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Naunyn-Schmiedeberg's Archives of Pharmacology

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https://www.readbyqxmd.com/read/28717838/the-triterpenoid-alpha-beta-amyrin-prevents-the-impaired-aortic-vascular-reactivity-in-high-fat-diet-induced-obese-mice
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
https://www.readbyqxmd.com/read/28660304/differences-in-the-renal-antifibrotic-cgmp-cgki-dependent-signaling-of-serelaxin-zaprinast-and-their-combination
#10
Veronika Wetzl, Elisabeth Schinner, Frieder Kees, Lothar Faerber, Jens Schlossmann
Renal fibrosis is an important factor for end-stage renal failure. However, only few therapeutic options for its treatment are established. Zaprinast, a phosphodiesterase 5 inhibitor, and serelaxin, the recombinant form of the naturally occurring hormone relaxin, are differently acting modulators of cyclic guanosine monophosphate (cGMP) signaling. Both agents enhance cGMP availability in kidney tissue. These substances alone or in combination might interfere with the development of kidney fibrosis. Therefore, we compared the effects of combination therapy with the effects of monotherapy on renal fibrosis...
June 28, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28656320/rho-kinase-and-the-nitric-oxide-pathway-modulate-basilar-arterial-reactivity-to-acetylcholine-and-angiotensin-ii-in-streptozotocin-induced-diabetic-mice
#11
Md Zahorul Islam, Cuong Van Dao, Atsushi Miyamoto, Mitsuya Shiraishi
Diabetes mellitus comprises a heterogeneous group of metabolic disorders with underlying hyperglycemia and secondary cardiovascular complications. Growing evidence suggests that vascular dysfunction is among the most important causes of diabetic cardiovascular disease. Therefore, we determined whether streptozotocin (STZ)-induced diabetes in mice affects blood pressure and cerebral arterial responsiveness to angiotensin (Ang) II and acetylcholine (ACh), which are important modulators of cerebrovascular autoregulation...
June 27, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28646254/cytoprotective-effects-of-diallyl-trisulfide-against-valproate-induced-hepatotoxicity-new-anticonvulsant-strategy
#12
Ahmed A Shaaban, Dina S El-Agamy
Sodium valproate (VP) is an important antiepileptic drug, although it can produce deleterious hepatotoxic reactions. Diallyl trisulfide (DATS) is the principle component of garlic oil that possesses antioxidant properties. This study explored the potential hepatoprotective activity of DATS against VP-induced hepatic damage and its underlying mechanisms. In addition, the study assessed the effect of DATS on VP antiepileptic activity. Rats were given DATS once daily at two different doses along with VP for 2 weeks...
June 23, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28643087/antioxidant-and-antiapoptotic-actions-of-selegiline-protect-against-3-np-induced-neurotoxicity-in-rats
#13
Sara A Wahdan, Mariane G Tadros, Amani E Khalifa
The present study was designed to investigate the neuroprotective effect of selegiline on 3-nitropropionic acid (3-NP)-induced neurotoxicity. Selegiline was intraperitoneally injected at doses 2.5, 5, and 10 mg/kg, 3 days prior to and continued daily, 30 min before 3-NP administration. 3-NP (20 mg/kg, i.p.) was administered for four consecutive days. 3-NP-treated rats exhibited PPI deficits, locomotor hypoactivity, increased striatal and cortical lipid peroxidation, and reduced respective glutathione (GSH) levels as well as catalase and superoxide dismutase (SOD) activities...
June 23, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28643086/gallic-and-ellagic-acids-two-natural-immunomodulator-compounds-solve-infection-of-macrophages-by-leishmania-major
#14
Michel Muálem de Moraes Alves, Lucas Moreira Brito, Adriana Cunha Souza, Bárbara Cristina Silva Holanda Queiroz, Thaynara Parente de Carvalho, Joilson Ferreira Batista, Jéssica Sara de Sousa Macêdo Oliveira, Ivete Lopes de Mendonça, Silvéria Regina de Sousa Lira, Mariana Helena Chaves, Juan Carlos Ramos Gonçalves, Sabrina Maria Portela Carneiro, Daniel Dias Rufino Arcanjo, Fernando Aécio de Amorim Carvalho
Leishmaniasis is a complex of parasitic protozoan diseases caused by more than 20 different species of parasites from Leishmania genus. Conventional treatments are high costly, and promote a sort of side effects. Besides, protozoan resistance to treatments has been reported. Natural products have been investigated as a source of new therapeutic alternatives, not only acting directly against the parasite but also being able to synergistically act on the host immune system in order to control parasitemia. Gallic acid (GA) and ellagic acid (EA) are plant-derived phenolic compounds which are able to induce antiinflammatory, gastroprotective, and anticarcinogenic activities...
June 22, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28612111/probable-mechanisms-involved-in-the-antipsychotic-like-activity-of-methyl-jasmonate-in-mice
#15
Olajide S Annafi, Oritoke M Aluko, Anthony T Eduviere, Osarume Omorogbe, Solomon Umukoro
Psychosis is a chronic neuropsychiatric disorder that affects millions of individuals worldwide and impairs the quality of life and productivity of the patients. The clinical efficacy of antipsychotic drugs has been compromised by adverse effects, relapse, and therapeutic failures, thus necessitating search for alternative agents. Methyl jasmonate (MJ) is a bioactive compound reported to have beneficial effects in various neurological disorders. This study was undertaken to investigate the antipsychotic-like effects of MJ in mice...
June 13, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28589248/quercetin-and-tin-protoporphyrin-attenuate-hepatic-ischemia-reperfusion-injury-role-of-ho-1
#16
Yara Atef, Hassan M El-Fayoumi, Yousra Abdel-Mottaleb, Mona F Mahmoud
Ischemia reperfusion (IR) injury occurs in many clinical situations such as organ transplantation and hepatectomies resulting in oxidative stress and immune activation. Heme oxygenase-1(HO-1) is the rate-limiting step in the heme-degradation pathway and has a critical cytoprotective role. Induction of HO-1 improves liver I/R injury. Quercetin, a plant pigment (flavonoid), is an antioxidant and HO-1 inducer. Tin protoporphyrin (SnPP) is a HO-1 inhibitor. This study was designed to investigate the protective effect of quercetin in hepatic I/R injury and the role of HO-1...
June 6, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28577050/anticonvulsive-activity-of-1s-verbenone-involving-rna-expression-of-bdnf-cox-2-and-c-fos
#17
Cynthia Germoglio Farias de Melo, Paula Regina Rodrigues Salgado, Diogo Vilar da Fonsêca, Renan Marinho Braga, Marcelo Ricardo Dutra Caldas Filho, Ingrid Eulália Vieira de Farias, Hilzeth de Luna Freire Pessôa, Eleonidas Moura Lima, Ian Porto Gurgel do Amaral, Damião Pergentino de Sousa, Reinaldo Nóbrega de Almeida
(1S)-(-)-verbenone (VRB) is a monoterpene present in the essential oils of many plants which has shown therapeutic effect; however, its anticonvulsant activity has not yet been evaluated. The present work sought to investigate the anticonvulsant activity of VRB using pilocarpine and pentylenetetrazole-induced seizure testing; seeking also probable mechanisms of action. VRB caused no significant changes in motor coordination. Also, no significant data was observed in the pilocarpine-induced seizure tests. In the PTZ-induced seizures test, VRB showed anticonvulsant activity at doses of 200 mg/kg i...
June 2, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28509114/implicating-the-potential-role-of-orexin-in-hypertension
#18
REVIEW
Monika Rani, Raghuvansh Kumar, Pawan Krishan
Orexins (orexin A and orexin B), neuropeptides of hypothalamic origin also known as hypocretins, have been well documented for regulating the different physiological functions including feeding, sleep wakefulness, stress, and reward. However, from the past few years, orexins have evolved as an emerging biomarker for various endocrine disorders including diabetes mellitus and obesity which ultimately leads to various cardiovascular risk factors. Orexins exist in two isoforms orexin A and orexin B and exert their effect by acting on the G protein-coupled receptors orexin 1 receptor (OX1R) and orexin 2 receptor (OX2R)...
May 16, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28474169/denominator-changes-may-obscure-results-from-single-well-assays-%C3%AE-3-adrenoceptor-ligand-induced-changes-of-cell-number-as-example
#19
LETTER
Katerina Okeke, Martina B Michel-Reher, Martin C Michel
No abstract text is available yet for this article.
May 4, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28593342/the-role-of-dual-leucine-zipper-kinase-dlk-in-%C3%AE-cell-apoptosis-a-potential-target-for-the-prevention-and-treatment-of-type-2-diabetes-commentary-to-b%C3%A3-rchers-et-al-tnf-%C3%AE-induced-dlk-activation-contributes-to-apoptosis-in-the-%C3%AE-cell-line-hit
#20
EDITORIAL
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