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indomethacin

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https://www.readbyqxmd.com/read/28223151/testosterone-rapidly-increases-ca-2-activated-k-currents-causing-hyperpolarization-in-human-coronary-artery-endothelial-cells
#1
Katesirin Ruamyod, Wattana B Watanapa, Chairat Shayakul
Testosterone has endothelium-dependent vasodilatory effects on the coronary artery, with some reports suggesting endothelial ion channel involvement. This study employed the whole-cell patch clamp technique to investigate the effect of testosterone on ion channels in human coronary artery endothelial cells (HCAECs) and the mechanisms involved. We found that 0.03-3μM testosterone significantly induced a rapid, concentration-dependent increase in total HCAEC current (EC50, 71.96±1.66nM; maximum increase, 59...
February 18, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28222030/sub-chronic-indomethacin-treatment-and-its-effect-on-the-male-reproductive-system-of-albino-rats-possible-protective-role-of-black-tea-extract
#2
Ishwar B Bagoji, Gavishiddappa A Hadimani, Saeed M Yendigeri, Kusal K Das
BACKGROUND: Indomethacin is commonly used as a nonsteroidal anti-inflammatory drug (NSAID) to treat inflammation, arthritis and joint pains. Unfortunately, it has a wide range of adverse effects on the physiological system, including gonads. This study aimed to assess possible beneficial effects of black tea extract (BTE) against indomethacin-induced alteration of gonadal hormone levels in male rats. MATERIALS AND METHODS: Adult male rats were divided into Group I (control), Group II (indomethacin, 5 mg/kg body weight [bwt...
February 21, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28216886/obtaining-a-dry-extract-from-the-mikania-laevigata-leaves-with-potential-for-antiulcer-activity
#3
Mariana Viana Pinto, Ezequiane Machado Oliveira, Jose Luiz Rodrigues Martins, Jose Realino de Paula, Elson Alves Costa, Edemilson Cardoso da Conceição, Maria Teresa Freitas Bara
BACKGROUND: Mikania laevigata leaves are commonly used in Brazil as a medicinal plant. OBJECTIVE: To obtain hydroalcoholic dried extract by nebulization and evaluate its antiulcerogenic potential. MATERIALS AND METHODS: Plant material and hydroalcoholic extract were processed and analyzed for their physicochemical characteristics. A method using HPLC was validated to quantify coumarin and o-coumaric acid. Hydroalcoholic extract was spray dried and the powder obtained was characterized in terms of its physicochemical parameters and potential for antiulcerogenic activity...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28215165/synthesis-characterization-and-comparison-of-local-analgesic-anti-inflammatory-ulcerogenic-activity-of-copper-and-zinc-complexes-of-indomethacin
#4
Abhijit Sukul, Saikat Kumar Poddar, Sanjana Haque, Sajal Kumar Saha, Sreedam Chandra Das, Zobaer Al Mahmud, S M AbdurRahman, Abhijit Sukul
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAID) exert gastrointestinal upset by inhibiting mucosal cyclooxygenase (COX) activity for which complexation technique with metals has been adopted to overcome this drawback. OBJECTIVE: The study aimed to overcome the gastrointestinal side effects associated with indomethacin treatment by synthesizing copper (Cu) and zinc (Zn) complexes of indomethacin along with assessing potential pharmacological effects of these complexes...
February 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#5
Cinara Soares Vidal, Anita Oliveira Brito Pereira Bezerra Martins, Andressa de Alencar Silva, Maria Rayane Correia de Oliveira, Jaime Ribeiro-Filho, Thaís Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Jackson Roberto Guedes da Silva Almeida, Lucindo Jose Quintans, Irwin Rose Alencar de Menezes
BACKGROUND: Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE: The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28212299/exogenous-and-endogenous-hydrogen-sulfide-protects-gastric-mucosa-against-the-formation-and-time-dependent-development-of-ischemia-reperfusion-induced-acute-lesions-progressing-into-deeper-ulcerations
#6
Marcin Magierowski, Katarzyna Magierowska, Magdalena Hubalewska-Mazgaj, Zbigniew Sliwowski, Robert Pajdo, Grzegorz Ginter, Slawomir Kwiecien, Tomasz Brzozowski
Hydrogen sulfide (H₂S) is an endogenous mediator, synthesized from l-cysteine by cystathionine γ-lyase (CSE), cystathionine β-synthase (CBS) or 3-mercaptopyruvate sulfurtransferase (3-MST). The mechanism(s) involved in H₂S-gastroprotection against ischemia/reperfusion (I/R) lesions and their time-dependent progression into deeper gastric ulcerations have been little studied. We determined the effect of l-cysteine, H₂S-releasing NaHS or slow H₂S releasing compound GYY4137 on gastric blood flow (GBF) and gastric lesions induced by 30 min of I followed by 3, 6, 24 and 48 h of R...
February 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28207272/controlling-the-release-of-indomethacin-from-glass-solutions-layered-with-a-rate-controlling-membrane-using-fluid-bed-processing-part-2-the-influence-of-formulation-parameters-on-drug-release
#7
Aswin Dereymaker, Jirka Pelgrims, Frederick Engelen, Peter Adriaensens, Guy Van den Mooter
This study aimed to investigate the pharmaceutical performance of an indomethacin-polyvinylpyrrolidone (PVP) glass solution applied using fluid bed processing as a layer on inert sucrose spheres, and subsequently top-coated with a release rate controlling membrane consisting of either ethyl cellulose or Eudragit RL. The implications of the addition of a pore former (PVP) and the coating medium (ethanol or water) on the diffusion and release behavior were also considered. In addition, the role of a charge interaction between drug and controlled release polymer on the release was investigated...
February 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28206770/controlling-the-release-of-indomethacin-from-glass-solutions-layered-with-a-rate-controlling-membrane-using-fluid-bed-processing-part-1-surface-and-cross-sectional-chemical-analysis
#8
Aswin Dereymaker, David J Scurr, Elisabeth D Steer, Clive J Roberts, Guy Van den Mooter
Fluid bed coating has been shown to be a suitable manufacturing technique to formulate poorly soluble drugs in glass solutions. Layering inert carriers with a drug-polymer mixture enables these beads to be immediately filled into capsules, thus avoiding additional, potentially destabilizing, downstream processing. In this study fluid bed coating is proposed for the production of controlled release dosage forms of glass solutions by applying a second, rate controlling membrane on top of the glass solution. Adding a second coating layer adds to the physical and chemical complexity of the drug delivery system so a thorough understanding of the physical structure and phase behavior of the different coating layers is needed...
February 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28205100/efficacy-of-oral-supplemental-hydration-for-the-prevention-of-contrast-induced-nephropathy-in-rats
#9
Tamaki Matsunami, Kazuo Hino, Rie Dosho, Sho Miyatake, Goro Ebisu, Ryohei Kuwatsuru
PURPOSE: To compare oral rehydration solution (ORS) with saline infusion for preventing contrast-induced nephropathy (CIN) in a rat model. MATERIALS AND METHODS: Adult male Sprague-Dawley rats (310-360 g) received intravenous indomethacin (10 mg/kg), N (G)-nitro-L-arginine methyl ester (10 mg/kg), and iohexol (10 mL/kg) to induce acute contrast-induced renal injury (CIN group); control rats received saline only. For hydration, rats received either continuous infusion (20 mL/kg/h) of saline or three oral doses (20 mL/kg each) of ORS...
February 15, 2017: Japanese Journal of Radiology
https://www.readbyqxmd.com/read/28197935/anti-inflammatory-effect-of-total-saponin-fraction-from-dioscorea-nipponica-makino-on-gouty-arthritis-and-its-influence-on-nalp3-inflammasome
#10
Qi Zhou, Dong-Hua Yu, Ning Zhang, Shu-Min Liu
OBJECTIVE: To investigate the mechanism of Chinese herbal medicine Dioscorea nipponica for the treatment of monosodium urate crystals-induced gouty arthritis (GA) in rats. METHODS: Sixty male Wistar rats were divided into 6 groups: normal, model, indomethacin and three total saponin (900, 300 and 100 mg/kg) groups. The liver, kidney and serum levels of lysosomal enzymes, antioxidant capacities, and inflammatory factors were measured. In addition, the mRNA and protein levels of the NALP3 inflammasome components in the mononuclear cells of rats' peripheral blood were analyzed using real-time polymerase chain reaction and Western blotting methods, respectively...
February 15, 2017: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28192663/surfactant-free-solid-dispersions-of-hydrophobic-drugs-in-an-amorphous-sugar-matrix-dried-from-an-organic-solvent
#11
Koji Takeda, Yuto Gotoda, Daichi Hirota, Fumihiro Hidaka, Tomo Sato, Tsutashi Matsuura, Hiroyuki Imanaka, Naoyuki Ishida, Koreyoshi Imamura
The technique for homogeneously dispersing hydrophobic drugs in a water-soluble solid matrix (solid dispersion) is a subject that has been extensively investigated in the pharmaceutical industry. Herein, a novel technique for dispersing a solid, without the need to use a surfactant, is reported. A freeze-dried amorphous sugar sample was dissolved in an organic solvent, that contained a soluble model hydrophobic component. The suspension of the sugar and the model hydrophobic component was vacuum foam dried to give a solid powder...
February 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28192151/angiotensin-1-7-dependent-vasorelaxation-of-the-renal-artery-exhibits-unique-angiotensin-and-bradykinin-receptor-selectivity
#12
Mariam H M Yousif, Ibrahim F Benter, Debra I Diz, Mark C Chappell
Angiotensin-(1-7) [Ang-(1-7)] exhibits blood pressure lowering actions, inhibits cell growth, and reduces tissue inflammation and fibrosis which may functionally antagonize an activated Ang II-AT1 receptor axis. Since the vascular actions of Ang-(1-7) and the associated receptor/signaling pathways varies in different vascular beds, the current study established the vasorelaxant properties of the heptapeptide in the renal artery of male Wistar male rats. Ang-(1-7) produced an endothelium-dependent vasodilator relaxation of isolated renal artery segments pre-contracted by a sub-maximal concentration of phenylephrine (PE) (10(-7)M)...
February 9, 2017: Peptides
https://www.readbyqxmd.com/read/28190472/gastroprotective-and-anti-secretory-mechanisms-of-2-phenylquinoline-an-alkaloid-isolated-from-galipea-longiflora
#13
Eduardo Breviglieri, Luisa Mota da Silva, Thaise Boeing, Lincon Bordignon Somensi, Benhur Judah Cury, Alberto Gimenez, Valdir Cechinel Filho, Sérgio Faloni de Andrade
BACKGROUND: We previously described the gastroprotective effect of 2-phenylquinoline (2-PQ), the main alkaloid isolated from the bark of Galipea longiflora (Rutaceae). However, despite the significant and promising results, the pharmacological mechanisms of the gastroprotection induced by 2-PQ have not been investigated. PURPOSE: To evaluate the mechanisms underlying the gastroprotective effects of 2-PQ. STUDY DESIGN: We used an in vivo mouse ulcer model and in vitro methodologies involving H⁺/K⁺-ATPase and L929 murine fibroblasts...
February 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28188165/indomethacin-therapy-effective-in-a-patient-with-depletion-syndrome-from-secretory-villous-adenoma
#14
Matthew David Kagan, Kara Schmidt, Gurtej Sangha
This paper details the case of a 26-year-old woman with depletion syndrome and the effectiveness of her treatment with indomethacin. Villous adenomas are benign neoplasms with a high incidence of becoming malignant. A small percentage of villous adenomas are known to cause depletion syndrome, also referred to as the McKittrick-Wheelock syndrome, a condition characterised by secretory diarrhoea, dehydration, hyponatremia, hypokalaemia, hypochloraemia, metabolic acidosis and acute renal failure. Prostaglandin-E2 mediates the hypersecretion mechanism observed in depletion syndrome, and can be inhibited by cyclo-oxygenase inhibitors...
February 10, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28179107/pro-inflammatory-immune-to-brain-signaling-is-involved-in-neuroendocrine-responses-to-acute-emotional-stress
#15
Jordi Serrats, Jan-Sebastian Grigoleit, Elena Alvarez-Salas, Paul E Sawchenko
Activation of the hypothalamo-pituitary-adrenal (HPA) axis by inflammatory stressors (e.g., bacterial lipopolysaccharide) is thought to involve vascular transduction of circulating cytokines, with perivascular macrophages (PVMs) along with endothelia, effecting activation of HPA control circuitry via inducible (cyclooxygenase-2- or COX-2- dependent) prostaglandin synthesis. To test the stressor-specificity of this mechanism, we examined whether ablation of PVMs or pharmacologic blockade of COX activity affected HPA responses to a representative emotional stressor, restraint...
February 4, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28178591/attenuation-of-stress-induced-memory-deficits-by-nonsteroidal-anti-inflammatory-drugs-nsaids-in-rats-role-of-antioxidant-enzymes
#16
Shaista Emad, Sara Qadeer, Sana Sadaf, Zehra Batool, Saida Haider, Tahira Perveen
BACKGROUND: Repeated stress paradigms have been shown to cause devastating alterations on memory functions. Stress is linked with inflammation. Psychological and certain physical stressors could lead to neuroinflammation. Inflammatory process may occur by release of mediators and stimulate the production of prostaglandins through cyclooxygenase (COX). Treatment with COX inhibitors, which restrain prostaglandin production, has enhanced memory in a number of neuroinflammatory states showing a potential function for raised prostaglandins in these memory shortfalls...
November 29, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28177685/vasodilatory-effects-and-underlying-mechanisms-of-the-ethyl-acetate-extracts-from-gastrodia-elata-blume
#17
Rong Dai, Ting Wang, Xiaoqin Si, Yuanyuan Jia, Lili Wang, Yan Yuan, Qing Lin, Cui Yang
The objective of this study was to assess the ethyl acetate extracts of Gastrodia elata Blume (GEB) on vascular tone and the mechanisms involved. GEB was extracted with 95% EtOH followed by a further extraction with ethyl acetate. The effects of GEB and its ingredients on the isometric tensions of the aortic rings from rats were measured. The ethyl acetate extract of GEB induced a vasodilatatory effect on rat aorta which was partially dependent on endothelium. Four chemical compounds isolated from GEB were identified as 3, 4-dihydroxybenzaldehyde (DB), 4-hydroxy benzaldehyde (HB), 4-methoxybenzyl alcohol (MA) and 4, 4'-dihydroxydiphenyl methane (DM), respectively...
December 17, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28176666/role-of-sulforaphane-in-protection-of-gastrointestinal-tract-against-h-pylori-and-nsaid-induced-oxidative-stress
#18
Akinori Yanaka
BACKGROUND: Sulforaphane (SFN), a phytochemical found in abundance in broccoli sprouts, potently induces a variety of antioxidant enzymes, and thereby protects cells from injury induced by various kinds of oxidative stresses. It has been suggested that both H. pylori infection and intake of non-steroidal anti-inflammatory drugs (NSAIDs) induce chronic oxidative stress in gastrointestinal (GI) mucosa, thereby causing mucosal injury in the GI tract. Therefore, it would be a reasonable assumption that SFN protects GI mucosa against oxidative injury induced by H...
February 6, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28176198/constituents-of-leaves-from-bauhinia-curvula-benth-exert-gastroprotective-activity-in-rodents-role-of-quercitrin-and-kaempferol
#19
Ana Paula Beber, Priscila de Souza, Thaise Boeing, Lincon Bordignon Somensi, Luísa Nathália Bolda Mariano, Benhur Judah Cury, Ligia Moura Burci, Cristiane Bezerra da Silva, Euclésio Simionatto, Sérgio Faloni de Andrade, Luísa Mota da Silva
The Bauhinia genus is known as "Pata-de-Vaca" and a wide variety of these species are used in Brazilian folk medicine due to their gastroprotective properties. This study aimed to investigate the antiulcer efficacy of the hydroalcoholic extract from B. curvula (HEBC) leaves, as well as its semi-purified fraction (SPFr) and the contribution of their phytochemicals constituents for this effect. For that, ethanol 60%/HCl 0.3 M- and indomethacin-induced gastric ulcer were performed in rodents. Gastric ulcerated tissues were processed for histological, histochemical and biochemical analysis...
February 7, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28174191/augmentation-of-muscle-blood-flow-by-ultrasound-cavitation-is-mediated-by-atp-and-purinergic-signaling
#20
J Todd Belcik, Brian P Davidson, Aris Xie, Melinda D Wu, Mrinal Yadava, Yue Qi, Sherry Liang, Chae Ryung Chon, Azzdine Y Ammi, Joshua Field, Leanne Harmann, William M Chilian, Joel Linden, Jonathan R Lindner
BACKGROUND: - Augmentation of tissue blood flow by therapeutic ultrasound is thought to rely on convective shear. Microbubble contrast agents that undergo ultrasound-mediated cavitation markedly amplify these effects. We hypothesized that purinergic signalling is responsible for shear-dependent increases in muscle perfusion during therapeutic cavitation. METHODS: -Unilateral exposure of the proximal hindlimb of mice (with or without ischemia produced by iliac ligation) to therapeutic ultrasound (1...
February 7, 2017: Circulation
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