Kinetic basis for the activation of human cyclooxygenase-2 rather than cyclooxygenase-1 by nitric oxide

2018 ◽  
Vol 16 (5) ◽  
pp. 765-770 ◽  
Author(s):  
Jie Qiao ◽  
Lixin Ma ◽  
Justine Roth ◽  
Yamin Li ◽  
Yi Liu
Keyword(s):  
Nitric Oxide ◽  
Cyclooxygenase 2 ◽  
Cyclooxygenase 1

Kinetic basis for the activation of human cyclooxygenase-2 by nitric oxide.

scholarly journals gem-Difluorobisarylic derivatives: design, synthesis and anti-inflammatory effect

BMC Chemistry ◽  
2019 ◽  
Vol 13 (1) ◽  
Author(s):  
Abeer J. Ayoub ◽  
Layal Hariss ◽  
Nehme El-Hachem ◽  
Ghewa A. El-Achkar ◽  
Sandra E. Ghayad ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Protein Expression ◽  
Interleukin 6 ◽  
Cyclooxygenase 2 ◽  
Prostaglandin E ◽  
Diaryl Ethers ◽  
Cyclooxygenase 1 ◽  
Anti Inflammatory ◽  
Oxide Synthase

Abstract Introduction New fluorinated diaryl ethers and bisarylic ketones were designed and evaluated for their anti-inflammatory effects in primary macrophages. Methods The synthesis of the designed molecules started from easily accessible and versatile gem-difluoro propargylic derivatives. The desired aromatic systems were obtained using Diels–Alder/aromatization sequences and this was followed by Pd-catalyzed coupling reactions and, when required, final functionalization steps. Both direct inhibitory effects on cyclooxygenase-1 or -2 activities, protein expression of cyclooxygenase-2 and nitric oxide synthase-II and the production of prostaglandin E2, the pro-inflammatory nitric oxide and interleukin-6 were evaluated in primary murine bone marrow-derived macrophages in response to lipopolysaccharide. Docking of the designed molecules in cyclooxygenase-1 or -2 was performed. Results Only fluorinated compounds exerted anti-inflammatory activities by lowering the secretion of interleukin-6, nitric oxide, and prostaglandin E2, and decreasing the protein expression of inducible nitric oxide synthase and cyclooxygenase-2 in mouse primary macrophages exposed to lipopolysaccharide, as well as cyclooxygenase activity for some inhibitors with different efficiencies depending on the R-groups. Docking observation suggested an inhibitory role of cyclooxygenase-1 or -2 for compounds A3, A4 and A5 in addition to their capacity to inhibit nitrite, interleukin-6, and nitric oxide synthase-II and cyclooxygenase-2 expression. Conclusion The new fluorinated diaryl ethers and bisarylic ketones have anti-inflammatory effects in macrophages. These fluorinated compounds have improved potential anti-inflammatory properties due to the fluorine residues in the bioactive molecules.

Transient Up-regulation of Spinal Cyclooxygenase-2 and Neuronal Nitric Oxide Synthase following Surgical Inflammation

2003 ◽  
Vol 98 (1) ◽  
pp. 170-180 ◽  
Author(s):  
Sharron Dolan ◽  
James G. Kelly ◽  
Marie Huan ◽  
Andrea M. Nolan
Keyword(s):  
Nitric Oxide ◽  
Spinal Cord ◽  
Cyclooxygenase 2 ◽  
Lumbar Spinal Cord ◽  
Chain Reaction ◽  
Cyclooxygenase 1 ◽  
Polymerase Chain ◽  
Neuronal Nos ◽  
Lumbar Spinal ◽  
Oxide Synthase

Background Surgery induces pain and hyperalgesia postoperatively. The products of cyclooxygenases and nitric oxide synthase (NOS) have been implicated in the development of inflammatory pain and hyperalgesia experimentally, and the use of drugs clinically that modify cyclooxygenase activity has been advocated in the management of perioperative pain. However, regulation of these enzymes following surgery has not been studied. Methods Adult female sheep (n = 12) undergoing a midline laparotomy for collection of ova were used in this study. Lumbar and cervical spinal cord tissue was collected from animals euthanized 1 day and 6 or 7 days after surgery and processed for cyclooxygenase (cyclooxygenase-1 and cyclooxygenase-2), neuronal NOS mRNA expression using reverse-transcription polymerase chain reaction and hybridization. Tissues were also processed for NADPH-diaphorase staining and cyclooxygenase-1 and cyclooxygenase-2 protein expression by immunohistochemistry and Western blotting. Results No alteration in cyclooxygenase-1 or cyclooxygenase-2 mRNA or protein concentrations were detected in spinal cord by reverse-transcription polymerase chain reaction and Western blotting, respectively, at 1 day or 6 or 7 days after surgery. However, using techniques that localize mRNA and protein expression ( hybridization and immunohistochemistry, respectively), increases in cyclooxygenase-2 were identified in lamina V dorsal horn neurons in lumbar spinal cord 1 day after surgery. A significant increase in neuronal NOS mRNA was observed in lumbar spinal cord 1 day after surgery, localized to laminae I-II and lamina V neurons, which returned to baseline concentrations by 6 to 7 days. NADPH-diaphorase staining was significantly increased in laminae I-II in lumbar spinal cord 1 day after surgery but not after 6 to 7 days. Conclusions Spinal cyclooxygenase and neuronal NOS pathways are differentially altered following surgical inflammation. The early and transient nature of these changes suggests that these enzymes are implicated in postoperative pain and hypersensitivity.

Comparative Effects of Selective Cyclooxygenase 1 and Cyclooxygenase 2 Inhibitors on Myeloperoxidase and 3α-Hydroxysteroid Dehydrogenase

1996 ◽  
Vol 10 (2) ◽  
pp. 73-79 ◽  
Author(s):  
Nicholas L. Rider ◽  
Donald Pinto ◽  
Maryanne Covington ◽  
Michael J. Orwat ◽  
John Giannaras ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Cyclooxygenase 2 ◽  
Cyclooxygenase 1 ◽  
Cyclooxygenase 2 Inhibitors

Inhibition of inducible nitric oxide synthase and cyclooxygenase-2 expression by flavonoids isolated from Tanacetum microphyllum

2006 ◽  
Vol 6 (11) ◽  
pp. 1723-1728 ◽  
Author(s):  
José Antonio Guerra ◽  
María Francisca Molina ◽  
María José Abad ◽  
Angel María Villar ◽  
Paulina Bermejo
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Inducible Nitric Oxide Synthase ◽  
Cyclooxygenase 2 ◽  
Oxide Synthase ◽  
Inducible Nitric Oxide

Pro-Inflammatory Enzymes, Cyclooxygenase 1, Cyclooxygenase 2, and 5-Lipooxygenase, Inhibited by Stabilized Rice Bran Extracts

2009 ◽  
Vol 12 (3) ◽  
pp. 615-623 ◽  
Author(s):  
Bill Roschek ◽  
Ryan C. Fink ◽  
Dan Li ◽  
Matthew McMichael ◽  
Christine M. Tower ◽  
...  
Keyword(s):  
Rice Bran ◽  
Cyclooxygenase 2 ◽  
Cyclooxygenase 1
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