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Cox 2 inhibitors

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https://www.readbyqxmd.com/read/29777723/effect-of-acetylcholinesterase-inhibitors-donepezil-and-rivastigmine-on-the-activity-and-expression-of-cyclooxygenases-in-a-model-of-the-inflammatory-action-of-fluoride-on-macrophages-obtained-from-thp-1-monocytes
#1
Marta Goschorska, Irena Baranowska-Bosiacka, Izabela Gutowska, Maciej Tarnowski, Katarzyna Piotrowska, Emilia Metryka, Krzysztof Safranow, Dariusz Chlubek
Inflammation is an important factor in the development of many diseases of the central nervous system, including Alzheimer's disease and other types of dementia. ‪Given that acetylcholinesterase inhibitors are also currently believed to have anti-inflammatory properties, the purpose of this study was to investigate the effect of acetylcholinesterase inhibitors (rivastigmine, donepezil) on cyclooxygenase activity and expression using the proinflammatory action of fluoride (F- ) on cultured macrophages obtained from THP-1 monocytes...
May 16, 2018: Toxicology
https://www.readbyqxmd.com/read/29777264/empagliflozin-reduces-cardiovascular-events-mortality-and-renal-events-in-participants-with-type-2-diabetes-after-coronary-artery-bypass-graft-surgery-subanalysis-of-the-empa-reg-outcome%C3%A2-randomised-trial
#2
Subodh Verma, C David Mazer, David Fitchett, Silvio E Inzucchi, Egon Pfarr, Jyothis T George, Bernard Zinman
AIMS/HYPOTHESIS: After coronary artery bypass graft (CABG) surgery in individuals with type 2 diabetes, there remains a considerable residual cardiovascular risk. In the EMPA-REG OUTCOME® trial in participants with type 2 diabetes and established cardiovascular disease, empagliflozin reduced the risk of cardiovascular death by 38%, all-cause mortality by 32%, hospitalisation for heart failure by 35% and incident or worsening nephropathy by 39% vs placebo when given in addition to standard of care...
May 19, 2018: Diabetologia
https://www.readbyqxmd.com/read/29777058/gpr40-is-a-low-affinity-epoxyeicosatrienoic-acid-receptor-in-vascular-cells
#3
Sang Kyu Park, Anja Herrnreiter, Sandra L Pfister, Kathryn M Gauthier, Benjamin A Falck, John R Falck, William B Campbell
Endothelium-derived epoxyeicosatrienoic acids (EETs) have numerous vascular activities mediated by G protein--coupled receptors. Long-chain free fatty acids and EETs activate GPR40, prompting us to investigate the role of GPR40 in some vascular EET activities. 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 ± 0.08 μM, 0.91 ± 0.08 μM, 3.9 ± 0.06 μM and 19 ± 0.37 nM, respectively)...
May 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29769213/chemopreventive-efficacy-of-the-cyclooxygenase-2-cox-2-inhibitor-celecoxib-is-predicted-by-adenoma-expression-of-cox-2-and-15-pgdh
#4
Jiping Wang, Nancy L Cho, Ann G Zauber, Meier Hsu, Dawn Dawson, Amitabh Srivastava, Kisha A Mitchell-Richards, Sanford D Markowitz, Monica M Bertagnolli
BACKGROUND: The APC trial showed that cyclooxygenase-2 (Cox-2) inhibitor, celecoxib, decreased adenoma development in patients at high risk for colorectal cancer. A prospectively planned analysis of the APC trial tested the hypothesis that expression of target enzymes in adenomas removed before beginning study treatment would identify individuals at high risk of adenoma development, and/or predict response to Cox-2 inhibition. METHODS: Pre-treatment adenomas were examined using immunohistochemistry (IHC) to assess expression of Cox-2 (high vs...
May 16, 2018: Cancer Epidemiology, Biomarkers & Prevention
https://www.readbyqxmd.com/read/29766544/dipeptidyl-peptidase-4-inhibitor-use-is-associated-with-decreased-risk-of-fracture-in-patients-with-type-2-diabetes-a-population-based-cohort-study
#5
Wen-Hsuan Hou, Kai-Cheng Chang, Chung-Yi Li, Huang-Tz Ou
AIMS: To investigate the putative link between dipeptidyl peptidase-4 inhibitor (DPP-4i) use and the risk of fracture in patients with type 2 diabetes. METHODS: This propensity-score-matched population-based cohort study was performed between 2009 and 2013 on patients with type 2 diabetes who were stable metformin users. A total of 3,996 patients with type 2 diabetes used DPP-4i as a second-line antidiabetic drug. The same number of matched non-DPP-4i users were followed up until fracture occurrence, health insurance policy termination, or the end of 2013...
May 16, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29766222/cisplatin-increases-the-number-of-enterochromaffin-cells-containing-substance-p-in-rat-intestine
#6
Yusuke Obara, Takuji Machida, Yuho Takano, Saki Shiga, Asami Suzuki, Naoya Hamaue, Kenji Iizuka, Masahiko Hirafuji
We previously reported that cisplatin potentiated ileal 5-hydroxytryptamine (5-HT) metabolism and caused pathological changes with an inflammatory response in the delayed phase (72 h) after administration to rats. In the present study, we further investigated the time-dependent effect of cisplatin on ileal 5-HT metabolism and the effects of combining cisplatin and anti-inflammatory drugs on ileal tryptophan hydroxylase expression and pica (the consumption of non-nutritive materials such as kaolin). Cyclooxygenase-2 (COX-2) expression was significantly increased at 24 h after cisplatin (5 mg/kg, intraperitoneal) administration...
May 15, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29765253/use-of-histamine-h-2-receptor-antagonists-and-outcomes-in-patients-with-heart-failure-a-nationwide-population-based-cohort-study
#7
Kasper Adelborg, Jens Sundbøll, Morten Schmidt, Hans Erik Bøtker, Noel S Weiss, Lars Pedersen, Henrik Toft Sørensen
Background: Histamine H2 receptor activation promotes cardiac fibrosis and apoptosis in mice. However, the potential effectiveness of histamine H2 receptor antagonists (H2RAs) in humans with heart failure is largely unknown. We examined the association between H2RA initiation and all-cause mortality among patients with heart failure. Methods: Using Danish medical registries, we conducted a nationwide population-based active-comparator cohort study of new users of H2RAs and proton pump inhibitors (PPIs) after first-time hospitalization for heart failure during the period 1995-2014...
2018: Clinical Epidemiology
https://www.readbyqxmd.com/read/29765245/the-epidemiology-of-outpatient-pain-treatment-in-pediatrics
#8
Stacy Baldridge, Laura Wallace, Aditi Kadakia
Background: There is limited real-world, population-level data on the prevalence and treatment of pain in children. An understanding of pediatric pain conditions and its management can help inform provider education, treatment guidelines, and design of pediatric pain studies. Therefore, in this study, we aimed to describe the prevalence of conditions associated with acute and chronic pain in pediatric patients and to characterize pediatric pain treatment with nonsteroidal anti-inflammatory drugs, cyclooxygenase-2 (COX-2) inhibitors, opioids (immediate release or extended release), antidepressants, topical analgesics, anticonvulsants, and other therapies based on a large, real-world sample...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29765153/cox-2-mediates-pro-tumorigenic-effects-of-pkc%C3%AE%C2%B5-in-prostate-cancer
#9
Rachana Garg, Jorge M Blando, Carlos J Perez, Priti Lal, Michael D Feldman, Emer M Smyth, Emanuela Ricciotti, Tilo Grosser, Fernando Benavides, Marcelo G Kazanietz
The pro-oncogenic kinase PKCε is overexpressed in human prostate cancer and cooperates with loss of the tumor suppressor Pten for the development of prostatic adenocarcinoma. However, the effectors driving PKCε-mediated phenotypes remain poorly defined. Here, using cellular and mouse models, we showed that PKCε overexpression acts synergistically with Pten loss to promote NF-κB activation and induce cyclooxygenase-2 (COX-2) expression, phenotypic traits which are also observed in human prostate tumors. Targeted disruption of PKCε from prostate cancer cells impaired COX-2 induction and PGE2 production...
May 16, 2018: Oncogene
https://www.readbyqxmd.com/read/29764964/cardiovascular-cv-risk-after-initiation-of-abatacept-versus-tnf-inhibitors-in-rheumatoid-arthritis-patients-with-and-without-baseline-cv-disease
#10
Yinzhu Jin, Eun Ha Kang, Gregory Brill, Rishi J Desai, Seoyoung C Kim
OBJECTIVE: To evaluate the cardiovascular safety of abatacept (ABA) versus tumor necrosis factor inhibitors (TNFi) in rheumatoid arthritis (RA) patients with and without underlying cardiovascular disease (CVD). METHODS: We identified RA patients with and without baseline CVD who initiated ABA or TNFi by using data from 2 large US insurance claims databases: Medicare (2008-2013) and Truven MarketScan (2006-2015). After stratifying by baseline CVD, ABA initiators were 1:1 propensity score (PS) matched to TNFi initiators to control for > 60 baseline covariates...
May 15, 2018: Journal of Rheumatology
https://www.readbyqxmd.com/read/29764240/ferrous-glycinate-regulates-cell-energy-metabolism-by-restricting-hypoxia-induced-factor-1%C3%AE-expression-in-human-a549-cells
#11
Yung-Ting Kuo, Jhong-Huei Jheng, Mei-Chen Lo, Wei-Lu Chen, Shyang-Guang Wang, Horng-Mo Lee
Iron or oxygen regulates the stability of hypoxia inducible factor-1α (HIF-1α). We investigated whether ferrous glycinate would affect HIF-1α accumulation, aerobic glycolysis and mitochondrial energy metabolism in human A549 lung cancer cells. Incubation of A549 cells with ferrous glycinate decreased the protein levels of HIF-1α, which was abrogated by proteosome inhibitor, or prolyl hydroxylase inhibitor. Addition of ferrous glycinate decreased protein levels of glucose transporter-1, hexokinase-2, and lactate dehydrogenase A, and decreased pyruvate dehydrogenase kinase-1 (PDK-1) and pyruvate dehydrogenase (PDH) phosphorylation in A549 cells...
May 15, 2018: Free Radical Research
https://www.readbyqxmd.com/read/29763636/inhibition-of-cox-2-mpges-1-and-5-lox-in-macrophages-by-leonurine-ameliorates-monosodium-urate-crystal-induced-inflammation
#12
Yanzhuo Liu, Chenfan Duan, Honglei Chen, Chenlong Wang, Xiaoxiao Liu, Miao Qiu, Honglin Tang, Feng Zhang, Xiaoyang Zhou, Jing Yang
Cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and microsomal prostaglandin E synthase-1 (mPGES-1)-derived eicosanoids play an essential role in human inflammatory disorders. Here, we investigated whether inhibition of COX-2/mPGES-1 and 5-LOX in macrophages by leonurine ameliorates monosodium urate (MSU) crystal-induced inflammation. Virtual screening assay and in vitro enzyme inhibition assay showed that leonurine was a potential inhibitor of COX-2, mPGES-1 and 5-LOX. Compared with COX-2 inhibitor celecoxib, leonurine (30 mg/kg) significantly decreased ankle perimeter, gait score and neutrophil number in synovial fluid in MSU crystal-treated rats, accompanied with the decreased expression of COX-2, mPGES-1 and 5-LOX and production of prostaglandin E2 (PGE2 ) and leukotriene B4 (LTB4 ) in the synovial fluid macrophages...
May 15, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29758489/fisetin-inhibits-the-generation-of-inflammatory-mediators-in-interleukin-1%C3%AE-induced-human-lung-epithelial-cells-by-suppressing-the-nf-%C3%AE%C2%BAb-and-erk1-2-pathways
#13
Hui-Ling Peng, Wen-Chung Huang, Shu-Chen Cheng, Chian-Jiun Liou
Fisetin, a flavone that can be isolated from fruits and vegetables, has anti-tumor and anti-oxidative properties and ameliorates airway hyperresponsiveness in asthmatic mice. This study investigated whether fisetin can suppress the expression of inflammatory mediators and intercellular adhesion molecule 1 (ICAM-1) in A549 human lung epithelial cells that were stimulated with interleukin-1β (IL-1β) to induce inflammatory responses. A549 cells were treated with fisetin (3-30 μM) and then with IL-1β. Fisetin significantly inhibited COX-2 expression and reduced prostaglandin E2 production, and it suppressed the levels of IL-8, CCL5, monocyte chemotactic protein 1, tumor necrosis factor α, and IL-6...
May 11, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29758412/anti-inflammatory-effect-of-the-extracts-from-the-branch-of-taxillus-yadoriki-being-parasitic-in-neolitsea-sericea-in-lps-stimulated-raw264-7-cells
#14
Su Bin Park, Gwang Hun Park, Ha Na Kim, Ho-Jun Son, Hun Min Song, Hyun-Seok Kim, Hyung Jin Jeong, Jin Boo Jeong
Mistletoe has been used as the herbal medicine to treat hypertension, diabetes mellitus, inflammation, arthritis and viral infection. In this study, we evaluated the anti-inflammatory effect of extracts of branch from Taxillus yadoriki being parasitic in Neolitsea sericea (TY-NS-B) using in vitro model. TY-NS-B significantly inhibited LPS-induced secretion of NO and PGE2 in RAW264.7 cells. TY-NS-B was also observed to inhibit LPS-mediated iNOS COX-2 expression. In addition, TY-NS-B attenuated production of inflammatory cytokines such as TNF-α and IL-1β induced by LPS...
May 11, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29756563/cyclooxygenase-2-inhibitors-as-a-therapeutic-target-in-inflammatory-diseases
#15
Miguel D Ferrer, Carla Busquests-Cortes, Xavier Capo, Silvia Tejada, Josep A Tur, Antoni Pons, Antoni Sureda
Inflammation plays a crucial role in the development of many complex diseases and disorders including autoimmune diseases, metabolic syndrome, neurodegenerative diseases, and cardiovascular pathologies. Prostaglandins play a regulatory role in inflammation. Cyclooxygenases are the main mediators of inflammation by catalyzing the initial step of arachidonic acid metabolism and prostaglandin synthesis. The differential expression of the constitutive isoform COX-1 and the inducible isoform COX-2, and the finding that COX-1 is the major form expressed in the gastro-intestinal tract, lead to the search for COX-2-selective inhibitors as anti-inflammatory agents that might diminish the gastrointestinal side effects of traditional non-steroidal anti-inflamatory drugs (NSAIDs)...
May 13, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29756394/prognostic-impact-of-the-pretreatment-aspartate-transaminase-alanine-transaminase-ratio-in-patients-treated-with-first-line-systemic-tyrosine-kinase-inhibitor-therapy-for-metastatic-renal-cell-carcinoma
#16
Minyong Kang, Jiwoong Yu, Hyun Hwan Sung, Hwang Gyun Jeon, Byong Chang Jeong, Se Hoon Park, Seong Soo Jeon, Hyun Moo Lee, Han Yong Choi, Seong Il Seo
OBJECTIVES: To examine the prognostic role of the pretreatment aspartate transaminase/alanine transaminase or De Ritis ratio in patients with metastatic renal cell carcinoma receiving first-line systemic tyrosine kinase inhibitor therapy. METHODS: We retrospectively searched the medical records of 579 patients with metastatic renal cell carcinoma who visited Samsung Medical Center, Seoul, Korea, from January 2001 through August 2016. After excluding 210 patients, we analyzed 360 patients who received first-line tyrosine kinase inhibitor therapy...
May 13, 2018: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/29755548/ameliorative-effect-of-beraprost-sodium-on-celecoxib-induced-cardiotoxicity-in-rats
#17
Shafique Ahmad, Bibhu Prasad Panda, Mohammad Fahim, Neha Dhyani, Kiran Dubey
Selective COX-2 inhibitors are most widely used analgesic and anti-inflammatory drugs; however, its maximal use is highly associated with various serious abnormal cardiovascular events. Beraprost sodium (BPS), prostacyclin analogue has been shown to vasodilatory, antiplatelates, anti-inflmmatory, and antioxidant activity. The objective of the present study was to evaluate the effect of BPS on celecoxib cardiotoxicity in rats. Toxicity was induced in male Albino rats (250-280 g) by celecoxib (100 mg/kg/day)...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29755544/physicochemical-stress-degradation-evaluation-and-pharmacokinetic-study-of-azgh101-a-new-synthesized-cox2-inhibitor-after-i-v-and-oral-administration-in-male-and-female-rats
#18
Hoda Bahmanof, Simin Dadashzadeh, Afshin Zarghi, Alireza Shafaati, Seyed Mohsen Foroutan
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX-1 and COX-2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al . reported 6-benzoyl-2-(4-(methylsulfonyl) phenyl) quinoline-4-carboxylic acid (AZGH101) as a novel derivative of ketoprofen with improved selectivity index (COX-1/COX-2 inhibitory potency) in comparison with ketoprofen. In this study, the log P and stability of AZGH101 were evaluated and the pharmacokinetic characteristics of this compound were investigated following intravenous (10 mg/kg), and oral administration (20 mg/kg), to Wistar rats...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29755541/design-synthesis-and-biological-evaluation-of-novel-peptide-like-analogues-as-selective-cox-2-inhibitors
#19
Mohammad Ali Ahmaditaba, Mohammad Hassan Houshdar Tehrani, Afshin Zarghi, Sorayya Shahosseini, Bahram Daraei
A new series of peptide-like derivatives containing different aromatic amino acids and possessing pharmacophores of COX-2 inhibitors as SO2 Me or N3 attached to the para position of an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. The synthetic reactions were based on the solid phase peptide synthesis method using Wang resin. One of the analogues, i.e. , compound 2d, as the representative of these series was recognized as the most effective and the highest selective COX-2 inhibitor with IC50 value of 0...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29754125/projected-real-world-effectiveness-of-using-aggressive-low-density-lipoprotein-cholesterol-targets-among-elderly-statin-users-following-acute-coronary-syndromes-in-canada
#20
David A Alter, Jack V Tu, Maria Koh, Cynthia A Jackevicius, Peter C Austin, Mohammad R Rezai, R Sacha Bhatia, Sharon Johnston, Jacob A Udell, Dennis T Ko
BACKGROUND: The extent to which outcome benefits may be achieved through the implementation of aggressive low-density lipoprotein (LDL) cholesterol targets in real world settings remains unknown, especially among elderly statin users following acute coronary syndromes. METHODS AND RESULTS: A population-based cohort study consisting of 19 544 post-acute coronary syndrome statin-users aged ≥66 years between January 1, 2017 and March 31, 2014 was used to project the number of adverse outcome events (acute myocardial infarction or death from any cause) that could be prevented if all post-acute coronary syndrome elderly statin users were treated to 1 of 2 LDL cholesterol target levels (≤50 and ≤70 mg/dL)...
May 12, 2018: Journal of the American Heart Association
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