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Celecoxib

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https://www.readbyqxmd.com/read/28212885/epinephrine-promotes-cox-2-dependent-immune-suppression-in-myeloid-cells-and-cancer-tissues
#1
Ravikumar Muthuswamy, Nana J Okada, Frank J Jenkins, Kandace McGuire, Priscilla F McAuliffe, Herbert J Zeh, David L Bartlett, Callen Wallace, Simon Watkins, Jill D Henning, Dana H Bovbjerg, Pawel Kalinski
Activation of the sympathetic nervous system (e.g., due to stress) has been implicated in cancer progression and recurrence, but its cancer-promoting effects have been variable between different studies. Here, we report that although catecholamines, mediators of systemic sympathetic activity, display only weak immunosuppressive impact on their own, their combination with inflammatory signals leads to the induction of COX-2 and multiple COX-2-dependent suppressive factors in human myeloid cells and cancer tissues...
February 14, 2017: Brain, Behavior, and Immunity
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
#2
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/28203404/the-role-of-cyclooxygenase-2-in-the-protection-against-apoptosis-in-vascular-endothelial-cells-induced-by-cigarette-smoking
#3
Zhihui Shi, Yan Chen, Yanfang Pei, Yingjiao Long, Caihong Liu, Jun Cao, Ping Chen
BACKGROUND: Apoptosis has been demonstrated to be an important upstream event in the pathogenesis of chronic obstructive pulmonary disease (COPD). Cyclooxygenase-2 (COX-2) seems to be biologically relevant in COPD. However, the role of COX-2 in the apoptosis in vascular endothelial cells induced by cigarette smoke extract (CSE) remains to be elucidated. Our recent study found that the prostacyclin, one of the COX products in the microvascular endothelium, inhibited apoptosis in the emphysematous lungs of rats induced by CSE...
January 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28194863/oxygen-activated-palladium-nanoparticle-catalyzed-ultrafast-cross-coupling-of-organolithium-reagents
#4
Dorus Heijnen, Filippo Tosi, Carlos Vila, Marc C A Stuart, Philip H Elsinga, Wiktor Szymanski, Ben L Feringa
The discovery of an ultrafast cross-coupling of alkyl- and aryllithium reagents with a range of aryl bromides is presented. The essential role of molecular oxygen to form the active palladium catalyst was established; palladium nanoparticles that are highly active in cross-coupling reactions with reaction times ranging from 5 s to 5 min are thus generated in situ. High selectivities were observed for a range of heterocycles and functional groups as well as for an expanded scope of organolithium reagents...
February 14, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28193314/celecoxib-mediated-activation-of-endoplasmic-reticulum-stress-induces-de-novo-ceramide-biosynthesis-and-apoptosis-in-hepatoma-hepg2-cells
#5
Hyo Jin Maeng, Jae-Hwi Song, Goon-Tae Kim, Yoo-Jeong Song, Kangpa Lee, Jae-Young Kim, Tae-Sik Park
Ceramides are the major sphingolipid metabolites involved in cell survival and apoptosis. When HepG2 hepatoma cells were treated with celecoxib, the expression of the genes in de novo sphingolipid biosynthesis and sphingomyelinase pathway was upregulated and cellular ceramide was elevated. In addition, celecoxib induced endoplasmic reticulum (ER) stress in a time-dependent manner. SPTLC2, a subunit of serine palmitoyltransferase, was overexpressed by adenovirus. Adenoviral overexression of SPTLC2 (AdSPTLC2) decreased cell viability of HEK293 and HepG2 cells...
February 10, 2017: BMB Reports
https://www.readbyqxmd.com/read/28191652/goniothalamin-and-celecoxib-effects-during-aging-targeting-pro-inflammatory-mediators-in-chemoprevention-of-prostatic-disorders
#6
Larissa Akemi Kido, Fabio Montico, Débora Barbosa Vendramini-Costa, Ronaldo Aloise Pilli, Valeria Helena Alves Cagnon
BACKGROUND: Prostate is highly affected by aging, which lead to inflammatory disorders that can predispose to cancer development. Chemoprevention has emerged as a new therapeutic approach, intensifying studies evaluating the biological properties of new compounds. The aim of this study was to characterize the inflammatory responses in the prostate ventral lobe from senile mice treated with Goniothalamin (GTN), a promising natural compound with anti-inflammatory and antiproliferative properties...
February 13, 2017: Prostate
https://www.readbyqxmd.com/read/28174660/mrgfus-for-desmoid-tumors-within-the-thigh-early-clinical-experiences
#7
Matthew D Bucknor, Viola Rieke
BACKGROUND: Desmoid tumors are benign but locally aggressive non-malignant tumors derived from fibroblasts. Surgery, chemotherapy, and radiation therapy have been the mainstay of treatment, but recurrence is common and side effects can result in significant morbidity. In this case series, we highlight our experiences performing treatments in the thigh, including strategies for optimizing ablation size and safety. CASE PRESENTATION: Since December 2014, 14 magnetic resonance-guided focused ultrasound (MRgFUS) treatments for desmoid tumors were performed at our institution in seven patients...
2017: Journal of Therapeutic Ultrasound
https://www.readbyqxmd.com/read/28164777/is-celecoxib-a-useful-adjunct-in-the-treatment-of-post-tonsillectomy-pain-in-the-adult-population-a-randomised-double-blind-placebo-controlled-study
#8
RANDOMIZED CONTROLLED TRIAL
T-T Ng, D Diamantaras, J Priestley, J Redman, N De Silva, V Mahanta
OBJECTIVE: To evaluate the efficacy and safety of celecoxib for pain management in post-tonsillectomy adult patients. DESIGN: A randomised, double-blind, placebo-controlled, phase 3 clinical trial was conducted in an adult population (aged 18-55 years), with a parallel group design using an allocation ratio of 1:1. METHODS: Eighty patients underwent elective tonsillectomy or adenotonsillectomy, operated on by one surgeon. They were discharged home with randomly assigned celecoxib or placebo, together with regular post-tonsillectomy medications (paracetamol and Endone)...
January 2017: Journal of Laryngology and Otology
https://www.readbyqxmd.com/read/28159531/a-validated-lc-ms-ms-method-for-the-estimation-of-glimepiride-and-pitavastatin-in-rat-plasma-application-to-drug-interaction-studies
#9
Shruti Surendran, David Paul, Ratna Sushmita, Lavanya Krishna, Nirbhay Kumar Tiwari, Sanjeev Giri, Nanjappan Satheeshkumar
Glimepiride (GLI) is prescribed for the management of type-2 diabetes where as pitavastatin (PIT) for the treatment of diabetes associated dyslipidemia. Both the drugs are metabolized by CYP2C9 and have the potential of altering the enzyme through either inhibition or induction. In this respect, we present a simple, fast and validated bioanalytical LC-MS/MS method for the simultaneous estimation of GLI and PIT from rat plasma. Waters XTerra RP HPLC column (4.6×100mm, 5μm) with mobile phase consisting of acetonitrile and 10mM ammonium acetate (pH-6...
January 9, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28148539/dtb-select-2-february-2017
#10
(no author information available yet)
MHRA clarifies spironolactone advice ● Statin dosing: morning or evening? ● PPI use and risk of community-acquired pneumonia ● Non-inferiority trials: caution needed ● CV safety of celecoxib? ● ADRs and emergency department visits ● Study questions use of duloxetine in stress incontinence ● New oral anticoagulants: more on GI bleeding risk.
February 2017: Drug and Therapeutics Bulletin
https://www.readbyqxmd.com/read/28139023/investigation-of-the-predictive-validity-of-laser-eps-on-normal-uvb-and-capsaicin-irritated-skin-with-4-analgesic-compounds-in-healthy-volunteers
#11
Klaus Schaffler, Laurent B Nicolas, Andreas Borta, Tobias Brand, Peter Reitmeir, Robert Roebling, Joachim Scholpp
AIMS: To assess predictivity of laser-(radiant-heat)-evoked-potentials (LEPs) from vertex-EEG, as algesimetric procedure, testing anti-nociceptive/anti-hyperalgesic effects of single oral doses of 4 marketed analgesics (different compound classes) vs. placebo with healthy volunteers in 3 skin types. METHODS: This was a randomized, placebo-controlled, single-blind, 5-way-crossover trial. Twenty-five healthy female/male Caucasians were included (receiving celecoxib 200 mg, pregabalin 150 mg, duloxetine 60 mg, lacosamide 100 mg, placebo) in a Williams design with CO2 -laser-induced painful stimuli on normal, UVB-inflamed and capsaicin-irritated skin...
January 31, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28130854/isotope-labelling-by-reduction-of-nitriles-application-to-the-synthesis-of-isotopologues-of-tolmetin-and-celecoxib
#12
Kate Ellis-Sawyer, Ryan A Bragg, Nick Bushby, Charles S Elmore, Michael J Hickey
The aryl methyl group is found in many drug-like compounds, but there are limited ways of preparing compounds with an isotope label in this methyl position. The process of cyanation of an aryl halide followed by complete reduction of the nitrile to a methyl group was investigated as a route for preparing stable and radiolabelled isotopologues of drug-like compounds. Using this methodology, carbon-13, deuterium, carbon-14 and tritium labelled isotopologues of the non-steroidal anti-inflammatory drug (NSAID) tolmetin were produced, as well as carbon-13, deuterium and carbon-14 labelled isotopologues of another NSAID, celecoxib...
January 28, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28127041/therapy-cardiovascular-safety-of-celecoxib-naproxen-and-ibuprofen
#13
Michael T Nurmohamed
No abstract text is available yet for this article.
January 27, 2017: Nature Reviews. Rheumatology
https://www.readbyqxmd.com/read/28126501/hyperalgesic-and-hypoalgesic-mechanisms-evoked-by-the-acute-administration-of-ccl5-in-mice
#14
Sara González-Rodríguez, Miguel G Álvarez, Mario García-Domínguez, Ana Lastra, Rafael Cernuda-Cernuda, Alicia R Folgueras, María Teresa Fernández-García, Agustín Hidalgo, Ana Baamonde, Luis Menéndez
We show here that the intraplantar administration of CCL5 in mice produces hyperalgesia at low doses but activates compensatory antinociceptive mechanisms at doses slightly higher. Thus, the injection of 3-10 ng of CCL5 evoked thermal hyperalgesia through the activation of CCR1 and CCR5 receptors, as demonstrated by the inhibitory effect exerted by the selective antagonists J113863 (0.01-0.1 μg) and DAPTA (0.3-3 μg), respectively. The prevention of this hyperalgesia by diclofenac (1-10 μg), the inhibitors of COX-1 SC-560 (0...
January 23, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28126288/medicinal-attributes-of-1-2-3-triazoles-current-developments
#15
REVIEW
Divya Dheer, Virender Singh, Ravi Shankar
1,2,3-Triazoles are important five-membered heterocyclic scaffold due to their extensive biological activities. This framework can be readily obtained in good to excellent yields on the multigram scale through click chemistry via reaction of aryl/alkyl halides, alkynes and NaN3 under ambient conditions. It has been an emerging area of interest for many researchers throughout the globe owing to its immense pharmacological scope. The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors (celecoxib, pyrazofurin), HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials...
January 18, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28124617/in-vitro-and-in-vivo-evaluation-of-dmso-and-azone-as-penetration-enhancers-for-cutaneous-application-of-celecoxib
#16
Thassia D Arc Senna, Hilton Antonio Mata Dos Santos, Daniel Mabundu Kibwila, Alvaro Costa Leitão, Alexandre Dos Santos Pyrrho, Marcelo De Pádula, Elaine Cruz Rosas, Tatiana Almeida Pádua, Marilisa Guimarães Lara, Maria Bernadete Riemma Pierre
BACKGROUND: Celecoxib (CXB) has been explored as an anti-inflammatory or chemopreventive drug for topical treatment of skin diseases and cancer. OBJECTIVE: The main aim of this work was to investigate the potential of dimethylsufoxide (DMSO) and Azone (AZ) as penetration enhancers (P.Es) for topical delivery of CXB. METHOD: The in vitro studies, drug release, skin permeability and potential cytotoxicity/genotoxicity were carried out with formulations containing or not DMSO or AZ (5% and 10%)...
January 25, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28124089/evening-primrose-oil-or-forskolin-ameliorates-celecoxib-enhanced-upregulation-of-tissue-factor-expression-in-mice-subjected-to-lipopolysaccharide-induced-endotoxemia
#17
Sarah M Mosaad, Sawsan A Zaitone, Amal A M Ahmed, Dina M Abo-Elmatty, Amani A El-Baz, Yasser M Moustafa
Celecoxib, a selective cyclooxygenase-2 inhibitor, produces thrombotic events in patients predisposed to cardiovascular risk factors. One theory reported an increase in endothelial expression of tissue factor (TF) as a predisposing factor. This work explored the effect of evening primrose oil (EPO), a source of prostaglandin E1, and forskolin (a cyclic adenosine monophosphate stimulator) against the prothrombotic effect of celecoxib in mice. Lipopolysaccharide mouse model of endotoxemia was used to induce an upregulation of TF activity...
January 26, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28119811/2-3-diaryl-3h-imidazo-4-5-b-pyridine-derivatives-as-potential-anticancer-and-anti-inflammatory-agents
#18
Erin Marie Kirwen, Tarun Batra, Chandrabose Karthikeyan, Girdhar Singh Deora, Vandana Rathore, Chaitanya Mulakayala, Naveen Mulakayala, Amy Catherine Nusbaum, Joel Chen, Haneen Amawi, Kyle McIntosh, Sahabjada, Neelam Shivnath, Deepak Chowarsia, Nisha Sharma, Md Arshad, Piyush Trivedi, Amit K Tiwari
In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives retrieved from our in-house database were evaluated for their cytotoxic activity against nine cancer cell lines. The results indicated that the compounds showed moderate cytotoxic activity against MCF-7, MDA-MB-468, K562 and SaOS2 cells, with K562 being the most sensitive among the four cancer cell lines...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28114089/-non-conventional-pharmacological-agents-for-the-treatment-of-bipolar-disorder-%C3%AE-systematic-review-of-the-evidence
#19
K N Fountoulakis, D Balaris, V Nikolaou, J Νimatoudis
Bipolar disorder (BD) has a complex and variable clinical picture which is characterized by many different phacets and phases and as a result its therapeutical options are also complex and often unsatisfactory. Typically the so-called "mood stabilizers" are used in the treatment of BD and in this class lithium and specific antiepileptics are included. The present study aimed to systematically review the literature concerning the presence of randomized double blind clinical trials of 'non conventional' pharmaceutical treatment options...
October 2016: Psychiatrikē, Psychiatriki
https://www.readbyqxmd.com/read/28112061/inflammation-and-depression-a-causal-or-coincidental-link-to-the-pathophysiology
#20
Brian E Leonard
This review summarises the evidence that chronic low grade inflammation triggers changes that contribute to the mental and physical ill health of patients with major depression. Inflammation, and the activation of the hypothalamic pituitary axis by stress, are normal components of the stress response but when stress is prolonged and the endocrine and immune system become chronic resulting in the activation of the peripheral macrophages, the central microglia and hypercortisolemia, the neuronal networks are damaged and become dysfunctional...
January 23, 2017: Acta Neuropsychiatrica
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