying Gong, Xiang Gu
Endoplasmic reticulum (ER) stress-induced apoptosis is a major cause of myocardial ischemia/reperfusion (I/R) injury. Emerging evidence indicates that glucagon-like peptide-1 (GLP-1) has potential cardioprotective effects. However, the precise mechanisms underlying the involvement of GLP-1 in I/R injury remain largely unknown. In the present study, we aimed to determine whether GLP-1 attenuates hypoxia/reoxygenation (H/R) injury in cardiomyocytes and to further elucidate the underlying signaling pathway. The results indicate that GLP-1 reversed the increased apoptotic ratio, the increased lactate dehydrogenase (LDH) levels, the reduced cell viability, the increased Caspase-3 activity, and the increased Bax/Bcl-2 ratio caused by H/R...
February 14, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Samar S Khalaf, Mohamed M Hafez, Eman T Mehanna, Noha M Mesbah, Dina M Abo-Elmatty
There is increasing evidence of a link between type 2 diabetes mellitus (T2DM) and cognitive decline. T2DM has been recognized as a risk factor for Alzheimer's disease (AD). The aim of this research was to investigate the biochemical and physiological effects of vildagliptin treatment alone, and in combination with memantine, in a rat model of combined T2DM and AD. The experimental study was carried out on 75 male Wistar rats weighing 180-200 g. The rats were divided into five groups (n = 15): normal group, Alzheimer diabetic control, treated with vildagliptin (10 mg/kg/day), treated with memantine (30 mg/kg/day), and treated with combination of drugs...
February 13, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Marius Mbiantcha, Rauf Khalid, Amadou Dawe, Arif Mehreen, Donatien Albert Atsamo, Gilbert Ateufack, Dar Hamza, William Yousseu Nana, Francis Tatsinkou Desire Bomba, Rehman Ur Naeem, Ahmad Izhar
Painful diabetic neuropathy (PDN) is known to adversely affect psychosocial functioning by enhancing levels of anxiety and depression. This study was designed to verify the antihypernociceptive, anxiolytic, and antidepressant-like effects of Combretin A and Combretin B (two triterpenes cycloartane-type isolated from the leaves of Combretum fragrans) in streptozotocin-induced diabetic neuropathy in mice. PDN was induced in mice by the administration of streptozotocin (STZ, 200 mg/kg, i.p.). The effect of oral administration of Combretin A (25 and 50 mg/kg) and Combretin B (25 and 50 mg/kg) on nociception (mechanical allodynia, thermal hyperalgesia, cold allodynia, and chemical hyperalgesia), anxiety (elevated plus maze, light-dark box test, social interaction), and depressant (open field test, forced swimming test, tail suspension test) was evaluated...
February 13, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Jolly Mounir William Labib, Sawsan Aboul-Fotouh, Mohamed Z Habib, Mohamed Abd Elrahman Ahmed Mekawy, Kawthar A Farrag, Ahmed M Abdel-Tawab
Depression and cardiovascular disease (CVD) are two faces of one coin. A pro-inflammatory state was previously suggested in the pathology of both diseases. We investigated the effect of chronic administration (2 weeks) of imipramine (20 mg/kg/day) and pentoxifylline (50 mg/kg/day) on behavioral, aortic histological abnormalities, and level of circulating endothelial progenitor cells (CEPCs) in peripheral blood of male Wistar rats exposed to chronic mild stress (CMS) and high-fat diet. Exposure to CMS and high-fat diet induced a depressive-like behavior alongside aortic immunohistochemical changes associated with an increase in aortic TNF-α level...
February 9, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Urmila Aswar, Umesh Mahajan, Amit Kandhare, Manoj Aswar
Ferulic acid (FA) is a phenolic compound with potent antioxidant activity. The objective of the study was to study the protective effects of FA on doxorubicin (Dox)-induced myocardial toxicity in rats. Wistar rats received vehicle (control) or Dox (20 mg/kg, i.p.) or telmisartan (Tel; 10 mg/kg, p.o.) or ferulic acid (20 mg/kg and 40 mg/kg, p.o.) for 7 days followed by treatment with Dox (20) on the fifth day of treatment, except the control group. On day 8, electrocardiographic parameters were recorded followed by blood withdrawal and then the animals were sacrificed for histopathology...
February 8, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Nermin T El-Said, Eman A Mohamed, Ragia A Taha
Doxorubicin (DOX) so far continues to be one of the most potent and effective anticancer drugs. Therefore, it is still needed to search for a safe and effective therapy that can opposite DOX-induced cardiotoxicity. Irbesartan (IRB), an angiotensin II receptor blocker, has a wide-ranging variety of biological activities. The present study was designed to explore the possible protective effects of IRB against DOX-induced cardiotoxicity and the underlying mechanisms. Rats were divided into four groups: control, IRB (40 mg/kg, orally/daily) for 3 weeks, DOX (2...
February 7, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Liu Li, Yi Ji, Junting Fan, Furong Li, Yan Li, Mianhua Wu, Haibo Cheng, Changliang Xu
Inflammation is one of the characteristic features during the development of human tumors. A pro-inflammatory cytokine that is known to promote inflammation during cancer development is the transforming growth factor-β (TGF-β). On the other hand, demethylzeylasteral (T-96) is a natural compound isolated from Tripterygium wilfordii Hook F, which has been reported to have various pharmacological properties including anti-inflammatory and immunosuppressive activities. We investigated the effects of T-96 on the highly metastatic breast cancer cell line, MDA-MB-231...
February 6, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Mohamed G Ewees, Tamer M Abdelghany, Abdel-Aziz H Abdel-Aziz, Mohamed S Abdelbakky
Methotrexate (MTX) is a widely used drug for treatment of many malignant, rheumatic, and autoimmune diseases. However, hepatotoxicity remains one of the most serious side effects of MTX. The extrinsic coagulation pathway is activated after tissue injury through the release of tissue factor (TF) which activates a cascade of clotting factors including prothrombin and fibrinogen. Liver sinusoidal endothelial cells express endothelial nitric oxide synthase (eNOS) as a source for nitric oxide (NO) that serves as vasodilator and antithrombotic factor...
January 28, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Yan Liu, Tingting Bi, Linxun Liu, Quangen Gao, Genhai Shen, Lei Qin
Gemcitabine (GEM) has been widely used for pancreatic cancer (PC) treatment but limited by the development of drug resistance. The agents that reverse its resistance and improve the chemo-sensitivity are urgently needed. S-Adenosylmethionine (SAM) is a precursor for polyamine biosynthesis in mammalian cells and plays a key role in biological transmethylation events. It is reported that SAM could be used as a therapeutic reagent for cancer treatments. In this study, we investigated the chemo-sensitization of SAM to potentiate the antitumor effect of GEM in PC...
January 25, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Wei Feng, Jian Wang, Xin Yan, Cui Zhai, Wenhua Shi, Qingting Wang, Qianqian Zhang, Manxiang Li
It has been demonstrated that activation of autophagy is involved in the development of pulmonary arterial hypertension (PAH). Recent studies have shown that cytosolic forkhead box protein O1 (FoxO1) activates autophagy in cancer cells. Paclitaxel has been found to potentially reverse PAH progression. However, the role of FoxO1 and the effects of paclitaxel on autophagy in the pathogenesis of PAH remain unknown. PAH was generated by intraperitoneal injection of monocrotaline (MCT) to rats. The right ventricular systolic pressure (RVSP), the right ventricle hypertrophy index (RV/LV+S), and the percentage of medial wall thickness (%MT) were used to detect the development of PAH...
January 25, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Davoud Sanajou, Saeed Nazari Soltan Ahmad, Vahid Hosseini, Ashkan Kalantary-Charvadeh, Yasser Marandi, Leila Roshangar, Saman Bahrambeigi, Mehran Mesgari-Abbasi
β-Lapachone (B-LAP) is a natural naphtaquinone with established anti-oxidative stress and anti-cancer activities. We aimed to investigate B-LAP protective potential against doxorubicin (DOX)-induced nephrotoxicity in mice. The mice received an oral dose of B-LAP followed by a single intraperitoneal injection of 20 mg/kg DOX a day later. They were then treated for 4 days with 1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg doses of B-LAP. Renal levels of NAD+ /NADH ratios, p-AMPKα, p-NF-κB p65, inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6) along with renal expressions of TNF-α, IL-1β, and IL-6 were examined...
January 23, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Samira Khabbazi, Mohammadhossein Hassanshahi, Alireza Hassanshahi, Yaser Peymanfar, Yu-Wen Su, Cory J Xian
Opioids are widely administered to alleviate pain, including chronic pain in advanced cancer patients. Among opioids, morphine is one of the most clinically effective drugs for the palliative management of severe pain. In the last few decades, there has been a debate around the possible influence of opioids such as morphine on tumour growth and metastasis. Whilst several in vitro and in vivo studies suggest the possible modulatory effects of morphine on tumour cells, little is known about the impact of this analgesic drug on other mediators such as matrix metalloproteinases (MMPs) that play a key role in the control of cancer cell invasion and metastasis...
January 17, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Hou Tingting, Liu Guangzhong, Zang Yanxiang, Yu DongDong, Sun Li, Weimin Li
Qiliqiangxin (QL) can attenuate myocardial remodeling and improve cardiac function in some cardiac diseases, including heart failure and hypertension. This study was to explore the effects and mechanism of QL on atrial structural remodeling in atrial fibrillation (AF). Twenty-one rabbits were randomly divided into a sham-operation group, pacing group (pacing with 600 beats per minute for 4 weeks), and treatment group (2.5 g/kg/day). Before pacing, the rabbits received QL-administered p.o. for 1 week. We measured atrial electrophysiological parameters in all groups to evaluate AF inducibility and the atrial effective refractory period (AERP)...
January 9, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Zípora Morgana Quinteiro Dos Santos, Marlene Quinteiro Dos Santos, Vilmair Zancanaro, Emyr Hiago Bellaver, Geisson Marcos Nardi, Jane Mary Lafayet Gelinski, Claudriana Locatelli
Acne vulgaris (AV), a severe chronic inflammatory dermatosis, commonly treated with systemic or topical antibiotics that exacerbate bacterial resistance and pose adverse side effects, new approaches for suppressing or reducing Propionibacterium acnes-induced inflammatory responses and thereby treating AV remain necessary. In response, the goal of our study was to investigate the therapeutic potential of phenolic compounds in the in vivo inflammatory process induced by P. acnes. Mice were intradermally challenged with a suspension containing 1...
January 7, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Gessica Brum Milani, Camila Camponogara, Mariana Piana, Cássia Regina Silva, Sara Marchesan Oliveira
To investigate the topical anti-inflammatory activity of the crude extract of Cariniana domestica fruit peels (CdE), its dichloromethane, n-butanol, and ethyl acetate (EtAc) fractions, and steroids (β-sitosterol, lupeol, and stigmasterol) isolated from the EtAc fraction in models of irritant contact dermatitis (ICD) croton oil-induced in mice. We induced skin inflammation by single (acute; 1 mg/ear) and multiple (chronic; 0.4 mg/ear) croton oil application. We topically applied C. domestica (CdE, fractions, and gel formulations) and β-sitosterol, lupeol, and stigmasterol immediately after applying croton oil...
January 7, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Stéphani Batista de Oliveira, Erika Ivanna Araya, Eder Gambeta, Luiz Eduardo Nunes Ferreira, Michele Franz-Montan, Rafaela Franco Claudino, Juliana Geremias Chichorro
Herein, it was investigated whether a complex of lidocaine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) would present a better antinociceptive profile in vivo when compared with plain lidocaine in models of orofacial pain. Plain lidocaine (LDC) and complexed lidocaine (LDC:HP-β-CD) were initially evaluated in vitro to determine the release rate of the two formulations. Subsequently, the effect of both formulations was evaluated in independent groups of rats submitted to the orofacial formalin test, induction of facial heat hyperalgesia by capsaicin and carrageenan, and induction of facial heat and mechanical hyperalgesia by constriction of the infraorbital nerve...
January 6, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Cem Yucel, Elcin Erdogan Yucel, Fatma Demet Arslan, Sumeyye Ekmekci, Erdem Kisa, Volkan Ulker, Murat Ucar, Yusuf Ozlem Ilbey, Orcun Celik, Banu Isbilen Basok, Zafer Kozacioglu
The aim of this study is to investigate the effects of all-trans retinoic acid (ATRA) use on cisplatin (CP)-induced nephrotoxicty. Twenty-eight rats were randomly divided into four groups. The rats in the control group were injected a single dose of 1 ml/kg saline intra-peritoneally (IP) during 10 days. The rats in the ATRA group were injected a single dose of ATRA during 10 days. The rats in the ATRA+CP group were injected a single dose of CP on the fourth day of the 10 days of ATRA treatment. The rats in the CP group were injected a single dose of CP on the fourth day of 10 days without administering a treatment...
January 4, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
Sunanda Panda, Rajesh Sharma, Anand Kar
Thyrotoxicosis is a clinical syndrome that commonly results from excess secretion and/or release of thyroid hormones in the circulation. It affects most of the body systems and if not treated properly may lead to serious health problems. In this investigation, we isolated a phenolic compound, chavibetol (CHV) from Piper betel leaf and evaluated its possible ameliorative effects in thyrotoxicosis of rats. Adult female rats were rendered thyrotoxic by the administration of L-thyroxine (L-T4 ) at 500 μg/kg/day, i...
January 4, 2019: Naunyn-Schmiedeberg's Archives of Pharmacology
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