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
-
Pharmacophore Modelling: A Forty Year Old Approach and its Modern Synergies
Current Medicinal Chemistry Capillary Degeneration and Right Ventricular Remodeling Due to Hypoxic Stress with Sugen5416
Current Vascular Pharmacology Neurogenic Drugs and Compounds
Recent Patents on CNS Drug Discovery (Discontinued) Recent Advancement of Direct-acting Antiviral Agents (DAAs) in Hepatitis C Therapy
Mini-Reviews in Medicinal Chemistry Celastrol and Terpenes as Anti-Infective Agents
Anti-Infective Agents in Medicinal Chemistry The Spectrum of Nimesulide-Induced-Hepatotoxicity. An Overview
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Molecular and Genetic Profiling of Prostate Cancer: Implications for Future Therapy
Current Cancer Therapy Reviews TMEM16A/B Associated CaCC: Structural and Functional Insights
Protein & Peptide Letters Wolbachia and Its Implications for the Immunopathology of Filariasis
Endocrine, Metabolic & Immune Disorders - Drug Targets Bioactivity and Pharmacological Actions of Carbon Monoxide-Releasing Molecules
Current Pharmaceutical Design Flavonoids and Anthranquinones as Xanthine Oxidase and Monoamine Oxidase Inhibitors: A New Approach Towards Inflammation and Oxidative Stress
Current Topics in Medicinal Chemistry Transgenic Mouse Models of Alzheimer Disease: Developing a Better Model as a Tool for Therapeutic Interventions
Current Pharmaceutical Design Effect of Dietary Supplementation of Black Seed (N. Sativa L.) on Lipid Profile of Patients Suffering from Diabetes
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry NMR Spectroscopy of Paramagnetic Heme Proteins
Current Inorganic Chemistry (Discontinued) Fluorescent Dyes for Bio-Applications in the Patent Literature
Recent Patents on Materials Science The Ambivalent Role of Apoptosis in Experimental Autoimmune Encephalomyelitis and Multiple Sclerosis
Current Pharmaceutical Design Molecular Imaging of Vascular Inflammation
Current Pharmaceutical Design Defining the Role of Food Allergy in a Population of Adult Patients with Eosinophilic Esophagitis
Inflammation & Allergy - Drug Targets (Discontinued) Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium
Current Drug Targets Relationship Between HIV-RNA Load in Blood and Semen in Antiretroviral-Naive and Experienced Men and Effect of Asymptomatic Sexually Transmissible Infections
Current HIV Research