ArticleProceedings of the National Academy of Sciences of the United States of America2002
Potent antiarthritic properties of a glucocorticoid derivative, NCX-1015, in an experimental model of arthritis.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 81 citations in OpenAlex.
- Numerical Optimization of Prednisolone-Tacrolimus Loaded Ultraflexible Transethosomes for Transdermal Delivery Enhancement; Box-Behnken Design, Evaluation, Optimization, and Pharmacokinetic Study.Gels (Basel, Switzerland) · 2023Article
- The long winding road to the safer glucocorticoid receptor (GR) targeting therapies.Oncotarget · 2022Review
- Nitric-Oxide-Releasing Dexamethasone Derivative NCX-1005 Improves Lung Function and Attenuates Inflammation in Experimental Lavage-Induced ARDS.Pharmaceutics · 2021Article
- Аtherosclerosis-like changes in the rabbit aortic wall induced by immunization with native high-density lipoproteins.Immunity, inflammation and disease · 2020Article
- Dexamethasone modified by gamma-irradiation as a novel anticancer drug in human non-small cell lung cancer.PloS one · 2018Article
- Novel Drug Delivery Systems Tailored for Improved Administration of Glucocorticoids.International journal of molecular sciences · 2017Review
- Inhibition of matrix metalloproteinase-9 by a barbiturate-nitrate hybrid ameliorates dextran sulphate sodium-induced colitis: effect on inflammation-related genes.British journal of pharmacology · 2017Article
- A novel nitro-dexamethasone inhibits agr system activity and improves therapeutic effects in MRSA sepsis models without antibiotics.Scientific reports · 2016Article
- Endothelial Response to Glucocorticoids in Inflammatory Diseases.Frontiers in immunology · 2016Review
- Comparative efficacy of a secretory phospholipase A2 inhibitor with conventional anti-inflammatory agents in a rat model of antigen-induced arthritis.Arthritis research & therapy · 2011Article
- Anti-inflammatory glucocorticoid drugs: reflections after 60 years.Inflammopharmacology · 2011Review
- Alpha-methylprednisolone conjugated cyclodextrin polymer-based nanoparticles for rheumatoid arthritis therapy.International journal of nanomedicine · 2008Article
- Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.Proceedings of the National Academy of Sciences of the United States of America · 2007Article
- Building a better aspirin: gaseous solutions to a century-old problem.British journal of pharmacology · 2007Review
- Calcitonin and prednisolone display antagonistic actions on bone and have synergistic effects in experimental arthritis.The American journal of pathology · 2007Article
- [Current insights into the development of new glucocorticoid receptor ligands].Zeitschrift fur Rheumatologie · 2005Review
- Anti-inflammatory effects of nitric oxide-releasing hydrocortisone NCX 1022, in a murine model of contact dermatitis.British journal of pharmacology · 2004Article
- Acetaminophen hepatotoxicity: NO to the rescue.British journal of pharmacology · 2004Article
- Enhanced anti-inflammatory potency of a nitric oxide-releasing prednisolone derivative in the rat.British journal of pharmacology · 2003Article
- NCX-1015, a nitric-oxide derivative of prednisolone, enhances regulatory T cells in the lamina propria and protects against 2,4,6-trinitrobenzene sulfonic acid-induced colitis in mice.Proceedings of the National Academy of Sciences of the United States of America · 2002Article
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5 authors.
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Abstract
Here, we describe the improved antiarthritic properties of a nitric oxide-releasing derivative of prednisolone that includes a sparing of the effects on bone. Glucocorticoids are widely used in the treatment of chronic inflammatory pathologies, but their use is often accompanied by side effects, including osteoporosis. Recently, a new steroid able to release low levels of nitric oxide showed potent inhibition of leukocyte trafficking and chemokine generation in models of acute inflammation. The objective of this study was to assess the anti-inflammatory activity of this nitric-oxide releasing glucocorticoid, nitro-prednisolone (NCX-1015), in parallel with the parent compound prednisolone and a control molecule lacking an NO group, (NCX-1016), in a model of rat collagen-induced arthritis. Dosing of rats with NCX-1015 (0.4-4 micromol/kg, i.p.) greatly reduced all parameters of inflammation. A significant but inferior anti-inflammatory effect also was obtained with prednisolone. Collagen-induced arthritic rats had elevated pyridinoline values (> 60% over naïve rats), indicating bone and cartilage erosion; this increase was prevented by NCX-1015 but not by prednisolone or NCX-1016 treatment. In vitro, prednisolone (1 nM), but not NCX-1015, elevated bone resorbing activity of rat primary osteoclasts. In conclusion, NCX-1015 is a steroid derivative with a potential for the treatment of chronic inflammatory pathologies and that has milder side effects anticipated on the bone compartment.
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