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https://www.readbyqxmd.com/read/28080073/copper-mediated-domino-cyclization-trifluoromethylation-deprotection-with-tmscf3-synthesis-of-4-trifluoromethyl-pyrazoles
#1
Quande Wang, Lisi He, Kin Keung Li, Gavin Chit Tsui
A copper-mediated synthesis of 4-(trifluoromethyl)pyrazoles is described. In one step from readily accessible α,β-alkynic tosylhydrazones, a remarkable domino sequence of cyclization, trifluoromethylation, and detosylation takes place to furnish the 4-CF3 N-H pyrazole cores with good functional group compatibility. The reaction conditions are mild and convenient, at room temperature in air, using the commercially available trifluoromethyltrimethylsilane (TMSCF3) as the CF3 source. The method can be applied to the synthesis of a 4-CF3 analogue of the anti-inflammatory drug celecoxib...
January 12, 2017: Organic Letters
https://www.readbyqxmd.com/read/28079986/establishment-of-an-in-vitro-3-d-model-for-cartilage-damage-in-rheumatoid-arthritis-ra
#2
Yvonne Peck, Li Ting Leom, Pei Fen Patricia Low, Dong-An Wang
Rheumatoid arthritis (RA) is a chronic inflammatory disease that leads to progressive joint destruction. To further understand the process of rheumatoid cartilage damage, an in vitro model consisting of an interactive tri-culture of synovial fibroblasts (SFs), LPS-stimulated macrophages and a primary chondrocyte-based tissue engineered construct was established. The tissue engineered construct has a similar composition to human cartilage, which are rich in collagen type II and proteoglycans. Data generated from this model revealed that healthy chondrocytes were activated in the presence of SFs and macrophages...
January 12, 2017: Journal of Tissue Engineering and Regenerative Medicine
https://www.readbyqxmd.com/read/28078603/a-comparison-of-the-anti-inflammatory-effects-of-cis-9-trans-11-conjugated-linoleic-acid-to-celecoxib-in-the-collagen-induced-arthritis-model
#3
Jake M Olson, Alexander W Haas, Jennifer Lor, Holly S McKee, Mark E Cook
Cyclooxygenase (COX)-2 inhibitors, such as celecoxib, for chronic inflammatory disease are associated with adverse health events, while cis-9, trans-11 (c9t11) conjugated linoleic acid (CLA) is anti-inflammatory without adverse events attributed to pure intake. Mechanistically, celecoxib and c9t11 disrupt the arachidonic acid cascade; however, the equivalency of anti-inflammatory effects between these compounds is unknown. Therefore, to test the hypothesis that 0.5% dietary c9t11 reduces inflammation equivalently to a celecoxib dose intended to treat rheumatoid arthritis (RA; 5 mg/kg bw), arthritic mice received diets containing one of the following supplements: 1% corn oil (CO, w/w), 0...
January 11, 2017: Lipids
https://www.readbyqxmd.com/read/28078252/the-evaluation-of-the-effect-of-herbal-extract-on-osteoarthritis-in-vitro-and-in-vivo-study
#4
Jaeyong Kim, Siyoung Yang, Chul-Yung Choi
In this study, the anti-osteoarthritis effects of Cynanchum wilfordii, Phlomis umbrosa, and Angelica gigas extract (CPAE), observed and confirmed in previously clinical studies were further investigated by in vitro and in vivo studies. Anabolic biomarkers related to healthy cartilage maintenance, such as aggrecan, type II collagen α-1 (Col2a1), sex determining region Y-box-9 (Sox-9), and catabolic biomarkers related to osteoarthritis, such as cyclooxygenase-2 (Cox-2), matrix metalloproteinase-13 (Mmp13), and nuclear factor kappa-light-chain-enhancer of activated B cells (Nfκb), were evaluated by quantitative reverse transcriptase polymerase chain reaction and reporter gene assay...
December 2016: Preventive Nutrition and Food Science
https://www.readbyqxmd.com/read/28076502/carcinogenesis-in-rats-subjected-to-a-new-model-ureterosigmoidostomy-and-treated-with-l-lysine
#5
Alessandra Marques Dos Santos, Joao Paulo Ferreira Coelho, Camila de Carvalho Juanes, Rafael Barbosa de Azevedo, Nayanna de Oliveira Ramos Melo, Francisco Vagnaldo Fechine Jamacaru, Conceição Aparecida Dornelas
PURPOSE: To evaluate the effects of L-lysine on the intestinal and urothelial epithelium of rats subjected to ureterosigmoidostomy (new model for surgical carcinogenesis). METHODS: Forty-two rats, 9 weeks of age, were divided into 6 groups. Animals in groups A, B, C were subjected to ureterosigmoidostomy (US) and treated with L-lysine, celecoxib and H2O, respectively. Groups D, E and F (non-operated controls) received L-lysine, celecoxib and H2O, respectively. The L-lysine dose was 150 mg/kg and that of celecoxib was 20 mg/kg...
December 2016: Acta Cirúrgica Brasileira
https://www.readbyqxmd.com/read/28072731/focal-segmental-glomerulosclerosis-lagged-behind-the-onset-of-rheumatoid-arthritis-by-7-years-a-case-report-and-literature-review
#6
Yang Liu, Hong-Yan Wen, Li-Hua Wang, Chen Wang
INTRODUCTION: The co-existence of focal segmental glomerulosclerosis (FSGS) and rheumatoid arthritis (RA), presenting either together or in succession, is very rare. A variety of histopathological features in the clinical renal disease may occur in RA. Only 8 studies have previously reported this poorly understood connection. CLINICAL FINDINGS/DIAGNOSES: A case of a 54-year-old male with RA lasting for more than 7 years developed cheirarthritis as the first signs...
January 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28057407/bifunctional-conjugates-with-potent-inhibitory-activity-towards-cyclooxygenase-and-histone-deacetylase
#7
Idris Raji, Fatima Yadudu, Emily Janeira, Shaghayegh Fathi, Lindsey Szymczak, James Richard Kornacki, Kensei Komatsu, Jian-Dong Li, Milan Mrksich, Adegboyega K Oyelere
We herein disclose a series of compounds with potent inhibitory activities towards histone deacetylases (HDAC) and cyclooxygenases (COX). These compounds potently inhibited the growth of cancer cell lines consistent with their anti-COX and anti-HDAC activities. While compound 2b showed comparable level of COX-2 selectivity as celecoxib, compound 11b outperformed indomethacin in terms of selectivity towards COX-2 relative to COX-1. An important observation with our lead compounds (2b, 8, 11b, and 17b) is their enhanced cytotoxicity towards androgen dependent prostate cancer cell line (LNCaP) relative to androgen independent prostate cancer cell line (DU-145)...
December 24, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28057325/design-synthesis-and-biological-screening-of-some-novel-celecoxib-and-etoricoxib-analogs-with-promising-cox-2-selectivity-anti-inflammatory-activity-and-gastric-safety-profile
#8
Shahinda S R Alsayed, Heba A H Elshemy, Mohamed A Abdelgawad, Mahmoud S Abdel-Latif, Khaled R A Abdellatif
Two new series of 4,6-diaryl-3-cyanopyridine 4a-r and 1,3,5-triaryl-2-pyrazolines 6a-f and were prepared. The new compounds were evaluated for their in vitro COX-2 selectivity and in vivo anti-inflammatory activity. Compounds 4o,r and 6d,f had moderate to high selectivity index (S.I.) compared to celecoxib (selectivity indexes of 4.5, 3.14, 4.79 and 3.21, respectively) and also, showed in vivo anti-inflammatory activity approximately equal to or higher than celecoxib (edema inhibition %=60.5, 64.5, 59.3 and 59...
December 26, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28054752/opposite-modulatory-effects-of-selective-and-non-selective-cyclooxygenase-inhibition-on-cardiovascular-and-autonomic-consequences-of-cyclosporine-in-female-rats
#9
Karim S Ibrahim, Ahmed F El-Yazbi, Hanan M El-Gowelli, Mahmoud M El-Mas
Non-steroidal anti-inflammatory drugs (NSAIDs) and the immunosuppressant drug cyclosporine (CSA) are concurrently administered in arthritis. Here, we investigated whether diclofenac (non-selective inhibitor of cyclooxygenase-1 and 2, COX-1/COX-2), celecoxib (selective COX-2 inhibitor) or SC560 (selective COX-1 inhibitor) interact variably with hemodynamic effects of CSA in conscious female rats. Changes caused by CSA (10 mg/kg i.v.) in blood pressure (BP), heart rate (HR), HR variability (HRV) and myocardial contractility were assessed in absence and presence of individual NSAIDs (10 mg/kg each)...
January 5, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28053596/celecoxib-enhances-anticancer-effect-of-cisplatin-and-induces-anoikis-in-osteosarcoma-via-pi3k-akt-pathway
#10
Bing Liu, Shigui Yan, Liyan Qu, Jian Zhu
BACKGROUND: COX-2, an inducible enzyme, is associated with inflammatory diseases and carcinogenesis. Overexpression of COX-2 occurs in many human malignancies, including osteosarcoma. COX-2 positivity is form 67 to 92% in osteosarcoma, and COX-2 expresses 141-fold more in cancer stem cell spheres than daughter adherent cells. In our study, we have reported that celecoxib, a cyclooxygenase-2 inhibitor, induces apoptosis in human osteosarcoma cell line MG-63 via down-regulation of PI3K/Akt...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/28038322/synthesis-anti-inflammatory-cyclooxygenases-inhibitions-assays-and-histopathological-study-of-poly-substituted-1-3-5-triazines-confirmation-of-regiospecific-pyrazole-cyclization-by-hmbc
#11
Heba A H Elshemy, Eman K A Abdelall, Amany A Azouz, Abeer Moawad, Waleed A M Ali, Nesreen M Safwat
Three novel triazines series were prepared. These series are pyrazolines (4a and 4b), pyrazoles (6a, 6b and 8a-d) and isoxazoles (7a and 7b). Such series were designed as COX-2 inhibitors. All compounds were characterized by using spectroscopic methods and elemental analysis. Regarding COX-2, compounds 5b, 4a and 3b were the most active with IC50 in the range of 0.55-0.87 μM. Most of synthesized compounds were relatively more potent to celecoxib (0.78 μM), diclofenac (2.94 μM) and indomethacin (7.24 μM)...
December 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28035420/argininosuccinate-lyase-interacts-with-cyclin-a2-in-cytoplasm-and-modulates-growth-of-liver-tumor-cells
#12
Yu-Hsuan Hung, Hau-Lun Huang, Wei-Ching Chen, Meng-Chi Yen, Chien-Yu Cho, Tzu-Yang Weng, Chih-Yang Wang, Yi-Ling Chen, Li-Tzong Chen, Ming-Derg Lai
Arginine is a critical amino acid in specific cancer types including hepatocellular carcinoma (HCC) and melanoma. Novel molecular mechanisms and therapeutic targets in arginine metabolism-mediated cancer formation await further identification. Our laboratory has previously demonstrated that arginine metabolic enzyme argininosuccinate lyase (ASL) promoted HCC formation in part via maintenance of cyclin A2 protein expression and arginine production for channeling to nitric oxide synthase. In this study, we investigated the mechanism by which ASL regulates cyclin A2 expression...
December 23, 2016: Oncology Reports
https://www.readbyqxmd.com/read/28034279/inhibition-of-a%C3%AE-1-42-oligomerization-fibrillization-and-acetylcholinesterase-activity-by-some-anti-inflammatory-drugs-an-in-vitro-study
#13
Hamendra Singh Parmar, Anshul Assaiya, Renuka Agrawal, Shalini Tiwari, Iram Mufti, Neha Jain, Elangovan Manivannan, Tushar Banerjee, Anil Kumar
Background-Number of contradictory reports are available on the effects of anti-inflammatory drugs on Alzheimer's disease (AD) including beneficial, adverse and stage dependent effects. We provide insights of the effects exert by some anti-inflammatory drugs on the chemistry of AD. Methods-Three different doses of dexamethasone (0.015, 0.030, 0.060 µM), piroxicam (5, 7.5, 10 µM), indomethacin (1, 1.25, 1.50 µM), diclofenac (0.6, 0.8, 1.0 µM), aspirin (90, 120, 150 µM) and celecoxib (30, 45, 60 µM) were used...
December 29, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28031712/minocycline-and-celecoxib-as-adjunctive-treatments-for-bipolar-depression-a-study-protocol-for-a-multicenter-factorial-design-randomized-controlled-trial
#14
Muhammad I Husain, Imran B Chaudhry, Munir M Hamirani, Fareed A Minhas, Ajmal Kazmi, John Hodsoll, Peter M Haddad, John Fw Deakin, Nusrat Husain, Allan H Young
BACKGROUND: Evidence suggests that the use of anti-inflammatory agents may improve depressive symptoms in patients with bipolar affective disorder. However, there are few well-designed clinical trials demonstrating the efficacy of these newer treatment strategies. PATIENTS AND METHODS: This is a multicenter, 3-month, randomized, placebo-controlled, double-blind, factorial design trial of minocycline and/or celecoxib added to TAU for the treatment of depressive symptoms in patients experiencing a DSM-5 bipolar I or II disorder and a current major depressive episode...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28027365/celecoxib-similar-to-2-nsaids-for-cardiovascular-safety
#15
Anita Slomski
No abstract text is available yet for this article.
December 27, 2016: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/28025308/2-5-dimethyl-celecoxib-extends-drosophila-life-span-via-a-mechanism-that-requires-insulin-and-target-of-rapamycin-signaling
#16
Qi Wu, Ting Lian, Xiaolan Fan, Chaochun Song, Uma Gaur, Xueping Mao, Deying Yang, Matthew D W Piper, Mingyao Yang
The search for antiaging drugs is a key component of gerontology research. A few drugs with positive effects on life span in model organisms have been found. Here, we report that 2,5-dimethyl-celecoxib, a derivative of the anti-inflammatory drug celecoxib, can extend Drosophila life span and delay aging by a mechanism involving insulin signaling and target of rapamycin signaling. Importantly, its positive effects were apparent when the treatment window was restricted to the beginning of life or the later half...
December 26, 2016: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
https://www.readbyqxmd.com/read/28025218/non-steroidal-anti-inflammatory-drug-use-is-associated-with-increased-risk-of-out-of-hospital-cardiac-arrest-a-nationwide-case-time-control-study
#17
Kathrine B Sondergaard, Peter Weeke, Mads Wissenberg, Anne-Marie Schjerning Olsen, Emil L Fosbol, Freddy K Lippert, Christian Torp-Pedersen, Gunnar H Gislason, Fredrik Folke
AIMS: Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used and have been associated with increased cardiovascular risk. Nonetheless, it remains unknown whether use of NSAIDs is associated with out-of-hospital cardiac arrest (OHCA). METHODS AND RESULTS: From the nationwide Danish Cardiac Arrest Registry, all persons with OHCA during 2001-2010 were identified. NSAID use 30 days before OHCA was categorized as follows: diclofenac, naproxen, ibuprofen, rofecoxib, celecoxib, and other...
December 26, 2016: European Heart Journal. Cardiovascular Pharmacotherapy
https://www.readbyqxmd.com/read/28024614/anomalous-dissolution-behavior-of-celecoxib-in-pvp-isomalt-solid-dispersions-prepared-using-spray-drier
#18
Roya Ghanavati, Azade Taheri, Alireza Homayouni
Celecoxib is a COX II inhibitor NSAID which is used for joint pains, rheumatoid arthritis and osteoarthritis, however due to its poor water solubility it shows very low oral bioavailability. Using solid dispersion formulations is one of the most promising strategies to increase solubility of poorly water soluble drugs. The purpose of this study is dissolution enhancement of celecoxib by preparation of solid dispersions via spray drying technique using PVP and Isomalt as hydrophilic carriers. Different ratios of celecoxib, Isomalt and PVP K30 (7:3:0, 5:5:0, 3:7:0, 1:9:0 and 3:5:2, 3:2:5) were prepared from 2% hydroalcoholic solutions (70:30 ethanol:water) using spray drier...
March 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28024294/celecoxib-administration-reduced-mortality-mesenteric-hypoperfusion-aortic-dysfunction-and-multiple-organ-injury-in-septic-rats
#19
Erdem Kamil Ozer, Mustafa Tugrul Goktas, Ibrahim Kilinc, Hulagu Bariskaner, Ceyhan Ugurluoglu, Alper Bektas Iskit
BACKGROUND: The cyclooxygenase (COX)-2 overexpression is associated with vascular injury and multiple organ failure in sepsis. However, constitutive COX-1 and basal COX-2 expressions have physiological effects. We aimed to investigate the effects of partial and selective COX-2 inhibition without affecting constitutive COX-1 and basal COX-2 activities by celecoxib on mesenteric artery blood flow (MABF), vascular reactivity, oxidative and inflammatory injuries, and survival in septic rats accomplished by cecal ligation and puncture (CLP)...
December 23, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28019014/non-steroidal-anti-inflammatory-drug-induced-cardiovascular-adverse-events-a-meta-analysis
#20
REVIEW
B R Gunter, K A Butler, R L Wallace, S M Smith, S Harirforoosh
WHAT IS KNOWN AND OBJECTIVE: Although non-steroidal anti-inflammatory drugs (NSAIDs) have been studied in randomized, controlled trials and meta-analyses in an effort to determine their cardiovascular (CV) risks, no consensus has been reached. These studies continue to raise questions, including whether cyclooxygenase-2 (COX-2) selectivity plays a role in conferring CV risk. We performed a meta-analysis of current literature to determine whether COX-2 selectivity leads to an increased CV risk...
February 2017: Journal of Clinical Pharmacy and Therapeutics
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