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Cox1 inhibiter

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https://www.readbyqxmd.com/read/29697164/a-supercritical-co-2-extract-of-neem-leaf-a-indica-and-its-bioactive-liminoid-nimbolide-suppresses-colon-cancer-in-preclinical-models-by-modulating-pro-inflammatory-pathways
#1
Mandakini J Patel, Shreya Tripathy, Keya D Mukhopadhyay, Tamna Wangjam, April B Cabang, Jay Morris, Michael J Wargovich
Colorectal cancer (CRC) is the third most commonly diagnosed cancer and the second leading cause of cancer death in men and women in the United States. Anti-inflammatory blockade has been proven to be a promising avenue of colorectal cancer prevention. However, NSAIDs while effective in curbing CRC risk are too toxic for long-term use in cancer prevention. The Neem tree (Azadirachta indica) is rich in liminoid terpenoids, collectively known as azadiractoids and has been shown to have anti-inflammatory effects...
April 26, 2018: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/29627858/first-detection-of-echinococcus-granulosus-sensu-stricto-g1-in-dogs-in-central-sudan
#2
Rihab Ali Omer, Arwid Daugschies, Sandra Gawlowska, Ayman Elnahas, Peter Kern, Sofia Bashir, Mohammed Sir Alkhatim Ali, Amin Osman, Thomas Romig
Eighty-four stray dogs shot as a part of a governmental rabies control program in two neighboring towns of central Sudan were examined for the presence of Echinococcus spp. and other intestinal helminths. Echinococcus worms were identified to species level by PCR and gene sequencing. For comparative reasons, rectal content of the necropsied dogs was examined for helminth eggs and subjected to copro-PCR for Echinococcus. At necropsy, 51.2% (43/84) of the dogs harbored Echinococcus canadensis (G6/7) worms with worm burdens ranging from 22,000 to 80,000...
May 2018: Parasitology Research
https://www.readbyqxmd.com/read/29602039/potent-and-selective-aldo-keto-reductase-1c3-akr1c3-inhibitors-based-on-the-benzoisoxazole-moiety-application-of-a-bioisosteric-scaffold-hopping-approach-to-flufenamic-acid
#3
Agnese Chiara Pippione, Irene Maria Carnovale, Davide Bonanni, Marcella Sini, Parveen Goyal, Elisabetta Marini, Klaus Pors, Salvatore Adinolfi, Daniele Zonari, Claudio Festuccia, Weixiao Yuan Wahlgren, Rosmarie Friemann, Renzo Bagnati, Donatella Boschi, Simonetta Oliaro-Bosso, Marco Lucio Lolli
The aldo-keto reductase 1C3 (AKR1C3) isoform plays a vital role in the biosynthesis of androgens and is considered an attractive target in prostate cancer (PCa). No AKR1C3-targeted agent has to date been approved for clinical use. Flufenamic acid and indomethacine are non-steroidal anti-inflammatory drugs known to inhibit AKR1C3 in a non-selective manner as COX off-target effects are also observed. Recently, we employed a scaffold hopping approach to design a new class of potent and selective AKR1C3 inhibitors based on a N-substituted hydroxylated triazole pharmacophore...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29357411/apol1-renal-risk-variants-induce-aberrant-thp-1-monocyte-differentiation-and-increase-eicosanoid-production-via-enhanced-expression-of-cyclooxygenase-2
#4
Hewang Lee, Hila Roshanravan, Ying Wang, Koji Okamoto, Junghwa Ryu, Shashi Shrivastav, Peng Qu, Jeffrey B Kopp
Apolipoprotein L1 (APOL1) genetic variants are strongly associated with kidney disease. We investigated the role of APOL1 variants in monocyte differentiation and eicosanoid production in macrophages, as activated tissue macrophages in kidney might contribute to kidney injury. In human monocyte THP-1 cells, transient overexpression of APOL1 (G0, G1, G2) by transfection resulted in a 5 to 11-fold increase in CD14 and CD68 gene expression, similar to that seen with phorbol-12-myristate acetate treatment. All APOL1 variants caused monocytes to differentiate into atypical M1 macrophages with marked increase in M1 markers CD80, TNF, IL1B, and IL6 and modest increase in the M2 marker CD163 as compared to control cells...
January 10, 2018: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29316620/could-aspirin-and-diets-high-in-fiber-act-synergistically-to-reduce-the-risk-of-colon-cancer-in-humans
#5
REVIEW
Pan Pan, Yi-Wen Huang, Kiyoko Oshima, Martha Yearsley, Jianying Zhang, Jianhua Yu, Mark Arnold, Li-Shu Wang
Early inhibition of inflammation suppresses the carcinogenic process. Aspirin is the most commonly used non-steroid anti-inflammatory drugs (NSAIDs), and it irreversibly inhibits cyclooxygenase-1 and -2 (COX1, COX2). Multiple randomized clinical trials have demonstrated that aspirin offers substantial protection from colon cancer mortality. The lower aspirin doses causing only minimal gastrointestinal disturbance, ideal for long-term use, can achieve only partial and transitory inhibition of COX2. Aspirin's principal metabolite, salicylic acid, is also found in fruits and vegetables that inhibit COX2...
January 6, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29251736/pge-2-ep-1-receptor-inhibits-vasopressin-dependent-water-reabsorption-and-sodium-transport-in-mouse-collecting-duct
#6
Rania Nasrallah, Joseph Zimpelmann, David Eckert, Jamie Ghossein, Sean Geddes, Jean-Claude Beique, Jean-Francois Thibodeau, Chris R J Kennedy, Kevin D Burns, Richard L Hébert
PGE2 regulates glomerular hemodynamics, renin secretion, and tubular transport. This study examined the contribution of PGE2 EP1 receptors to sodium and water homeostasis. Male EP1-/- mice were bred with hypertensive TTRhRen mice (Htn) to evaluate blood pressure and kidney function at 8 weeks of age in four groups: wildtype (WT), EP1-/-, Htn, HtnEP1-/-. Blood pressure and water balance were unaffected by EP1 deletion. COX1 and mPGE2 synthase were increased and COX2 was decreased in mice lacking EP1, with increases in EP3 and reductions in EP2 and EP4 mRNA throughout the nephron...
March 2018: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/29225179/synthesis-of-novel-benzodioxane-midst-piperazine-moiety-decorated-chitosan-silver-nanoparticle-against-biohazard-pathogens-and-as-potential-anti-inflammatory-candidate-a-molecular-docking-studies
#7
C S Karthik, H M Manukumar, A P Ananda, S Nagashree, K P Rakesh, L Mallesha, Hua-Li Qin, S Umesha, P Mallu, N B Krishnamurthy
Nanoparticles (NPs) are currently being investigated along with the use of biodegradable polymer containing active agents in many areas of medicine for targeted applications. The present study was aimed to synthesize novel compound Benzodioxane midst piperazine (BP) and characterization of a BP decorated chitosan silver nanoparticles (BP*C@AgNPs) and shown effective against hazardous pathogens, and also having anti-inflammatory property. It was further evaluated for molecular docking proofs, and toxicity. The BP*C@AgNPs had spherical shape with size of 36...
March 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29221664/mechanisms-of-damage-to-the-gastrointestinal-tract-from-nonsteroidal-anti-inflammatory-drugs
#8
REVIEW
Ingvar Bjarnason, Carmelo Scarpignato, Erik Holmgren, Michael Olszewski, Kim D Rainsford, Angel Lanas
Nonsteroidal anti-inflammatory drugs (NSAIDs) can damage the gastrointestinal tract, causing widespread morbidity and mortality. Although mechanisms of damage involve the activities of prostaglandin-endoperoxide synthase 1 (PTGS1 or cyclooxygenase [COX] 1) and PTGS1 (COX2), other factors are involved. We review the mechanisms of gastrointestinal damage induction by NSAIDs via COX-mediated and COX-independent processes. NSAIDs interact with phospholipids and uncouple mitochondrial oxidative phosphorylation, which initiates biochemical changes that impair function of the gastrointestinal barrier...
February 2018: Gastroenterology
https://www.readbyqxmd.com/read/28956230/toxicological-analysis-of-triadimefon-on-endocrine-disruption-and-oxidative-stress-during-rare-minnow-gobiocypris-rarus-larvae-development
#9
Jinhua Jiang, Gaojie Hu, Changpeng Zhang, Xueping Zhao, Qiang Wang, Liezhong Chen
Triadimefon (TDF) is a systemic wide-spectrum antifungal compound that is widely used in agriculture to inhibit fungal growth on various crops. Since previous studies focused on the embryo and adult life stages in the investigation of ecological impact, here we investigated the long-term effects of TDF (1, 10, 100 μg/L) on rare minnow during its larvae development. TDF caused an anti-estrogenic effect by decreasing vitellogenin (VTG) and CYP19a mRNA level, and inhibiting the aromatase activity and VTG levels after a 3, 6, 10, or 14-day exposure in rare minnow larvae...
December 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28931599/mrpl35-a-mitospecific-component-of-mitoribosomes-plays-a-key-role-in-cytochrome-c-oxidase-assembly
#10
Jodie M Box, Jasvinder Kaur, Rosemary A Stuart
Mitoribosomes perform the synthesis of the core components of the oxidative phosphorylation (OXPHOS) system encoded by the mitochondrial genome. We provide evidence that MrpL35 (mL38), a mitospecific component of the yeast mitoribosomal central protuberance, assembles into a subcomplex with MrpL7 (uL5), Mrp7 (bL27), and MrpL36 (bL31) and mitospecific proteins MrpL17 (mL46) and MrpL28 (mL40). We isolated respiratory defective mrpL35 mutant yeast strains, which do not display an overall inhibition in mitochondrial protein synthesis but rather have a problem in cytochrome c oxidase complex (COX) assembly...
November 15, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28881288/hydroxytriazole-derivatives-as-potent-and-selective-aldo-keto-reductase-1c3-akr1c3-inhibitors-discovered-by-bioisosteric-scaffold-hopping-approach
#11
Agnese C Pippione, Alessandro Giraudo, Davide Bonanni, Irene M Carnovale, Elisabetta Marini, Clara Cena, Annalisa Costale, Daniele Zonari, Klaus Pors, Maria Sadiq, Donatella Boschi, Simonetta Oliaro-Bosso, Marco L Lolli
The aldo-keto reductase 1C3 isoform (AKR1C3) plays a vital role in the biosynthesis of androgens, making this enzyme an attractive target for castration-resistant prostate cancer therapy. Although AKR1C3 is a promising drug target, no AKR1C3-targeted agent has to date been approved for clinical use. Flufenamic acid, a non-steroidal anti-inflammatory drug, is known to potently inhibit AKR1C3 in a non-selective manner as COX off-target effects are also observed. To diminish off-target effects, we have applied a scaffold hopping strategy replacing the benzoic acid moiety of flufenamic acid with an acidic hydroxyazolecarbonylic scaffold...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28844389/synthesis-and-biological-evaluations-of-new-nitric-oxide-anti-inflammatory-drug-hybrids
#12
Eman K A Abdelall, Abdou O Abdelhamid, Amany A Azouz
Three novel series of nitroso derivatives (11-15), isoxazolopyrazoles (17a-c) and isoxazolo[3,4-d]pyridazines (18a-c) were prepared from the hydroxyimoyl chloride 10. In vitro COX1⧹2 inhibition activities were evaluated, both of 17b and 18a proved a promising inhibitory activity with IC50 =1.12, 0.78μM in sequent. Carrageenan induced Paw edema, ulcer liability, nitric oxide (NO) release and histopathological study were determined. Most of the prepared compounds showed excellent activities. Reactions of 2-aminopyridine and enaminone with hydroxyimoyl chloride 10 were investigated and proved by 2D NMR...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28839250/pharmacological-profile-and-efficiency-in-vivo-of-diflapolin-the-first-dual-inhibitor-of-5-lipoxygenase-activating-protein-and-soluble-epoxide-hydrolase
#13
Ulrike Garscha, Erik Romp, Simona Pace, Antonietta Rossi, Veronika Temml, Daniela Schuster, Stefanie König, Jana Gerstmeier, Stefanie Liening, Markus Werner, Heiner Atze, Sandra Wittmann, Christina Weinigel, Silke Rummler, Gerhard K Scriba, Lidia Sautebin, Oliver Werz
Arachidonic acid (AA) is metabolized to diverse bioactive lipid mediators. Whereas the 5-lipoxygenase-activating protein (FLAP) facilitates AA conversion by 5-lipoxygenase (5-LOX) to pro-inflammatory leukotrienes (LTs), the soluble epoxide hydrolase (sEH) degrades anti-inflammatory epoxyeicosatrienoic acids (EETs). Accordingly, dual FLAP/sEH inhibition might be advantageous drugs for intervention of inflammation. We present the in vivo pharmacological profile and efficiency of N-[4-(benzothiazol-2-ylmethoxy)-2-methylphenyl]-N'-(3,4-dichlorophenyl)urea (diflapolin) that dually targets FLAP and sEH...
August 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28804553/sirt3-attenuates-doxorubicin-induced-cardiac-hypertrophy-and-mitochondrial-dysfunction-via-suppression-of-bnip3
#14
Qiong Du, Bin Zhu, Qing Zhai, Bo Yu
Doxorubicin (Dox) is an anthracycline antibiotic widely used in cancer treatment. Although its antitumor efficacy appears to be dose dependent, its clinical use is greatly restricted by development of cardiotoxicity. Sirtuin-3 (Sirt3) is the major deacetylase within the mitochondrial matrix that plays an important role in regulation of cardiac function. This study was performed to identify the regulatory role of Sirt3 on Dox-induced cardiac hypertrophy and mitochondrial dysfunction in rats in vivo and in vitro...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28668885/interactive-analysis-of-tx-1123-with-cyclo-oxygenase-design-of-cox2-selective-tx-analogs
#15
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
#16
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. Although the consequences of induced astrocytic aromatization are intensely studied, little is known about what factors induce aromatase...
August 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28571535/nonsteroidal-anti-inflammatory-drugs-exploiting-bivalent-coxib-tp-antagonists-for-the-control-of-cardiovascular-risk
#17
REVIEW
Silvia Carnevali, Carola Buccellati, Chiara Bolego, Massimo Bertinaria, G Enrico Rovati, Angelo Sala
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are some of the most widely prescribed or dispensed over the counter analgesics and antipyretics that act by inhibiting prostaglandins 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...
2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28539709/multipathway-integrated-adjustment-mechanism-of-glycyrrhiza-triterpenes-curing-gastric-ulcer-in-rats
#18
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
#19
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...
August 15, 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
#20
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...
July 5, 2017: European Journal of Pharmacology
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