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Cox 2 inhibitors

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https://www.readbyqxmd.com/read/28214973/a-multifunctional-alanine-rich-anti-inflammatory-peptide-bcp61-showed-potent-inhibitory-effects-by-inhibiting-both-nf-%C3%AE%C2%BAb-and-mapk-expression
#1
Yun Hee Choi, Yoon Seok Choi, Young Kyun Kim, Md Saifur Rahman, G C Pradeep, Jin Cheol Yoo, Joo-Won Suh
The purified BCP61 was reported to be a unique low-molecular-weight (MW) anti-microbial peptide because of its non-identical alanine-rich N-terminal sequence. In this study, we investigated the anti-inflammatory effects of BCP61 on induction of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), pro-inflammatory cytokines, nuclear factor-kappa B (NF-κB), and mitogen-activated protein kinases (MAPKs) in lipopolysaccharide (LPS)-stimulated Raw 264.7 cells. The treatment with BCP61, with varying concentrations of 10, 50, and 100 μg/mL, inhibited levels of expression of LPS-induced NF-κB and MAPKs (extracellular signal-related kinases (ERKs), c-Jun NH2-terminal kinase (JNK), and mitogen-activated protein (p38)) as well as production of pro-inflammatory mediators, such as nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6)...
February 18, 2017: Inflammation
https://www.readbyqxmd.com/read/28213268/fisetin-inhibits-il-1%C3%AE-induced-inflammatory-response-in-human-osteoarthritis-chondrocytes-through-activating-sirt1-and-attenuates-the-progression-of-osteoarthritis-in-mice
#2
Wenhao Zheng, Zhenhua Feng, Shengban You, Hui Zhang, Zhenyu Tao, Quan Wang, Hua Chen, Yaosen Wu
Osteoarthritis (OA) is a degenerative joint disease characterized by cartilage degradation and inflammation. Fisetin, a polyphenol extracted from fruits and vegetables, has been reported to have anti-inflammatory effects. Our study aimed to investigate the effect of fisetin on OA both in vitro and in vivo. In vitro, chondrocytes were pretreated with fisetin alone or fisetin combined with sirtinol (an inhibitor of SIRT1) for 2h before IL-1β stimulation. Production of NO, PGE2, TNF-α and IL-6 were evaluated by the Griess reaction and ELISAs...
February 14, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28212985/nonsteroidal-anti-inflammatory-drugs-in-clinical-and-experimental-epilepsy
#3
REVIEW
Beatrice Mihaela Radu, Florin Bogdan Epureanu, Mihai Radu, Paolo Francesco Fabene, Giuseppe Bertini
Current antiepileptic drugs have limited efficacy and provide little or no benefits in 30% of the patients. Given that a role for brain inflammation in epilepsy has been repeatedly reported in recent years, the potential of anti-inflammatory drugs should be explored in depth, as they may provide new therapeutical approaches in preventing or reducing epileptogenesis. Here, we review preclinical (both in vivo and in vitro) and clinical epilepsy studies in which nonsteroidal antiinflammatory drugs (NSAIDs), i...
February 9, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28212885/epinephrine-promotes-cox-2-dependent-immune-suppression-in-myeloid-cells-and-cancer-tissues
#4
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/28212823/cyp-epoxygenase-derived-h2o2-is-involved-in-the-endothelium-derived-hyperpolarization-edh-and-relaxation-of-intrarenal-arteries
#5
Mercedes Muñoz, Maria Elvira López-Oliva, Estéfano Pinilla, María Pilar Martínez, Ana Sánchez, Claudia Rodríguez, Albino García-Sacristán, Medardo Hernández, Luis Rivera, Dolores Prieto
Reactive oxygen species (ROS) like hydrogen peroxide (H2O2) are involved in the in endothelium-derived hyperpolarization (EDH)-type relaxant responses of coronary and mesenteric arterioles. The role of ROS in kidney vascular function has mainly been investigated in the context of harmful ROS generation associated to kidney disease. The present study was sought to investigate whether H2O2 is involved in the endothelium-dependent relaxations of intrarenal arteries as well the possible endothelial sources of ROS generation involved in these responses...
February 14, 2017: Free Radical Biology & Medicine
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
#6
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/28211343/immediate-reactions-to-more-than-1-nsaid-must-not-be-considered-cross-hypersensitivity-unless-tolerance-to-asa-is-verified
#7
D Pérez-Alzate, J A Cornejo-García, N Pérez-Sánchez, I Andreu, A García-Moral, J A Agúndez, J Bartra, I Doña, M J Torres, M Blanca, N Blanca-López, G Canto
BACKGROUND AND OBJECTIVES: Individuals who develop drug hypersensitivity reactions (DHRs) to chemically unrelated nonsteroidal anti-inflammatory drugs (NSAIDs) are considered cross-hypersensitive. The hallmark for this classification is that the patient presents a reaction after intake of or challenge with acetylsalicylic acid (ASA). Whether patients react to 2 or more NSAIDs while tolerating ASA remains to be studied (selective reactions, SRs). Objective: To identify patients with SRs to 2 or more NSAIDs including strong COX-1 inhibitors...
2017: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/28210513/seizure-following-the-use-of-the-cox-2-inhibitor-etoricoxib
#8
Valentina Arnao, Marianna Riolo, Brigida Fierro, Paolo Aridon
We describe a case of epileptic seizures occurring after the use of a COX-2 inhibitor. A 61-year-old man was admitted to our department because of a generalized tonic-clonic seizure. EEG showed generalized slowdown of the activity. Neuroimaging and blood samples studies did not evidence alterations, but a careful pharmacological history revealed that the patient had taken the COX-2 inhibitor etoricoxib to treat lumbago few days before the onset of clinical symptoms. No seizures were reported after etoricoxib discontinuation and an EEG resulted to be normal two months after this...
2017: Case Reports in Neurological Medicine
https://www.readbyqxmd.com/read/28207513/reduced-risk-of-all-cancer-and-solid-cancer-in-taiwanese-patients-with-rheumatoid-arthritis-treated-with-etanercept-a-tnf-%C3%AE-inhibitor
#9
Joung-Liang Lan, Chun-Hung Tseng, Jiunn-Horng Chen, Chi-Fung Cheng, Wen-Miin Liang, Gregory J Tsay
Biologics has been widely used in the treatment of rheumatoid arthritis. We aimed to determine whether etanercept, a TNF-α inhibitor (TNFi) that is used to treat patients with rheumatoid arthritis (RA), affects cancer risk.This retrospective matched cohort study used data in the Registry of Catastrophic Illness Database in Taiwan from January 1, 1996 to December 31, 2010. RA, all-cancer, and solid cancer were defined using International Classification of Disease codes (ICD-9-CM 714.X, 140-208, and 140-199, respectively)...
February 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28204833/small-heterodimer-partner-attenuates-hydrogen-peroxide-induced-expression-of-cyclooxygenase-2-and-inducible-nitric-oxide-synthase-by-suppression-of-activator-protein-1-and-nuclear-factor-%C3%AE%C2%BAb-in-renal-proximal-tubule-epithelial-cells
#10
Jung Sun Park, Hoon In Choi, Eun Hui Bae, Seong Kwon Ma, Soo Wan Kim
The orphan nuclear receptor, small heterodimer partner (SHP), plays a negative regulatory role in innate immune responses and is involved in various inflammatory signaling pathways. In the present study, we aimed to ascertain whether SHP is effective in preventing hydrogen peroxide (H2O2)-induced kidney tubular inflammation and explored the molecular mechanisms underlying the protective effects of SHP. Renal ischemia/reperfusion (I/R) injury was induced in mice by clamping both renal pedicles for 30 min...
March 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28203404/the-role-of-cyclooxygenase-2-in-the-protection-against-apoptosis-in-vascular-endothelial-cells-induced-by-cigarette-smoking
#11
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/28199967/pre-clinical-evaluation-of-small-molecule-loxl2-inhibitors-in-breast-cancer
#12
Joan Chang, Morghan C Lucas, Lidia E Leonte, Marc Garcia-Montolio, Lukram Babloo Singh, Alison D Findlay, Mandar Deodhar, Jonathan S Foot, Wolfgang Jarolimek, Paul Timpson, Janine T Erler, Thomas R Cox
Lysyl Oxidase-like 2 (LOXL2), a member of the lysyl oxidase family of amine oxidases is known to be important in normal tissue development and homeostasis, as well as the onset and progression of solid tumors. Here we tested the anti-tumor properties of two generations of novel small molecule LOXL2 inhibitor in the MDA-MB-231 human model of breast cancer. We confirmed a functional role for LOXL2 activity in the progression of primary breast cancer. Inhibition of LOXL2 activity inhibited the growth of primary tumors and reduced primary tumor angiogenesis...
February 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28199356/risk-of-dementia-from-proton-pump-inhibitor-use-in-asian-population-a-nationwide-cohort-study-in-taiwan
#13
Shu-Yu Tai, Chen-Yu Chien, Deng-Chyang Wu, Kun-Der Lin, Bo-Lin Ho, Yu-Han Chang, Yang-Pei Chang
INTRODUCTION: Concerns have been raised regarding the potential association between proton pump inhibitor (PPI) use and dementia. OBJECTIVE: This study aimed to examine this association in an Asian population. METHODS: Patients initiating PPI therapy between January 1, 2000 and December 31, 2003 without a prior history of dementia were identified from Taiwan's National Health Insurance Research Database. The outcome of interest was all-cause dementia...
2017: PloS One
https://www.readbyqxmd.com/read/28192731/isotrifoliol-inhibits-pro-inflammatory-mediators-by-suppression-of-tlr-nf-%C3%AE%C2%BAb-and-tlr-mapk-signaling-in-lps-induced-raw264-7-cells
#14
Hua Li, Jeong-Hyun Yoon, Hyo-Jun Won, Hyeon-Seon Ji, Heong Joo Yuk, Ki Hun Park, Ho-Yong Park, Tae-Sook Jeong
Soybeans, produced by Glycine max (L.) Merr., contain high levels of isoflavones, such as genistein and daidzein. However, soy leaves contain more diverse and abundant flavonol glycosides and coumestans, as compared to the soybean. This study investigated the anti-inflammatory effects of the major coumestans present in soy leaf (coumestrol, isotrifoliol, and phaseol) in lipopolysaccharide (LPS)-induced RAW264.7 cells. Coumestans significantly reduced LPS-induced nitric oxide (NO), prostaglandin E2 (PGE2), and reactive oxygen species (ROS) production; isotrifoliol had the most potent anti-inflammatory activity...
February 10, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28192529/first-line-antiretroviral-drug-discontinuations-in-children
#15
Melony Fortuin-de Smidt, Reneé de Waal, Karen Cohen, Karl-Günter Technau, Kathryn Stinson, Gary Maartens, Andrew Boulle, Ehimario U Igumbor, Mary-Ann Davies
INTRODUCTION: There are a limited number of paediatric antiretroviral drug options. Characterising the long term safety and durability of different antiretrovirals in children is important to optimise management of HIV infected children and to determine the estimated need for alternative drugs in paediatric regimens. We describe first-line antiretroviral therapy (ART) durability and reasons for discontinuations in children at two South African ART programmes, where lopinavir/ritonavir has been recommended for children <3 years old since 2004, and abacavir replaced stavudine as the preferred nucleoside reverse transcriptase inhibitor in 2010...
2017: PloS One
https://www.readbyqxmd.com/read/28192453/refining-criteria-for-selecting-candidates-for-a-safe-lopinavir-ritonavir-or-darunavir-ritonavir-monotherapy-in-hiv-infected-virologically-suppressed-patients
#16
Nicola Gianotti, Alessandro Cozzi-Lepri, Andrea Antinori, Antonella Castagna, Andrea De Luca, Benedetto Maurizio Celesia, Massimo Galli, Cristina Mussini, Carmela Pinnetti, Vincenzo Spagnuolo, Antonella d'Arminio Monforte, Francesca Ceccherini-Silberstein, Massimo Andreoni
OBJECTIVE: The primary objective of this study was to estimate the incidence of treatment failure (TF) to protease inhibitor monotherapies (PI/r-MT) with lopinavir/ritonavir (LPV/r) or darunavir/ritonavir (DRV/r). DESIGN: A multicenter cohort of HIV-infected patients with viral load (VL) ≤50 copies/mL, who underwent a switch from any triple combination therapy to PI/r-MT with either LPV/r or DRV/r. METHODS: VL was assessed in each center according to local procedures...
2017: PloS One
https://www.readbyqxmd.com/read/28188047/pretreatment-serum-prealbumin-as-an-independent-prognostic-indicator-in-patients-with-metastatic-renal-cell-carcinoma-using-tyrosine-kinase-inhibitors-as-first-line-target-therapy
#17
Wen Cai, Wen Kong, Baijun Dong, Jin Zhang, Yonghui Chen, Wei Xue, Yiran Huang, Lixin Zhou, Jiwei Huang
BACKGROUND: Although serum prealbumin is a sensitive marker to assess malnutrition, its prognostic impact in patients with metastatic renal cell carcinoma (mRCC) remains elusive. METHODS: Patients' data were retrospectively retrieved from the medical records of Renji Hospital affiliated to Shanghai Jiao Tong University School of Medicine from March 2006 to July 2015 to access overall survival (OS) and progression-free survival (PFS). The survival outcomes of patients with low pretreatment prealbumin (< 200 mg/L) and high pretreatment prealbumin (≥ 200 mg/L) were compared using a log-rank test and Cox proportional hazard regression model...
January 18, 2017: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/28187734/the-potential-neuroprotective-role-of-a-histone-deacetylase-inhibitor-sodium-butyrate-after-neonatal-hypoxia-ischemia
#18
Joanna Jaworska, Malgorzata Ziemka-Nalecz, Joanna Sypecka, Teresa Zalewska
BACKGROUND: Histone deacetylase inhibitor (HDACi), sodium butyrate (SB), has been shown to be neuroprotective in adult brain injury models. Potential explanation for the inhibitor action involves among others reduced inflammation. We therefore anticipated that SB will provide a suitable option for brain injury in immature animals. The aim of our study was to test the hypothesis that one of the mechanisms of protection afforded by SB after neonatal hypoxia-ischemia is associated with anti-inflammatory action...
February 10, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28185540/medicinal-chemistry-approaches-of-controlling-gastrointestinal-side-effects-of-non-steroidal-anti-inflammatory-drugs-endogenous-protective-mechanisms-and-drug-design
#19
Paraskevi Tziona, Panagiotis Theodosis-Nobelos, Eleni A Rekka
BACKGROUND: Non steroidal anti-inflammatory drugs are of the oldest and most widely used medicines. However, their untoward effects, especially gastrointestinal toxicity, remain the main obstacle to their application. Because of their mechanism of action, cycloxygenase (COX) inhibition, in combination with the weekly acidic character of most of them, major protective mechanisms of the gastrointestinal system are suppressed and deregulated. OBJECTIVE: In this review, several compounds designed to retain anti-inflammatory activity, but devoid of gastrointestinal side effects, are presented...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28182010/microrna-144-is-regulated-by-cp2-and-decreases-cox-2-expression-and-pge2-production-in-mouse-ovarian-granulosa-cells
#20
Jiawei Zhou, Bin Lei, Huanan Li, Lihua Zhu, Lei Wang, Hu Tao, Shuqi Mei, Fenge Li
Mammalian folliculogenesis is a complex process in which primordial follicles develop into pre-ovulatory follicles, followed by ovulation to release mature oocytes. In this study, we explored the role of miR-144 in ovulation. miR-144 was one of the differentially expressed microRNAs, which showed 5.59-fold changes, in pre-ovulatory ovarian follicles between Large White and Chinese Taihu sows detected by Solexa deep sequencing. We demonstrated that overexpression of miR-144 significantly decreased the luciferase reporter activity under the control of the cyclooxygenase-2 (COX-2) or mothers against decapentaplegic homologue 4 (Smad4) 3'-untranslated region (3'-UTR) and suppressed COX-2 and Smad4 expression...
February 9, 2017: Cell Death & Disease
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