Abstract
Inflammation is the primary host defense mechanism against all forms of injury. Excessive or inadequate activation of the system can have serious effects, as can the failure of inactivation mechanisms. Coumarins can reduce tissue edema and inflammation and inhibit prostaglandin biosynthesis, which involves fatty acid hydroperoxy intermediates. It is to be expected that coumarins might affect the formation and scavenging of reactive substances derived from oxygen species (ROS) and influence processes involving free radical-mediated injury, as can flavonoids. During these years a small number of (Q)SAR studies concerning coumarins as NSAIDs has been presented and reviewed. In this research we tried to examine the structure-function relationship for coumarins, presenting antiinflammatory activity. Coumarin (1), the prototypical compound presents anti-inflammatory activity. The hydroxylaromatic substituted derivatives (5- or 6- or 7-hydroxy or the vicinal dihydroxy) seems to be potent inhibitors of lipoxygenase. Several synthetic derivatives simple or more complicated were found to be potent antiinflammatories/antioxidant agents.
Keywords: Coumarins, antiinflammatories/antioxidant agents, structure-activity relationships
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title: The Anti-inflammatory Effect of Coumarin and its Derivatives
Volume: 6 Issue: 4
Author(s): D. J. Hadjipavlou-Litina, K. E. Litinas and C. Kontogiorgis
Affiliation:
Keywords: Coumarins, antiinflammatories/antioxidant agents, structure-activity relationships
Abstract: Inflammation is the primary host defense mechanism against all forms of injury. Excessive or inadequate activation of the system can have serious effects, as can the failure of inactivation mechanisms. Coumarins can reduce tissue edema and inflammation and inhibit prostaglandin biosynthesis, which involves fatty acid hydroperoxy intermediates. It is to be expected that coumarins might affect the formation and scavenging of reactive substances derived from oxygen species (ROS) and influence processes involving free radical-mediated injury, as can flavonoids. During these years a small number of (Q)SAR studies concerning coumarins as NSAIDs has been presented and reviewed. In this research we tried to examine the structure-function relationship for coumarins, presenting antiinflammatory activity. Coumarin (1), the prototypical compound presents anti-inflammatory activity. The hydroxylaromatic substituted derivatives (5- or 6- or 7-hydroxy or the vicinal dihydroxy) seems to be potent inhibitors of lipoxygenase. Several synthetic derivatives simple or more complicated were found to be potent antiinflammatories/antioxidant agents.
Export Options
About this article
Cite this article as:
Hadjipavlou-Litina J. D., Litinas E. K. and Kontogiorgis C., The Anti-inflammatory Effect of Coumarin and its Derivatives, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2007; 6 (4) . https://dx.doi.org/10.2174/187152307783219989
DOI https://dx.doi.org/10.2174/187152307783219989 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
VEGF Inhibitors in Cancer Therapy
Current Pharmaceutical Design TXNL1 Induces Apoptosis in Cisplatin Resistant Human Gastric Cancer Cell Lines
Current Cancer Drug Targets Recent Developments of p38α MAP Kinase Inhibitors as Antiinflammatory Agents Based on the Imidazole Scaffolds
Current Medicinal Chemistry Characterization of Heme Oxygenase in Adult Rodent Platelets
Current Neurovascular Research Update on the Therapy of Behçets Disease
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Inflammatory Mediators in Chronic Obstructive Pulmonary Disease
Current Drug Targets - Inflammation & Allergy Chronic Inflammatory Disorders and Accelerated Atherosclerosis: Chronic Kidney Disease
Current Pharmaceutical Design Regulatory Mechanism of the Gastric Hyperemic Response Following Barrier Disruption: Roles of Cyclooxygenase-1, the Prostaglandin E<sub>2</sub>/EP1 Receptor and Sensory Neurons
Current Pharmaceutical Design Particle Design of Membrane Emulsification for Protein Drug and Vaccine Delivery
Current Pharmaceutical Design Tianeptine: An Antidepressant with Memory-Protective Properties
Current Neuropharmacology The Brain, the Penis and Steroid Hormones: Clinical Correlates with Endothelial Dysfunction
Current Pharmaceutical Design Roles of TRAF6 in Central Nervous System
Current Neuropharmacology Interaction Between Bone and Muscle in Older Persons with Mobility Limitations
Current Pharmaceutical Design Vinyl Sulfone Containing Parasitic Cysteinyl Protease Inhibitors
Current Bioactive Compounds Application of Nanotechnology in Acupuncture
Current Nanoscience microRNAs, Gap Junctional Intercellular Communication and Mesenchymal Stem Cells in Breast Cancer Metastasis
Current Cancer Therapy Reviews Capsaicin-Sensitive Nociceptive Innervation of the Dura Mater: Implications for the Pathomechanism of Headache
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Role of Gut Microbiota in Human Health and Diseases
Current Nutrition & Food Science Potential Roles of Eosinophils in Cancer Therapy: Epidemiological Studies, Experimental Models, and Clinical Pathology
Recent Patents on Anti-Cancer Drug Discovery Patenting Human Genes and Stem Cells
Recent Patents on DNA & Gene Sequences