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Cox1 inhibiter

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https://www.readbyqxmd.com/read/28668885/interactive-analysis-of-tx-1123-with-cyclo-oxygenase-design-of-cox2-selective-tx-analogs
#1
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/28575175/central-administration-of-indomethacin-mitigates-the-injury-induced-upregulation-of-aromatase-expression-and-estradiol-content-in-the-zebra-finch-brain
#2
Alyssa L Pedersen, Jenna L Brownrout, Colin J Saldanha
Injury to the vertebrate brain causes neuroinflammation, characterized in part by increases in prostaglandins. In rodents and songbirds, brain injury also induces the transcription and translation of aromatase in reactive astrocytes around the site of damage. Interestingly, this induction is more rapid in female zebra finches relative to males. Induced aromatization is neuroprotective, as inhibition of aromatase and estrogen replacement, increases and decreases the extent of damage, respectively. While the consequences of induced astrocytic aromatization are intensely studied, little is known about what factor(s) induce aromatase...
June 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28571535/nonsteroidal-anti-inflammatory-drugs-exploiting-bivalent-coxib-tp-antagonists-for-the-control-of-cardiovascular-risk
#3
Silvia Carnevali, Carola Buccellati, Chiara Bolego, Massimo Bertinaria, Rovati G Enrico, Angelo Sala
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are some of the most widely prescribed or dispensed analgesics and antipyretics that act by inhibiting prostaglandins (PGs) and thromboxane synthesis. After the identification of a second isoform of COX, the pharmaceutical research focused on developing COX-2-selective drugs (COXIBs) considered as second generation NSAIDs that would retain the anti-inflammatory and analgesic activities of traditional NSAID without blunting the gastrointestinal cytoprotection sustained by COX1-derived products such as PGE2...
June 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28539709/multipathway-integrated-adjustment-mechanism-of-glycyrrhiza-triterpenes-curing-gastric-ulcer-in-rats
#4
Ying Wang, Shuai Wang, Yongrui Bao, Tianjiao Li, Xin Chang, Guanlin Yang, Xiansheng Meng
BACKGROUND: Gastric ulcer is a common chronic disease in human digestive system, which is difficult to cure, easy to relapse, and endangers human health seriously. Compared with western medicine, traditional Chinese medicine has a unique advantage in improving the general situation, stablizing medical condition, and with little side effects. Glycyrrhiza known as "king of all the medicine", has a range of pharmacological activities and is commonly used in a variety of proprietary Chinese medicines and formulations...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28527697/antibiotics-induce-mitonuclear-protein-imbalance-but-fail-to-inhibit-respiration-and-nutrient-activation-in-pancreatic-%C3%AE-cells
#5
Jaime Santo-Domingo, Isabelle Chareyron, Charlotte Broenimann, Steve Lassueur, Andreas Wiederkehr
Chloramphenicol and several other antibiotics targeting bacterial ribosomes inhibit mitochondrial protein translation. Inhibition of mitochondrial protein synthesis leads to mitonuclear protein imbalance and reduced respiratory rates as confirmed here in HeLa and PC12 cells. Unexpectedly, respiration in INS-1E insulinoma cells and primary human islets was unaltered in the presence of chloramphenicol. Resting respiratory rates and glucose stimulated acceleration of respiration were also not lowered when a range of antibiotics including, thiamphenicol, streptomycin, gentamycin and doxycycline known to interfere with bacterial protein synthesis were tested...
May 17, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28416371/modulation-by-nadph-oxidase-of-the-chronic-cardiovascular-and-autonomic-interaction-between-cyclosporine-and-nsaids-in-female-rats
#6
Ahmed F El-Yazbi, Karim S Ibrahim, Hanan M El-Gowelli, Nevine M El-Deeb, Mahmoud M El-Mas
Cyclosporine (CSA) and nonsteroidal antiinflammatory drugs (NSAIDs) are used together to manage arthritic disorders with an immune component. Previous reports showed contrasting effects for NSAIDs on CSA nephrotoxicity and acute elevations in blood pressure. Both effects were ameliorated or exaggerated after selective cyclooxygenase-2 (COX2) and nonselective COX inhibition, respectively. Here we investigated: (i) the interaction of CSA with NSAIDs possessing variable COX1/COX2 selectivities on hemodynamic, left ventricular (LV) and cardiac autonomic and histologic profiles, and (ii) role of NADPH-oxidase (NOX)/Rho-kinase (ROCK) pathway in the interaction...
April 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28356021/novel-thiourea-derivatives-bearing-sulfonamide-moiety-as-anticancer-agents-through-cox-2-inhibition
#7
Mostafa M Ghorab, Mohamed S A El-Gaby, Mansour S Alsaid, Yaseen A M M Elshaier, Aiten M Soliman, Fardous F El-Senduny, Farid A Badria
A series of novel thioureas 5a-n, 8, quinazoline 6, benzo[g]quinazoline 7 and benzo[1,3] dioxole 10, bearing a sulfonamide moiety were synthesized from the starting compound N-(2,6-dimethoxypyrimidin-4-yl)-4-isothiocyanatobenzenesulfonamide 2. The target compounds were screened against HepG2, MCF-7, Caco-2, HCT-116, PC-3 cancer cell lines and VERO-B normal cell line. Out of all the tested compounds, compound 5c showed a broad selective cytotoxicity against HepG2, MCF-7, Caco-2 and PC-3 cancer cells. Moreover, a sensitization assay was performed on Caco-2 cells, compound 5c proved to act as a chemosensitizer for cisplatin on colon cancer (Caco-2) cells...
March 27, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28069828/lpa1-receptor-mediated-thromboxane-a2-release-is-responsible-for-lysophosphatidic-acid-induced-vascular-smooth-muscle-contraction
#8
Péter Tibor Dancs, Éva Ruisanchez, Andrea Balogh, Cecília Rita Panta, Zsuzsanna Miklós, Rolf M Nüsing, Junken Aoki, Jerold Chun, Stefan Offermanns, Gábor Tigyi, Zoltán Benyó
Lysophosphatidic acid (LPA) has been recognized recently as an endothelium-dependent vasodilator, but several lines of evidence indicate that it may also stimulate vascular smooth muscle cells (VSMCs), thereby contributing to vasoregulation and remodeling. In the present study, mRNA expression of all 6 LPA receptor genes was detected in murine aortic VSMCs, with the highest levels of LPA1, LPA2, LPA4, and LPA6 In endothelium-denuded thoracic aorta (TA) and abdominal aorta (AA) segments, 1-oleoyl-LPA and the LPA1-3 agonist VPC31143 induced dose-dependent vasoconstriction...
April 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27895618/cyclooxygenase-1-as-a-potential-therapeutic-target-for-seizure-suppression-evidences-from-zebrafish-pentylenetetrazole-seizure-model
#9
Patrícia Gonçalves Barbalho, Benilton de Sá Carvalho, Iscia Lopes-Cendes, Claudia Vianna Maurer-Morelli
Cyclooxygenases (COX)-1 and -2 are isoenzymes that catalyze the conversion of arachidonic acid into prostaglandins (PGs). COX-2 and PGs are rapidly increased following seizures and are known to play important roles in the neuroinflammatory process. COX-2 isoform has been predominantly explored as the most suitable target for pharmacological intervention in epilepsy studies, while COX-1 remains poorly investigated. In the present study, we evaluated the effects of selective COX-1 inhibitor or selective COX-2 inhibitor on seizure suppression in the zebrafish pentylenetetrazole (PTZ)-seizure model...
2016: Frontiers in Neurology
https://www.readbyqxmd.com/read/27881647/activation-of-cox-2-pge2-promotes-sapovirus-replication-via-the-inhibition-of-nitric-oxide-production
#10
Mia Madel Alfajaro, Jong-Soon Choi, Deok-Song Kim, Ja-Young Seo, Ji-Yun Kim, Jun-Gyu Park, Mahmoud Soliman, Yeong-Bin Baek, Eun-Hyo Cho, Joseph Kwon, Hyung-Jun Kwon, Su-Jin Park, Woo Song Lee, Mun-Il Kang, Myra Hosmillo, Ian Goodfellow, Kyoung-Oh Cho
Enteric caliciviruses in the genera Norovirus and Sapovirus are important pathogens that cause severe acute gastroenteritis in both humans and animals. Cyclooxygenases (COXs) and their final product, prostaglandin E2 (PGE2), are known to play important roles in the modulation of both the host response to infection and the replicative cycles of several viruses. However, the precise mechanism(s) by which the COX/PGE2 pathway regulates sapovirus replication remains largely unknown. In this study, infection with porcine sapovirus (PSaV) strain Cowden, the only cultivable virus within the genus Sapovirus, markedly increased COX-2 mRNA and protein levels at 24 and 36 h postinfection (hpi), with only a transient increase in COX-1 levels seen at 24 hpi...
February 1, 2017: Journal of Virology
https://www.readbyqxmd.com/read/27826185/synthesis-anti-inflammatory-analgesic-cox1-2-inhibitory-activity-and-molecular-docking-studies-of-hybrid-pyrazole-analogues
#11
Md Jahangir Alam, Ozair Alam, Suroor Ahmad Khan, Mohd Javed Naim, Mohammad Islamuddin, Girdhar Singh Deora
This article reports on the design, synthesis, and pharmacological activity of a new series of hybrid pyrazole analogues: 5a-5u. Among the series 5a-5u, the compounds 5u and 5s exhibited potent anti-inflammatory activity of 80.63% and 78.09% and inhibition of 80.87% and 76.56% compared with the standard drug ibuprofen, which showed 81.32% and 79.23% inhibition after 3 and 4 hours, respectively. On the basis of in vivo studies, 12 compounds were selected for assessment of their in vitro inhibitory action against COX1/2 and TNFα...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27698065/fluid-shear-stress-promotes-placental-growth-factor-upregulation-in-human-syncytiotrophoblast-through-the-camp-pka-signaling-pathway
#12
Edouard Lecarpentier, Anthony Atallah, Jean Guibourdenche, Marylise Hebert-Schuster, Sarah Vieillefosse, Audrey Chissey, Bassam Haddad, Guillaume Pidoux, Daniele Evain-Brion, Abdul Barakat, Thierry Fournier, Vassilis Tsatsaris
The effects of fluid shear stress (FSS) on the human syncytiotrophoblast and its biological functions have never been studied. During pregnancy, the syncytiotrophoblast is the main source of placental growth factor (PlGF), a proangiogenic factor involved in the placental angiogenesis and the vascular adaptation to pregnancy. The role of FSS in regulating PlGF expression in syncytiotrophoblasts is unknown. We investigated the impact of FSS on the production and secretion of the PlGF by the human syncytiotrophoblasts in primary cell culture...
December 2016: Hypertension
https://www.readbyqxmd.com/read/27580512/role-of-cyclooxygenase-isoforms-in-encephalopathy-of-cirrhotic-rats
#13
Hsin-Ling Ho, Shao-Jung Hsu, Fa-Yauh Lee, Hui-Chun Huang, I-Fang Hsin, Ming-Chih Hou, Shou-Dong Lee
BACKGROUND: Hepatic encephalopathy (HE) is a complex neuropsychiatric syndrome secondary to acute or chronic liver failure. However, its pathophysiology remains obscure. Recently, we found that the inhibition of cyclooxygenase by indomethacin aggravated HE in rats with thioacetamide-induced acute hepatic failure, suggesting a pivotal role of cyclooxygenase in HE. This study was aimed at surveying the roles of cyclooxygenase isoforms responsible for prostaglandins synthesis, cyclooxygenase-1 (COX1) and COX2, in cirrhotic rats with HE...
November 2016: Journal of the Chinese Medical Association: JCMA
https://www.readbyqxmd.com/read/27293373/the-small-tellurium-based-compound-sas-suppresses-inflammation-in-human-retinal-pigment-epithelium
#14
Rima Dardik, Tami Livnat, Gilad Halpert, Shayma Jawad, Yael Nisgav, Shirley Azar-Avivi, Baoying Liu, Robert B Nussenblatt, Dov Weinberger, Benjamin Sredni
PURPOSE: Pathological angiogenesis and chronic inflammation greatly contribute to the development of choroidal neovascularization (CNV) in chorioretinal diseases involving abnormal contact between retinal pigment epithelial (RPE) and endothelial cells (ECs), associated with Bruch's membrane rupture. We explored the ability of the small organotellurium compound octa-O-bis-(R,R)-tartarate ditellurane (SAS) to mitigate inflammatory processes in human RPE cells. METHODS: Cell adhesion assays and analyses of gene and protein expression were used to examine the effect of SAS on ARPE-19 cells or primary human RPE cells that were grown alone or in an RPE-EC co-culture...
2016: Molecular Vision
https://www.readbyqxmd.com/read/26907476/opposing-roles-of-ltb4-and-pge2-in-regulating-the-inflammasome-dependent-scorpion-venom-induced-mortality
#15
Karina F Zoccal, Carlos A Sorgi, Juliana I Hori, Francisco W G Paula-Silva, Eliane C Arantes, Carlos H Serezani, Dario S Zamboni, Lúcia H Faccioli
Tityus serrulatus sting causes thousands of deaths annually worldwide. T. serrulatus-envenomed victims exhibit local or systemic reaction that culminates in pulmonary oedema, potentially leading to death. However, the molecular mechanisms underlying T. serrulatus venom (TsV) activity remain unknown. Here we show that TsV triggers NLRP3 inflammasome activation via K(+) efflux. Mechanistically, TsV triggers lung-resident cells to release PGE2, which induces IL-1β production via E prostanoid receptor 2/4-cAMP-PKA-NFκB-dependent mechanisms...
February 23, 2016: Nature Communications
https://www.readbyqxmd.com/read/26690700/prostaglandin-dependent-modulation-of-dopaminergic-neurotransmission-elicits-inflammation-induced-aversion-in-mice
#16
Michael Fritz, Anna M Klawonn, Anna Nilsson, Anand Kumar Singh, Joanna Zajdel, Daniel Björk Wilhelms, Michael Lazarus, Andreas Löfberg, Maarit Jaarola, Unn Örtegren Kugelberg, Timothy R Billiar, David J Hackam, Chhinder P Sodhi, Matthew D Breyer, Johan Jakobsson, Markus Schwaninger, Günther Schütz, Jan Rodriguez Parkitna, Clifford B Saper, Anders Blomqvist, David Engblom
Systemic inflammation causes malaise and general feelings of discomfort. This fundamental aspect of the sickness response reduces the quality of life for people suffering from chronic inflammatory diseases and is a nuisance during mild infections like common colds or the flu. To investigate how inflammation is perceived as unpleasant and causes negative affect, we used a behavioral test in which mice avoid an environment that they have learned to associate with inflammation-induced discomfort. Using a combination of cell-type–specific gene deletions, pharmacology, and chemogenetics, we found that systemic inflammation triggered aversion through MyD88-dependent activation of the brain endothelium followed by COX1-mediated cerebral prostaglandin E2 (PGE2) synthesis...
February 2016: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/26612417/inhibition-of-cox1-2-alters-the-host-response-and-reduces-ecm-scaffold-mediated-constructive-tissue-remodeling-in-a-rodent-model-of-skeletal-muscle-injury
#17
Christopher L Dearth, Peter F Slivka, Scott A Stewart, Timothy J Keane, Justin K Tay, Ricardo Londono, Qingnian Goh, Francis X Pizza, Stephen F Badylak
UNLABELLED: Extracellular matrix (ECM) has been used as a biologic scaffold material to both reinforce the surgical repair of soft tissue and serve as an inductive template to promote a constructive tissue remodeling response. Success of such an approach is dependent on macrophage-mediated degradation and remodeling of the biologic scaffold. Macrophage phenotype during these processes is a predictive factor of the eventual remodeling outcome. ECM scaffolds have been shown to promote an anti-inflammatory or M2-like macrophage phenotype in vitro that includes secretion of downstream products of cycolooxygenases 1 and 2 (COX1/2)...
February 2016: Acta Biomaterialia
https://www.readbyqxmd.com/read/26448933/efficient-mitochondrial-genome-editing-by-crispr-cas9
#18
Areum Jo, Sangwoo Ham, Gum Hwa Lee, Yun-Il Lee, SangSeong Kim, Yun-Song Lee, Joo-Ho Shin, Yunjong Lee
The Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)/Cas9 system has been widely used for nuclear DNA editing to generate mutations or correct specific disease alleles. Despite its flexible application, it has not been determined if CRISPR/Cas9, originally identified as a bacterial defense system against virus, can be targeted to mitochondria for mtDNA editing. Here, we show that regular FLAG-Cas9 can localize to mitochondria to edit mitochondrial DNA with sgRNAs targeting specific loci of the mitochondrial genome...
2015: BioMed Research International
https://www.readbyqxmd.com/read/26426354/a-taqman-based-multiplex-qpcr-assay-and-dna-extraction-method-for-phylotype-iib-sequevars-1-2-select-agent-strains-of-ralstonia-solanacearum
#19
Michael J Stulberg, Qi Huang
Ralstonia solanacearum race 3 biovar 2 strains belonging to phylotype IIB, sequevars 1 and 2 (IIB-1&2) cause brown rot of potato in temperate climates, and are quarantined pathogens in Canada and Europe. Since these strains are not established in the U.S. and because of their potential risk to the potato industry, the U.S. government has listed them as select agents. Cultivated geraniums are also a host and have the potential to spread the pathogen through trade, and its extracts strongly inhibits DNA-based detection methods...
2015: PloS One
https://www.readbyqxmd.com/read/26369685/non-steroidal-anti-inflammatory-drugs-nsaids-induced-dyspepsia
#20
REVIEW
Paul Ray-Yee Yap, Khean-Lee Goh
Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed group of drugs in the world. They are used primarily for pain relief in chronic inflammatory joint disease and act by inhibiting enzymes COX1 and COX2 and ultimately preventing the production of active prostanoids which are required for the innate inflammatory pathway. The use of NSAIDs have been associated with the development of gastrointestinal (GI) symptoms ranging from simple dyspepsia to life threatening GI bleeds and perforations...
2015: Current Pharmaceutical Design
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