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https://www.readbyqxmd.com/read/28733349/constitutive-ido1-expression-in-human-tumors-is-driven-by-cyclooxygenase-2-and-mediates-intrinsic-immune-resistance
#1
Marc Hennequart, Luc Pilotte, Stefania Cane, Delia Hoffmann, Vincent Stroobant, Etienne De Plaen, Benoît J Van den Eynde
Tumors use various mechanisms to avoid immune destruction. Cyclooxygenase-2 (COX-2) expression may be a driver of immune suppression in melanoma, but the mechanisms involved remain elusive. Here, we show that COX-2 expression drives constitutive expression of indoleamine 2,3-dioxygenase 1 (IDO1) in human tumor cells. IDO1 is an immunosuppressive enzyme that degrades tryptophan. In a series of seven human tumor lines, constitutive IDO1 expression depends on COX-2 and prostaglandin E2 (PGE2), which, upon autocrine signaling through the EP receptor, activates IDO1 via the PKC and PI3K pathways...
July 21, 2017: Cancer Immunology Research
https://www.readbyqxmd.com/read/28730562/therapeutical-approaches-to-paroxysmal-hemicrania-hemicrania-continua-and-short-lasting-unilateral-neuralgiform-headache-attacks-a-critical-appraisal
#2
Carlo Baraldi, Lanfranco Pellesi, Simona Guerzoni, Maria Michela Cainazzo, Luigi Alberto Pini
BACKGROUND: Hemicrania continua (HC), paroxysmal hemicrania (PH) and short lasting neuralgiform headache attacks (SUNCT and SUNA) are rare syndromes with a difficult therapeutic approach. The aim of this review is to summarize all articles dealing with treatments for HC, PH, SUNCT and SUNA, comparing them in terms of effectiveness and safety. METHODS: A survey was performed using the pubmed database for documents published from the 1st January 1989 onwards. All types of articles were considered, those ones dealing with symptomatic cases and non-English written ones were excluded...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28728606/levels-of-serum-biomarkers-from-a-two-year-multicentre-trial-are-associated-with-treatment-response-on-knee-osteoarthritis-cartilage-loss-as-assessed-by-magnetic-resonance-imaging-an-exploratory-study
#3
Johanne Martel-Pelletier, Jean-Pierre Raynauld, François Mineau, François Abram, Patrice Paiement, Philippe Delorme, Jean-Pierre Pelletier
BACKGROUND: There is an obvious need to identify biomarkers that could predict patient response to an osteoarthritis (OA) treatment. This post hoc study explored in a 2-year randomized controlled trial in patients with knee OA, the likelihood of some serum biomarkers to be associated with a better response to chondroitin sulfate in reducing cartilage volume loss. METHODS: Eight biomarkers were studied: hyaluronic acid (HA), C reactive protein (CRP), adipsin, leptin, N-terminal propeptide of collagen IIα (PIIANP), C-terminal crosslinked telopeptide of type I collagen (CTX-1), matrix metalloproteinase-1 (MMP-1), and MMP-3...
July 20, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/28727906/potential-of-telmisartan-in-the-treatment-of-benign-prostatic-hyperplasia
#4
Ismail Ogunbayode Ishola, Charles C Anunobi, Kehinde Habeeb Tijani, Olasunmbo Afolayan, Victoria U Udokwu
Benign prostatic hyperplasia (BPH) is a common health problem in aging men. This study was carried out to investigate the protective effect of telmisartan on testosterone induced-BPH in rats. Fifty-four male Wistar rats (200 - 250g) were randomly divided into 9 groups (n =6) and orally treated for 28 consecutive days: group 1- vehicle normal, olive oil (10 ml/kg); group 2- BPH model control (10 ml/kg); groups 3-5 - telmisartan (5, 10 or 20 mg/kg, respectively); group 6- pioglitazone (20 mg/kg); group 7- celecoxib (20 mg/kg); group 8- combination of telmisartan (5 mg/kg) and pioglitazone (20 mg/kg); group 9- combination of telmisartan (5 mg/kg) and celecoxib (20 mg/kg)...
July 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28720504/synthesis-of-novel-hybrids-of-pyrazole-and-coumarin-as-dual-inhibitors-of-cox-2-and-5-lox
#5
Fa-Qian Shen, Zhong-Chang Wang, Song-Yu Wu, Shen-Zhen Ren, Ruo-Jun Man, Bao-Zhong Wang, Hai-Liang Zhu
In our previous study, we designed a series of pyrazole derivatives as novel COX-2 inhibitors. In order to obtain novel dual inhibitors of COX-2 and 5-LOX, herein we designed and synthesized 20 compounds by hybridizing pyrazole with substituted coumarin who was reported to exhibit 5-LOX inhibition to select potent compounds using adequate biological trials sequentially including selective inhibition of COX-2 and 5-LOX, anti-proliferation in vitro, cells apoptosis and cell cycle. Among them, the most potent compound 11g (IC50=0...
July 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28718684/role-of-gsk-3%C3%AE-in-regulation-of-canonical-wnt-%C3%AE-catenin-signaling-and-pi3-k-akt-oncogenic-pathway-in-colon-cancer
#6
Shelly Jain, Preety Ghanghas, Chandan Rana, S N Sanyal
Non-steroidal anti-inflammatory drugs (NSAIDs) are emerging as novel chemopreventive agents because of their ability in blocking cellular proliferation, and thereby tumor development, and also by promoting apoptosis. GSK-3β, a serine threonine kinase and a negative regulator of the oncogenic Wnt/β-catenin signaling pathway, plays a critical role in the regulation of oncogenesis. Celecoxib and etoricoxib, the two cyclooxygenase-2 (COX-2) selective NSAIDs, and Diclofenac, a preferential COX-2 inhibitory NSAID, had shown uniformly the chemopreventive and anti-neoplastic effects in the early stage of colon cancer by promoting apoptosis as well as an over-expression of GSK-3β while down-regulating the PI3-K/Akt oncogenic pathway...
July 18, 2017: Cancer Investigation
https://www.readbyqxmd.com/read/28713941/additive-antitumor-effects-of-celecoxib-and-simvastatin-on-head-and-neck-squamous-cell-carcinoma-in%C3%A2-vitro
#7
Thomas Gehrke, Agmal Scherzad, Stephan Hackenberg, Pascal Ickrath, Philipp Schendzielorz, Rudolf Hagen, Norbert Kleinsasser
Lipid-lowering statins as well as non-steroidal anti-inflammatory drugs (NSAIDs) have been reported to possess cancer-protective effects in many epidemiologic cohort studies. However, the underlying mechanisms of these findings are mostly unknown. To evaluate possible additive antitumor effects of statins and NSAIDs in vitro, PJ-41 and HLaC78 head and neck squamous cell carcinoma cells (HNSCC) were treated with 40 µM celecoxib, 50 µM simvastatin or a combination of both. Analysis of tumor viability, proliferation, apoptosis, cell cycle changes and secretion of interleukin-6 (IL-6) and interleukin-8 (IL-8) was conducted via MTT assay, Annexin V-propidium iodide test, cell cycle analysis, colony assay and enzyme-linked immunosorbent assay (ELISA)...
July 10, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28704574/unveiling-the-target-promiscuity-of-pharmacologically-active-compounds-in-silico
#8
Petra Schneider, Gisbert Schneider
Drug discovery is governed by the desire to find ligands with defined modes of action. It has been realized that even designated selective drugs may have more macromolecular targets than is commonly thought. Consequently, it will be mandatory to consider multi-target activity for the design of future medicines. Computational models assist medicinal chemists in this effort by helping to eliminate unsuitable lead structures and spot undesired drug effects early in the discovery process. Here, we present a straightforward computational method to find previously unknown targets of pharmacologically active compounds...
July 13, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28697127/celecoxib-oral-administration-for-prevention-of-post-endoscopic-retrograde-cholangiopancreatography-pancreatitis-a-randomized-prospective-trial
#9
Kunihiro Kato, Masatsugu Shiba, Yuki Kakiya, Hirotsugu Maruyama, Masaki Ominami, Shusei Fukunaga, Satoshi Sugimori, Yasuaki Nagami, Toshio Watanabe, Kazunari Tominaga, Yasuhiro Fujiwara
OBJECTIVES: Rectal nonsteroidal anti-inflammatory drugs have reported promising prophylactic activity in post-endoscopic retrograde cholangiopancreatography (ERCP) pancreatitis (PEP). Conversely, cyclooxygenase-2 enzyme has been suggested to contribute to experimental acute pancreatitis. The aim of this study was to evaluate the efficacy of oral administration of celecoxib, a cyclooxygenase-2 inhibitor, for the prevention of PEP. METHODS: We performed a prospective randomized controlled study...
August 2017: Pancreas
https://www.readbyqxmd.com/read/28682418/effects-of-epoxyeicosatrienoic-acids-eets-on-retinal-macular-degeneration-in-rat-models
#10
F Mei, J-G Wang, Z-J Chen, Z-L Yuan
OBJECTIVE: Here we use a rat model to investigate the effects of epoxyeicosatrienoic acids (EETs) on retinal macular degeneration along with pathological and physiological mechanisms of the disease. MATERIALS AND METHODS: Six choroidal neovascularization (CNV) rats were created with a 532 nm laser and received intravitreal injections of EETs in both eyes. On day 1, 3, 7 and 14 after photocoagulation, the thickness and area of CNV were measured with HE staining and choroidal flat mounts...
June 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28676124/evaluation-of-rational-nonsteroidal-anti-inflammatory-drugs-and-gastro-protective-agents-use-association-rule-data-mining-using-outpatient-prescription-patterns
#11
Oraluck Pattanaprateep, Mark McEvoy, John Attia, Ammarin Thakkinstian
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) and gastro-protective agents should be co-prescribed following a standard clinical practice guideline; however, adherence to this guideline in routine practice is unknown. This study applied an association rule model (ARM) to estimate rational NSAIDs and gastro-protective agents use in an outpatient prescriptions dataset. METHODS: A database of hospital outpatients from October 1st, 2013 to September 30th, 2015 was searched for any of following drugs: oral antacids (A02A), peptic ulcer and gastro-oesophageal reflux disease drugs (GORD, A02B), and anti-inflammatory and anti-rheumatic products, non-steroids or NSAIDs (M01A)...
July 4, 2017: BMC Medical Informatics and Decision Making
https://www.readbyqxmd.com/read/28672892/the-mediation-of-interleukin-17-and-chemokine-ligand-2-in-pelvic-pain-of-experimental-autoimmune-prostatitis
#12
Xiaodong Liu, Shicheng Fan, Mingxing Zheng, Jianheng Chen, Jianhua Zhang, Hao Li
The present study aimed to determine the expression and mediation of interleukin-17 (IL-17) and chemokine ligand 2 (CCL2) in a rat model with experimental autoimmune prostatitis (EAP). A total of 44 Sprague Dawley (SD) rats were used in the present study. Of these, a total of 20 two-month-old SD rats were randomly divided into a normal control (n=10) and a model group (EAP group, n=10). The remaining 24 two-month old SD rats were treated in the same way as EAP rats and subsequently randomly divided into a tacrolimus group (n=8), a celecoxib group (n=8) and a normal saline (NS) control group (n=8)...
July 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28669741/design-synthesis-and-biological-evaluation-of-some-novel-indolizine-derivatives-as-dual-cyclooxygenase-and-lipoxygenase-inhibitor-for-anti-inflammatory-activity
#13
Sushant K Shrivastava, Pavan Srivastava, Robin Bandresh, Prabhash Nath Tripathi, Avanish Tripathi
Some novel indolizine derivatives were synthesized by bioisosteric modification of imidazo[1,2-a]pyridine for anti-inflammatory activity. The physicochemical characterization and structure of compounds were elucidated by state of the art spectroscopic technique. Induced fit docking was performed for initial screening to elucidate the interactions with corresponding amino acids of cyclooxygenase (COX-1, COX-2) and lipoxygenase (LOX) enzymes. The target compounds 53-60 were then evaluated against in vivo carrageenan and arachidonic acid induced rat paw edema models for anti-inflammatory activity...
June 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28668885/interactive-analysis-of-tx-1123-with-cyclo-oxygenase-design-of-cox2-selective-tx-analogs
#14
Kazuto Ohkura, Yohei Tatematsu, Yuki Kawaguchi, Yoshihiro Uto, Hitoshi Hori
BACKGROUND: To date, two cyclo-oxygenase (COX) isoforms, COX1 and COX2, have been identified. In the present study, the COX-inhibitory activities of TX-1123 derivatives with the 2-hydroxyarylidene-4-cyclopentene-1,3-dione structure were examined, and the binding profiles of TX-1123 to COXs were analyzed using docking simulations. MATERIALS AND METHODS: X-Ray data on COX1 [protein data bank (PDB) ID=1PGG] and COX2 (PDB ID=3LN1) were used for molecular interactive simulations...
July 2017: Anticancer Research
https://www.readbyqxmd.com/read/28666869/celecoxib-induced-apoptosis-against-different-breast-cancer-cell-lines-by-down-regulated-nf-%C3%AE%C2%BAb-pathway
#15
Guanying Wang, Jian Li, Lingxiao Zhang, Shangke Huang, Xinhan Zhao, Xiaoai Zhao
Inducible cyclooxgenase-2 (COX-2) is commonly overexpressed in breast tumors and is a target for cancer therapy. Here, we studied the effect of Celecoxib, a COX-2 inhibitor on two molecular breast cancer subtypes-MDA-MB-231 and SK-BR-3. Firstly, MDA-MB-231 and SK-BR-3 cells were treated with various concentration of Celecoxib for 24 and 48 h. Celecoxib-inhibition of NF-κB (p52 and p65) transcriptional activity and effect of Caspase 3 pathway were examined by western blotting. COX-2 mRNA was assessed by RT-PCR...
June 27, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28666323/exploring-the-in-vitro-potential-of-celecoxib-derivative-ar-12-as-an-effective-antiviral-compound-against-four-dengue-virus-serotypes
#16
Pouya Hassandarvish, Adrian Oo, Amin Jokar, Alexander Zukiwski, Stefan Proniuk, Sazaly Abu Bakar, Keivan Zandi
Objectives: With no clinically effective antiviral options available, infections and fatalities associated with dengue virus (DENV) have reached an alarming level worldwide. We have designed this study to evaluate the efficacy of the celecoxib derivative AR-12 against the in vitro replication of all four DENV serotypes. Methods: Each 24-well plate of Vero cells infected with all four DENV serotypes, singly, was subjected to treatments with various doses of AR-12...
June 28, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28663087/superiority-of-aromatase-inhibitor-and-cyclooxygenase-2-inhibitor-combined-delivery-hyaluronate-targeted-versus-pegylated-protamine-nanocapsules-for-breast-cancer-therapy
#17
Ahmed O Elzoghby, Shaimaa K Mostafa, Maged W Helmy, Maha A ElDemellawy, Salah A Sheweita
Despite several reports have revealed the beneficial effect of co-administration of COX-2 inhibitors with aromatase inhibitors in managing postmenopausal breast cancer; no nanocarriers for such combined delivery have been developed till now. Therefore, protamine nanocapsules (PMN-NCs) have been developed to co-deliver letrozole (LTZ) that inhibits aromatase-mediated estrogen biosynthesis and celecoxib (CXB) that synergistically inhibits aromatase expression. Inspired by the CD44-mediated tumor targeting ability of hyaluronate (HA), we developed HA-coated PMN-NCs (HA-NCs) via electrostatic layer-by-layer assembly...
June 27, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28658301/the-effect-of-anti-rheumatic-medications-for-coronary-artery-diseases-risk-in-patients-with-rheumatoid-arthritis-might-be-changed-over-time-a-nationwide-population-based-cohort-study
#18
Yao-Min Hung, Lichi Lin, Chyong-Mei Chen, Jeng-Yuan Chiou, Yu-Hsun Wang, Paul Yung-Pou Wang, James Cheng-Chung Wei
OBJECTIVES: To determine whether anti-rheumatic drug usage is associated with risk of coronary artery diseases (CAD) in incident Rheumatoid Arthritis (RA) patients. METHODS: Data were obtained from the Taiwan National Health Insurance Research Database. The study cohort comprised 6260 patients who were newly diagnosed with RA between 2001-2010. The study endpoint was occurrence of CAD according to the ICD-9-CM codes. We used the WHO Defined Daily Dose (DDD) as a tool to assess the drugs exposure...
2017: PloS One
https://www.readbyqxmd.com/read/28657872/desmoid-tumors-and-celecoxib-with-sorafenib
#19
LETTER
Nicolas Benech, Thomas Walter, Jean-Christophe Saurin
New England Journal of Medicine, Volume 376, Issue 26, Page 2595-2597, June 2017.
June 29, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28654916/inhibition-of-cox2-enhances-the-chemosensitivity-of-dichloroacetate-in-cervical-cancer-cells
#20
Bo Li, Xinzhe Li, Haojun Xiong, Peng Zhou, Zhenhong Ni, Teng Yang, Yan Zhang, Yijun Zeng, Jintao He, Fan Yang, Nan Zhang, Yuting Wang, Yingru Zheng, Fengtian He
Dichloroacetate (DCA), a traditional mitochondria-targeting agent, has shown promising prospect as a sensitizer in fighting against malignancies including cervical cancer. But it is unclear about the effect of DCA alone on cervical tumor. Moreover, previous reports have demonstrated that the increased cyclooxygenase-2 (COX2) expression is associated with chemoresistance and poor prognosis of cervical cancer. However, it is still unknown whether COX2 can affect the sensitivity of DCA in cervical cancer cells...
June 16, 2017: Oncotarget
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