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Naunyn-Schmiedeberg's Archives of Pharmacology

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https://www.readbyqxmd.com/read/28785775/t3-peptide-a-fragment-of-tumstatin-stimulates-proliferation-and-migration-of-cardiac-fibroblasts-through-activation-of-akt-signaling-pathway
#1
Jumpei Yasuda, Kana Fukui, Muneyoshi Okada, Hideyuki Yamawaki
Proliferation and migration of cardiac fibroblasts are important in early stage of wound-healing after myocardial infarction. The effects of tumstatin, a cleaved fragment of collagen type IV α3 chain, on these functions of cardiac fibroblasts have not been clarified. In this study, we examined it by using T3 peptide, an active fragment of tumstatin. Cardiac fibroblasts were isolated from ventricles of adult male Wistar rats. Proliferation was examined by a cell counting assay. Boyden chamber assay was performed to examine migration...
August 7, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28780600/the-anti-influenza-drug-oseltamivir-reduces-atrial-fibrillation-in-an-experimental-whole-heart-model
#2
Gerrit Frommeyer, André Mittelstedt, Julian Wolfes, Christian Ellermann, Simon Kochhäuser, Patrick Leitz, Dirk G Dechering, Lars Eckardt
Recent experimental studies suggested direct effects of the anti-influenza drug oseltamivir on cardiac electrophysiology. We therefore aimed at analyzing potential antiarrhythmic effects of oseltamivir on atrial fibrillation (AF) in an experimental whole-heart model. Twelve rabbit hearts were isolated and Langendorff perfused. Thereafter, hearts were paced at cycle lengths of 350, 250, and 200 ms in the atrium. A standardized protocol employing atrial burst pacing induced AF in 4 of 12 hearts under baseline conditions (33%, 11 episodes)...
August 6, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28780599/liraglutide-ameliorates-cardiotoxicity-induced-by-doxorubicin-in-rats-through-the-akt-gsk-3%C3%AE-signaling-pathway
#3
Noha A T Abbas, Soad L Kabil
Doxorubicin (Dox)-induced cardiotoxicity constitutes the major adverse effect that limited its use. We investigated the possible protective effects of liraglutide on Dox-induced cardiotoxicity in rats. Rats were divided into the following groups: control group rats received normal saline [1 ml/kg, intraperitoneal (i.p.)]; doxorubicin group rats received doxorubicin (1.25 mg/kg, i.p.), four times per week for 4 weeks; and liraglutide group rats received doxorubicin (1.25 mg/kg, i.p.) four times per week for 4 weeks then received liraglutide (100 μg/kg, i...
August 5, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28779210/a-marginal-anticancer-effect-of-regorafenib-on-pancreatic-carcinoma-cells-in-vitro-ex-vivo-and-in-vivo
#4
Barbara Mayer, Svetlana Karakhanova, Nathalie Bauer, Li Liu, Yifan Zhu, Pavel P Philippov, Jens Werner, Alexandr V Bazhin
Activation of receptor tyrosine kinases is recognized as a hallmark of cancer. Vascular endothelial growth factor (VEGF) and its receptor VEGFR are the prominent players in the induction of tumor neoangiogenesis. Strategies to inhibit VEGF and VEGFR are under intensive investigation in preclinical and clinical settings. Regorafenib is a multikinase inhibitor targeting some VEGFR and other receptor kinases. Preclinical results led to the FDA approval of regorafenib for treatment of metastatic colorectal cancer patients...
August 4, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28761978/propolis-alleviates-concanavalin-a-induced-hepatitis-by-modulating-cytokine-secretion-and-inhibition-of-reactive-oxygen-species
#5
Fatma Mounieb, Laila Ramadan, El-Sayed Akool, Amany Balah
Viral hepatitis-induced oxidative stress accompanied by increased levels of transforming growth factor-β (TGF-β) and hepatic fibrosis are hallmarks of hepatitis C virus infection. The present study was designed to investigate the potential protective effect of propolis against liver injury induced by concanavalin A (Con A), a T-cell-dependent model that causes an immune-mediated hepatitis in a similar pattern to the one induced by viral infections. In the present study, rats were randomly divided into four groups...
July 31, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28761977/calcineurin-inhibitors-regulate-fibroblast-growth-factor-23-fgf23-synthesis
#6
Ludmilla Bär, Claudia Großmann, Michael Gekle, Michael Föller
Fibroblast growth factor 23 (FGF23) inhibits renal phosphate reabsorption and calcitriol formation, effects depending on Klotho as a co-receptor for FGF23. In addition, FGF23/Klotho strongly influences aging and the onset of age-associated diseases. The synthesis of FGF23 by bone cells is induced by store-operated Ca(2+) entry (SOCE) through Orai1 in UMR106 osteoblast-like cells. Ca(2+) entry activates the phosphatase calcineurin in many cell types which dephosphorylates nuclear factor of activated T cells (NFAT) thereby stimulating its transcriptional activity...
July 31, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28756460/ursolic-acid-activates-the-tgr5-receptor-to-enhance-glp-1-secretion-in-type-1-like-diabetic-rats
#7
Shih-Hsiang Lo, Yingxiao Li, Kai Chun Cheng, Chiang-Shan Niu, Juei-Tang Cheng, Ho-Shan Niu
Endogenous Takeda G-protein-coupled receptor 5 (TGR5), G-protein-coupled bile acid receptor 1 (GPBAR1), regulates glucose metabolism. In animals, TGR5 activation by a chemical agonist may increase incretin secretion and reduce the blood sugar level. Recently, betulinic acid has been suggested to activate TGR5. Ursolic acid is a well-known pentacyclic triterpenoid that is similar to betulinic acid. It is of special interest to determine the potential effect of ursolic acid on TGR5. Therefore, we transfected cultured Chinese hamster ovary (CHO-K1) cells with the TGR5 gene...
July 30, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28733880/effect-of-asiatic-acid-on-the-ang-ii-at1r-nadph-oxidase-nf-%C3%AE%C2%BAb-pathway-in-renovascular-hypertensive-rats
#8
Putcharawipa Maneesai, Sarawoot Bunbupha, Upa Kukongviriyapan, Laddawan Senggunprai, Veerapol Kukongviriyapan, Parichat Prachaney, Poungrat Pakdeechote
Asiatic acid, a triterpenoid compound derived from Centella asiatica, has been demonstrated to have antioxidant and anti-inflammatory effects. The present study evaluated the effects of asiatic acid on hemodynamic alterations, renin-angiotensin system (RAS), oxidative stress, and inflammation in 2K-1C hypertensive rats. Renovascular hypertension was induced in male Sprague-Dawley rats and treated with vehicle, asiatic acid (30 mg/kg/day), or captopril (5 mg/kg/day) for 4 weeks. We observed that 2K-1C hypertensive rats exhibited hemodynamic alterations such as high blood pressure, heart rate, hindlimb vascular resistance, and low hindlimb blood flow...
July 21, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28733879/anticancer-activity-of-salicin-and-fenofibrate
#9
Marwa Sabaa, Hassan M ELFayoumi, Shimaa Elshazly, Mahmoud Youns, Waleed Barakat
Cancer refers to a disorder of cell proliferation that leads to tumor production. Cancer is usually treated by surgery, chemotherapeutic drugs, and radiation. Despite the presence of many anticancer drugs, cancer is still an uncontrolled disease and is a major cause of death worldwide. In addition, most anticancer drugs have severe side effects that can limit their use in some patients. This study aims to investigate the possible anticancer activity of two clinically used drugs: a natural antioxidant agent (salicin) and an antihyperlipidemic agent (fenofibrate) against two breast cancer models (in vivo EAC and in vitro MCF7) and the pancreatic cancer cell line (Panc-1)...
July 21, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28730281/pk-pd-studies-on-non-selective-pde-inhibitors-in-rats-using-camp-as-a-marker-of-pharmacological-response
#10
Artur Świerczek, Elżbieta Wyska, Sebastian Baś, Marta Woyciechowska, Jacek Mlynarski
In recent years, phosphodiesterase (PDE) inhibitors have been frequently tested for the treatment of experimental inflammatory and immune disorders. It is suggested that anti-inflammatory properties of PDE inhibitors are related to their ability to increase cAMP levels. The aim of this study was to verify the hypothesis that cAMP may be a useful marker of pharmacological response following administration of non-selective PDE inhibitors (pentoxifylline and (±)-lisofylline) to endotoxemic rats. Male Wistar rats were administered LPS (1 mg kg(-1), i...
July 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28730280/evidence-for-the-involvement-of-the-gabaergic-but-not-serotonergic-transmission-in-the-anxiolytic-like-effect-of-bisabolol-in-the-mouse-elevated-plus-maze
#11
Mohaddeseh Abouhosseini Tabari, Mohammad Amir Bagherpour Tehrani
Bisabolol (α-(-)-bisabolol) is a sesquiterpene which is a part of the essential oil of a variety of plants, but its common source is German chamomile. Several bioactivities including anti-inflammatory, anti-nociceptive, and anti-tumor effects were attributed to bisabolol. However, the neuropharmacological properties of bisabolol have not yet been reported. The present study evaluated behavioral effects of bisabolol using elevated plus maze (EPM), open field test (OFT), and rotarod test. Moreover, this study also examined whether the 5-HT1A and GABAA-benzodiazepine receptor systems are involved in the anxiolytic-like effects of bisabolol...
July 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28717838/the-triterpenoid-alpha-beta-amyrin-prevents-the-impaired-aortic-vascular-reactivity-in-high-fat-diet-induced-obese-mice
#12
Flávia Almeida Santos, Karine Maria Martins Bezerra Carvalho, Francisco José Batista-Lima, Paulo Iury Gomes Nunes, Ana Flávia Seraine Custódio Viana, Armenio André de Carvalho Almeida da Silva, Said Gonçalves da Cruz Fonseca, Mariana Helena Chaves, Vietla Satyanarayana Rao, Pedro Jorge Caldas Magalhães, Teresinha Silva de Brito
To characterize the protective effects of the triterpenoid mixture alpha, beta-amyrin (AMY, 20 mg/kg, during 15 days) on the reactivity of isolated aorta of high-fat diet (HFD)-induced obese mice. Male Swiss mice were fed with HFD or normal diet (ND) for 15 weeks. Contractions of thoracic aorta in response to KCl or phenylephrine (PHE) and relaxation by acetylcholine (ACh) or sodium nitroprusside (SNP) were analyzed. HFD-fed mice developed hyperglycemia, hyperlipidemia, and significant body weight gain, parameters prevented by AMY treatment...
July 17, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28710683/highly-selective-cb2-receptor-agonist-a836339-has-gastroprotective-effect-on-experimentally-induced-gastric-ulcers-in-mice
#13
M Salaga, H Zatorski, M Zielińska, P Mosinska, J-P Timmermans, R Kordek, M Storr, J Fichna
Cannabinoid type 2 (CB2) receptors are distributed in central and peripheral tissues, including immunocytes and the gastrointestinal (GI) tract, suggesting that CB2 receptor agonists represent potential therapeutics in GI inflammatory states. In this study, we investigated the effect of highly selective CB2 agonist, A836339, on the development of gastric lesions. We used two models of gastric ulcer (GU) induced by ethanol (EtOH) and diclofenac. To confirm the involvement of CB2 receptors, a selective CB2 antagonist, AM630 was used...
July 14, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28698893/cytotoxicity-against-tumor-cell-lines-and-anti-inflammatory-properties-of-chitinases-from-calotropis-procera-latex
#14
Carolina Araújo Viana, Márcio V Ramos, José Delano Barreto Marinho Filho, Letícia Veras Costa Lotufo, Ingrid Samantha Tavares Figueiredo, Jefferson Soares de Oliveira, Pietro Mastroeni, José Vitor Lima-Filho, Nylane Maria Nunes Alencar
The role of chitinases from the latex of medicinal shrub Calotropis procera on viability of tumor cell lines and inflammation was investigated. Soluble latex proteins were fractionated in a CM Sepharose Fast-Flow Column and the major peak (LPp1) subjected to ion exchange chromatography using a Mono-Q column coupled to an FPLC system. In a first series of experiments, immortalized macrophages were cultured with LPp1 for 24 h. Then, cytotoxicity of chitinase isoforms (LPp1-P1 to P6) was evaluated against HCT-116 (colon carcinoma), OVCAR-8 (ovarian carcinoma), and SF-295 (glioblastoma) tumor cell lines in 96-well plates...
July 11, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28689255/identification-of-morin-as-an-agonist-of-imidazoline-i-3-receptor-for-insulin-secretion-in-diabetic-rats
#15
Mang Hung Lin, Chia-Chen Hsu, Jenshinn Lin, Juei-Tang Cheng, Ming Chang Wu
Morin is a flavonoid contained in guava that is known to reduce hyperglycemia in diabetics. Morin has been demonstrated to increase plasma insulin. However, the mechanism(s) remains unknown. The present study is designed to investigate the effect of morin on the imidazoline receptor (I-R) that regulates insulin secretion. We used Chinese hamster ovary (CHO) cells transfected with an I-R expression construct (NISCH-CHO-K1 cells) to identify the direct effect of morin on the I-R. Moreover, the imidazoline I3 receptor (I-3R) is known to be present in pancreatic β cells and involved in insulin secretion...
July 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28689254/desensitization-of-the-human-5-ht4-receptor-in-isolated-atria-of-transgenic-mice
#16
Ulrich Gergs, Julia Fritsche, Stephanie Fabian, Josepha Christ, Joachim Neumann
In the human cardiovascular system, serotonin (5-HT) exerts positive inotropic and chronotropic effects mediated by 5-HT4 receptors. Moreover, 5-HT4 receptor stimulation can cause arrhythmias in the human heart. Response to 5-HT can fade due to desensitization of the receptor system and/or activation of phosphodiesterases. In this study, we investigated a potential desensitization of the human 5-HT4(a) receptor expressed in the mouse heart. Therefore, we have used atrial preparations of transgenic (TG) mice with cardiac myocyte-specific overexpression of the human 5-HT4(a) receptor and their non-transgenic littermates (WT)...
July 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28689253/effect-of-arteether-and-pyrimethamine-coadministration-on-the-pharmacokinetic-and-pharmacodynamic-profile-of-ormeloxifene
#17
Abhisheak Sharma, Swati Jaiswal, Mahendra Shukla, Jawahar Lal
The study was intended to investigate the effect of concomitant administration of antimalarial drug (pyrimethamine or arteether) on pharmacokinetic and post coitus contraceptive efficacy of ormeloxifene in female Sprague-Dawley rats. A serial sampling technique coupled with LC-MS/MS detection was utilized for quantification of ormeloxifene in plasma samples collected from female rats treated with ormeloxifene only and ormeloxifene with pyrimethamine or arteether. Coitus-proven female rats were utilized to investigate the effect of pyrimethamine or arteether coadministration on contraceptive efficacy of ormeloxifene by investigating the presence or absence of implantations and status of corpora lutea on day 10 post coitum...
July 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28687854/neuroprotective-effects-of-vitamin-d-alone-or-in-combination-with-lamotrigine-against-lithium-pilocarpine-model-of-status-epilepticus-in-rats
#18
Amal M Mahfoz, Ali F Abdel-Wahab, Mohamed A Afify, Naiyer Shahzad, Ibrahim A A Ibrahim, Naser A ElSawy, Ghazi A Bamagous, Saeed S Al Ghamdi
Status epilepticus (SE) is considered one of the major serious forms of epilepsy with high mortality rate. Since the currently available antiepileptic drugs have low efficacy and high adverse effects, new more efficient and safe therapies are critically needed. There is increasing evidence supporting dietary and alternative therapies for epilepsy, including the ketogenic diet, modified Atkins diet, and omega-3 fatty acids. Recent studies have shown significant prophylactic and therapeutic potential of vitamin D (vit-D) use in many neurological disorders...
July 7, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28685234/prostanoid-ep3-receptor-agonist-sulprostone-enhances-pacemaker-activity-of-colonic-interstitial-cells-of-cajal
#19
Man Woo Kim, Han Yi Jiao, Seok Won Kim, Chan Guk Park, Mei Jin Wu, Chansik Hong, Seok Choi, Jae Yeoul Jun
EP receptor activation by PGE2 regulates gastrointestinal motility by modulating smooth muscle contractility. Interstitial cells of Cajal (ICCs) are pacemaker cells that regulate smooth muscle activity. We aimed to determine effects of the EP3 receptor agonist sulprostone on pacemaker potentials in colonic ICCs. We performed a whole cell patch clamp, RT-PCR, and Ca(2+) imaging in cultured ICCs from mouse colon. Sulprostone depolarized the membrane and increased pacemaker frequency. EP3 receptor antagonist blocked these sulprostone-induced effects...
July 6, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28669009/neuroprotective-effects-of-at1-receptor-antagonists-after-experimental-ischemic-stroke-what-is-important
#20
Juraj Culman, Toni Jacob, Sven O Schuster, Kjell Brolund-Spaether, Leonie Brolund, Ingolf Cascorbi, Yi Zhao, Peter Gohlke
The present study conducted in rats defines the requirements for neuroprotective effects of systemically administered AT1 receptor blockers (ARBs) in acute ischaemic stroke. The inhibition of central effects to angiotensin II (ANG II) after intravenous (i.v.) treatment with candesartan (0.3 and 3 mg/kg) or irbesartan and losartan (3 and 30 mg/kg) was employed to study the penetration of these ARBs across the blood-brain barrier. Verapamil and probenecid were used to assess the role of the transporters, P-glycoprotein and the multidrug resistance-related protein 2, in the entry of losartan and irbesartan into the brain...
July 2, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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