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Celecoxib

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https://www.readbyqxmd.com/read/29341436/a-novel-nir-fluorescent-probe-for-monitoring-cox-2-in-inflammation-and-tumor
#1
Qi Zhang, Zhihao Han, Ji Tao, Wancun Zhang, Ping Li, Liping Tang, Yueqing Gu
Targeting COX-2 for molecular imaging is an attractive approach applicable for its overexpression in inflammation and many malignancies. Herein, for monitoring COX-2, we synthesize a specific COX-2 probe CMP, based on celecoxib and a water-soluble near-infrared dye MPA. Its high affinity for binding to COX-2 is verified by molecular docking, dynamics simulation and inhibition assay. At cellular level, CMP selectively accumulates in cytoplasm of COX-2-positive cells. In vivo assays, probe guided-imaging in inflamed or cancerous tissues confirms that CMP can bind to the locally endogenic COX-2 and exhibit intense fluorescence...
January 17, 2018: Journal of Biophotonics
https://www.readbyqxmd.com/read/29332199/analysis-of-the-data-on-pregnancy-and-lactation-provided-by-patient-information-leaflets-of-anti-rheumatic-drugs-in-argentina
#2
Miguel Ormaza Sabando, Maira Arias Saavedra, Gabriel Sequeira, Eduardo Kerzberg
To analyse the level of consistency and updating of the information on pregnancy and lactation provided by patient information leaflets (PILs) of the antirheumatic drugs approved in Argentina. Inconsistencies between the 2016 EULAR Task Force recommendations on the use of anti-rheumatic drugs during pregnancy and lactation and the information provided by PILs of the same drugs approved in Argentina were analysed along with inconsistencies within the PILs of different registered trademarks of these drugs. Eighty-eight PILs of 32 drugs were analysed...
January 13, 2018: Rheumatology International
https://www.readbyqxmd.com/read/29329257/synthesis-and-pharmacological-activities-of-pyrazole-derivatives-a-review
#3
REVIEW
Khalid Karrouchi, Smaail Radi, Youssef Ramli, Jamal Taoufik, Yahia N Mabkhot, Faiz A Al-Aizari, M'hammed Ansar
Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety...
January 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29327156/effectiveness-of-celecoxib-for-pain-relief-and-antipyresis-in-second-trimester-medical-abortions-with-misoprostol-a-randomized-controlled-trial
#4
Hatern Tintara, Peangpailin Voradithi, Thanapan Choobun
PURPOSE: To evaluate the effectiveness of celecoxib for pain relief and antipyresis during second trimester abortion using sublingual misoprostol. METHODS: Fifty-six pregnant women of gestational age 14-24 weeks were randomly assigned in a double-blind randomized controlled trial to receive 400 mg of celecoxib or placebo just before sublingual administration of misoprostol 400 µg every 6 h. Pain and body temperature (BT) were assessed every 1 h until the abortion or 24 h after the first dose of misoprostol...
January 11, 2018: Archives of Gynecology and Obstetrics
https://www.readbyqxmd.com/read/29325910/corrigendum-to-additional-effect-of-metformin-and-celecoxib-against-lipid-dysregulation-and-adipose-tissue-inflammation-in-high-fat-fed-rats-with-insulin-resistance-and-fatty-liver-eur-j-pharmacol-789-2016-60-67
#5
Chieh-Hua Lu, Yi-Jen Hung, Po-Shiuan Hsieh
No abstract text is available yet for this article.
January 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29316651/cpt-11-induced-delayed-diarrhea-develops-via-reduced-aquaporin-3-expression-in-the-colon
#6
Risako Kon, Yuika Tsubota, Moe Minami, Saki Kato, Yukari Matsunaga, Hiroshi Kimura, Yuta Murakami, Tetsuya Fujikawa, Ryoya Sakurai, Rei Tomimoto, Yoshiaki Machida, Nobutomo Ikarashi, Kiyoshi Sugiyama
While irinotecan (CPT-11) has a potent anti-cancer effect, it also causes serious diarrhea as an adverse reaction. In this study, we analyzed the pathogenic mechanism of CPT-11-induced delayed diarrhea by focusing on water channel aquaporin-3 (AQP3) in the colon. When rats received CPT-11, the expression level of AQP3 was reduced during severe diarrhea. It was found that the expression levels of inflammatory cytokines and the loss of crypt cells were increased in the colon when CPT-11 was administered. When celecoxib, an anti-inflammatory drug, was concomitantly administered, both the diarrhea and the reduced expression of AQP3 induced by CPT-11 were suppressed...
January 6, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29308684/increase-of-reactive-oxygen-species-in-different-tissues-during-lipopolysaccharide-induced-fever-and-antipyresis-an-electron-paramagnetic-resonance-study
#7
Bruna R B Gomes, Marina Firmino, Jardeson S Jorge, Maria L O Ferreira, Thays M Rodovalho, Simone N Weis, Gloria E P Souza, Paulo C Morais, Marcelo V Sousa, Paulo E N Souza, Fabiane H Veiga-Souza
Fever is a regulated increase in body temperature and a component of the acute-phase response, triggered mainly after the invasion of pathogens in the body. Reactive oxygen species (ROS) are generated during the physiological and pathological processes, and can act as both signaling molecules as well as promoters of oxidative stress. Male Wistar rats, pretreated with oral doses of acetaminophen, celecoxib, dipyrone, or ibuprofen 30 min before an intravenous lipopolysaccharide (LPS) or sterile saline injection, showed a reduced febrile response in all animals tested...
January 8, 2018: Free Radical Research
https://www.readbyqxmd.com/read/29306822/celecoxib-a-cyclooxygenase-2-inhibitor-offers-chemoprevention-against-reproductive-and-neurobehavioural-abnormalities-induced-by-atrazine-in-male-wistar-rats
#8
O E Kale, T O Oyesola, F S Raji
The cyclooxygenase-2/prostanoid pathway (COX-2) serves as a potential therapeutic target in various pathological conditions. Thus, the modulatory effect of celecoxib (CXB), a COX-2 inhibitor, in atrazine-induced toxicity was investigated. Five groups (n = 6 rats per group) of adult male Wistar rats received corn oil (2 ml/kg), atrazine (ATZ, 300 mg/kg) and CXB (5.7 mg/kg) respectively and their combinations via the oral route. Results obtained showed reduced (p < 0.05) sperm motility (25.8%) and counts (27...
December 30, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29306052/celecoxib-prevents-cognitive-impairment-and-neuroinflammation-in-soluble-amyloid-%C3%AE-treated-rats
#9
Emanuela Mhillaj, Maria Grazia Morgese, Paolo Tucci, Anna Furiano, Livio Luongo, Maria Bove, Sabatino Maione, Vincenzo Cuomo, Stefania Schiavone, Luigia Trabace
Recent findings suggest that soluble forms of amyloid-β (sAß) peptide contribute to synaptic and cognitive dysfunctions in early stages of Alzheimer's disease (AD). On the other hand, neuroinflammation and cyclooxygenase-2 (COX-2) enzyme have gained increased interest as key factors involved early in AD, although the signaling pathways and pathophysiologic mechanisms underlying a link between sAß-induced neurotoxicity and inflammation are still unclear. Here, we investigated the effects of selective COX-2 enzyme inhibition on neuropathological alterations induced by sAβ administration in rats...
January 3, 2018: Neuroscience
https://www.readbyqxmd.com/read/29304843/effect-of-cox-2-inhibition-on-tendon-to-bone-healing-and-pge2-concentration-after-anterior-cruciate-ligament-reconstruction
#10
Martin Sauerschnig, Josef Stolberg-Stolberg, Carmen Schmidt, Valerie Wienerroither, Michael Plecko, Karin Schlichting, Carsten Perka, Christian Dynybil
BACKGROUND: Non-steroidal anti-inflammatory drugs are commonly used to reduce pain and inflammation in orthopaedic patients. Selective cyclooxygenase-2 (COX-2) inhibitors have been developed to minimize drug-specific side effects. However, they are suspected to impair both bone and tendon healing. The objective of this study is to evaluate the effect of COX-2 inhibitor administration on tendon-to-bone healing and prostaglandin E (PGE2) concentration. METHODS: Thirty-two New Zealand white rabbits underwent reconstructions of the anterior cruciate ligaments and were randomized into four groups: Two groups postoperatively received a selective COX-2 inhibitor (Celecoxib) on a daily basis for 3 weeks, the two other groups received no postoperative COX-2 inhibitors at all and were examined after three or 6 weeks...
January 5, 2018: European Journal of Medical Research
https://www.readbyqxmd.com/read/29290997/targeting-g-protein-coupled-receptor-related-signaling-pathway-in-a-murine-xenograft-model-of-appendiceal-pseudomyxoma-peritonei
#11
Ashok K Dilly, Brendon D Honick, Yong J Lee, Zong S Guo, Herbert J Zeh, David L Bartlett, Haroon A Choudry
Cancer cells aberrantly express mucins to enhance their survival. Relative chemoresistance of appendiceal pseudomyxoma peritonei (PMP) is attributed to abundant extracellular mucin 2 (MUC2) protein production. We hypothesized that simultaneous MUC2 inhibition and apoptosis induction would be effective against mucinous tumors. In vitro studies were conducted using LS174T cells (MUC2-secreting human colorectal cancer cells), PMP explant tissue, and epithelial organoid cultures (colonoids) derived from mucinous appendix cancers...
December 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/29289887/novel-click-modifiable-thioquinazolinones-as-anti-inflammatory-agents-design-synthesis-biological-evaluation-and-docking-study
#12
Ghandoura Moussa, Rana Alaaeddine, Lynn M Alaeddine, Rasha Nassra, Ahmed S F Belal, Azza Ismail, Ahmed F El-Yazbi, Yasser S Abdel-Ghany, Aly Hazzaa
Click chemistry was used to synthesize a new series of thioquinazolinone molecules equipped with propargyl moiety,1,2,3-triazolyl and isoxazolyl rings. Our design was based on merging pharmacophores previously reported to exhibit COX-2 inhibitory activities to a thioquinazolinone-privileged scaffold. The synthesized compounds were subjected to in vitro cyclooxygenase COX-1/COX-2 and 15-LOX inhibition assays. Compounds 2c, 3b, 3h, 3j, and 3k showed COX-2 inhibition with IC50 (μM) 0.18, 0.19, 0.11, 0.16 and 0...
December 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29282893/autophagy-novel-applications-of-nonsteroidal-anti-inflammatory-drugs-for-primary-cancer
#13
REVIEW
Chen Yu, Wei-Bing Li, Jun-Bao Liu, Jian-Wei Lu, Ji-Feng Feng
In eukaryotic cells, autophagy is a process associated with programmed cell death. During this process, cytoplasmic proteins and organelles are engulfed by double-membrane autophagosomes, which then fuse with lysosomes to form autolysosomes. These autolysosomes then degrade their contents to recycle the cellular components. Autophagy has been implicated in a wide variety of physiological and pathological processes that are closely related to tumorigenesis. In recent years, an increasing number of studies have indicated that nonsteroidal anti-inflammatory drugs, such as celecoxib, meloxicam, sulindac, aspirin, sildenafil, rofecoxib, and sodium salicylate, have diverse effects in cancer that are mediated by the autophagy pathway...
December 28, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/29281684/candida-albicans-derived-mannoproteins-activate-nf-%C3%AE%C2%BAb-in-reporter-cells-expressing-tlr4-md2-and-cd14
#14
Traci Ness, Mahmud Abdallah, Jaime Adams, Claudia Alvarado, Edwin Gunn, Brittany House, John Lamb, Jack Macguire, Emily Norris, Rebekah Robinson, Morgan Sapp, Jill Sharma, Ronald Garner
The ability of soluble C. albicans 20A (serotype A) mannoprotein (CMP) to serve as a ligand for toll-like receptor 4 (TLR4) and its co-receptors was examined using commercially available and stably-transfected HEK293 cells that express human TLR4, MD2 and CD14, but not MR. These TLR4 reporter cells also express an NF-κB-dependent, secreted embryonic alkaline phosphatase (SEAP) reporter gene. TLR4-reporter cells exhibited a dose-dependent SEAP response to both LPS and CMP, wherein peak activation was achieved after stimulation with 40-50 μg/mL of CMP...
2017: PloS One
https://www.readbyqxmd.com/read/29276267/limited-influence-of-excipients-in-extemporaneous-compounded-suspensions
#15
Eli Dijkers, Valerie Nanhekhan, Astrid Thorissen, Diego Marro, Marta Uriel
Objective: The objective of this study was to identify whether compounding oral suspensions with SyrSpend SF based on tablets or capsules is a suitable alternative for using raw pharmaceutical materials. Methods: Suspensions based on 5 different tablets and capsules were studied in SyrSpend SF. The summary of product characteristics of these different tablets and capsules were obtained from the manufacturer. Our hypothesis was that, if the maximum beyond-use date of the study was reached, the excipient did not seem to have an influence on the stability of the active pharmaceutical ingredient (API) within the studied time frame...
June 2017: Hospital Pharmacy
https://www.readbyqxmd.com/read/29275640/lost-in-translation-a-critical-look-at-the-role-that-animal-models-of-obsessive-compulsive-disorder-play-in-current-drug-discovery-strategies
#16
Kurt Leroy Hoffman, Hugo Cano-Ramírez
Obsessive-compulsive disorder (OCD) is a severe neuropsychiatric illness estimated to affect between 1-3% of the population. In today's literature, there are a number well-validated and convincing animal models of OCD described. Areas covered: Herein, the authors look at the role that animal models of OCD (including transgenic models, deer mouse stereotypy, quinpirole sensitization, post-training signal attenuation, and mouse marble burying) have played in determining the current directions of OCD drug discovery...
December 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29274661/perioperative-celecoxib-and-postoperative-opioid-use-in-hand-surgery-a-prospective-cohort-study
#17
Jeffrey G Stepan, Daniel A London, Daniel A Osei, Martin I Boyer, Agnes Z Dardas, Ryan P Calfee
PURPOSE: Prescription opioid abuse is an epidemic in the United States; multimodal analgesia has been suggested as a potential solution to decrease postoperative opioid use. The primary aim of this study was to determine the effect of perioperative celecoxib on opioid intake. Secondary goals were to determine whether perioperative administration of celecoxib decreased postoperative patient-reported pain and whether patient demographic characteristics could predict postoperative pain and opioid intake...
December 21, 2017: Journal of Hand Surgery
https://www.readbyqxmd.com/read/29250535/hpv16-e6-promotes-breast-cancer-proliferation-via-upregulation-of-cox-2-expression
#18
Y X Wang, Y Z Li, Z Y Zhang, J Q Wang, J Cui, X L Qian
Background. Breast cancer remains the leading cause of cancer-related mortality worldwide. It has been indicated that human papillomaviruses 16 (HPV16) might participate in the pathogenesis and development of breast cancer. However, the detected rate of HPV16 varies with region. We will investigate HPV16 E6 expression in North China and explore the effects and mechanism of HPV16 E6 on breast cancer proliferation in this study. Methods. The expressions of HPV16 E6 and COX-2 in paraffin-embedded tissues of the invasive ductal breast cancer were detected by qPCR and IHC...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29248935/potential-of-moringa-oleifera-in-the-treatment-of-benign-prostate-hyperplasia-role-of-antioxidant-defence-systems
#19
Ismail Ishola, Charles Anunobi, Kayode Yemitan, Olasunmbo Afolayan, Tobi Durojaiye
OBJECTIVE: This study sought to evaluate the protective effect of ethanolic leaf extract of Moringa Oleifera (M. oleifera ) on testosterone-induced benign prostatic hyperplasia (BPH) in male Sprague-Dawley rats. MATERIALS AND METHODS: BPH was induced in rats by administration of testosterone propionate (3 mg/kg, s.c., in olive oil) for 4 weeks. M. oleifera (50, 100 or 200 mg/kg), celecoxib (20 mg/kg) or M. oleifera (50 mg/kg) + celecoxib (20 mg/kg) were orally administered daily 15 min before testosterone...
December 17, 2017: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
https://www.readbyqxmd.com/read/29248723/iodine-prevents-the-increase-of-testosterone-induced-oxidative-stress-in-a-model-of-rat-prostatic-hyperplasia
#20
Michelle Quintero-García, Evangelina Delgado-González, Ana Sánchez-Tusie, Mario Vázquez, Carmen Aceves, Brenda Anguiano
Oxidative stress and inflammation are involved in the development and/or progression of benign prostatic hyperplasia (BPH). Molecular iodine (I2) induces antiproliferative and apoptotic effects in prostate cancer cells, but it is unknown if I2 regulates oxidative stress in the normal and/or tumoral prostate. The purpose of this study was to analyze the effects of I2 and celecoxib (Cxb) on oxidative stress and inflammation in a model of prostatic hyperplasia. Cxb was used as positive control of cyclooxygenase-2 (COX-2) inhibition...
December 14, 2017: Free Radical Biology & Medicine
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