Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are of huge therapeutic benefit in the treatment of rheumatoid arthritis and various types of inflammatory conditions. The target for these drugs is cyclooxygenase (COX), a rate-limiting enzyme involved in the conversion of arachidonic acid into inflammatory prostaglandins. COX-2 selective inhibitors are believed to have the same anti-inflammatory, anti-pyretic and analgesic activities as that of nonselective inhibitor NSAIDs with little or none of the gastrointestinal side effects. Thus, in the last 6-7 years several selective COX-2 inhibitors including coxibs were discovered and introduced into clinic. Recent reports evidence that selective COX-2 inhibitor such as rofecoxib, can lead to thrombotic cardiovascular events through inhibition of prostacyclin formation in the infracted heart. This has resulted in withdrawal of rofecoxib from the clinic in September 2004. Moreover, the COX-2/COX-1 selectivity ratio is vital in the design of COX-2 inhibitory drugs, as it is clear from rofecoxib, which is more than 50-fold COX-2 selective. After looking at all above mentioned facts, natural product-based compounds seem better as these compounds are generally supposed to be devoid of severe side effects. The literature indicates that natural product-based compounds are mainly COX-1 selective. Through minor semisynthetic changes in the structures, their selectivity towards COX-2 can be increased. The present review article addresses natural product COX inhibitors of plant and marine origin, reported during last ten years and their advantages, possible leads for further development and current status. In addition we describe our experience in the characterization, design and synthesis of potential natural COX inhibitors.
Keywords: Anti-inflammatory, natural products, cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2)
Current Medicinal Chemistry
Title: Cyclooxygenase Inhibitory Natural Products: Current Status
Volume: 13 Issue: 6
Author(s): Sanjay M. Jachak
Affiliation:
Keywords: Anti-inflammatory, natural products, cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2)
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are of huge therapeutic benefit in the treatment of rheumatoid arthritis and various types of inflammatory conditions. The target for these drugs is cyclooxygenase (COX), a rate-limiting enzyme involved in the conversion of arachidonic acid into inflammatory prostaglandins. COX-2 selective inhibitors are believed to have the same anti-inflammatory, anti-pyretic and analgesic activities as that of nonselective inhibitor NSAIDs with little or none of the gastrointestinal side effects. Thus, in the last 6-7 years several selective COX-2 inhibitors including coxibs were discovered and introduced into clinic. Recent reports evidence that selective COX-2 inhibitor such as rofecoxib, can lead to thrombotic cardiovascular events through inhibition of prostacyclin formation in the infracted heart. This has resulted in withdrawal of rofecoxib from the clinic in September 2004. Moreover, the COX-2/COX-1 selectivity ratio is vital in the design of COX-2 inhibitory drugs, as it is clear from rofecoxib, which is more than 50-fold COX-2 selective. After looking at all above mentioned facts, natural product-based compounds seem better as these compounds are generally supposed to be devoid of severe side effects. The literature indicates that natural product-based compounds are mainly COX-1 selective. Through minor semisynthetic changes in the structures, their selectivity towards COX-2 can be increased. The present review article addresses natural product COX inhibitors of plant and marine origin, reported during last ten years and their advantages, possible leads for further development and current status. In addition we describe our experience in the characterization, design and synthesis of potential natural COX inhibitors.
Export Options
About this article
Cite this article as:
Jachak M. Sanjay, Cyclooxygenase Inhibitory Natural Products: Current Status, Current Medicinal Chemistry 2006; 13 (6) . https://dx.doi.org/10.2174/092986706776055698
DOI https://dx.doi.org/10.2174/092986706776055698 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
- Announcements
Related Articles
-
Compositions for Treatment of Cancer and Inflammation
Recent Patents on Anti-Cancer Drug Discovery Oral Tolerance in the Treatment of Rheumatoid Arthritis
Current Drug Targets - Inflammation & Allergy Pro- and Anti-Arrhythmic Effects of Anti-Inflammatory Drugs
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cytokine-Directed Therapy in Asthma
Current Drug Targets - Inflammation & Allergy The Role of Coagulation in Chronic Inflammatory Disorders: A Jack of All Trades
Current Pharmaceutical Design Evaluation of in vivo Anti-inflammatory and Analgesic Activities of Novel Derivatives of Ugi-4CR
Mini-Reviews in Medicinal Chemistry Monoclonal Antibodies: New Therapeutic Agents for Autoimmune Hemolytic Anemia?
Endocrine, Metabolic & Immune Disorders - Drug Targets Neutrophil Derived Microvesicles: Emerging Role of a Key Mediator to the Immune Response
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of 1,4-Benzothiazine Derivatives in Medicinal Chemistry
Mini-Reviews in Medicinal Chemistry Antifolates - Past, Present and Future
Current Medicinal Chemistry - Anti-Cancer Agents Irreversible Inhibition of Serine Proteases – Design and In Vivo Activity of Diaryl α-Aminophosphonate Derivatives
Current Medicinal Chemistry Ω-3 Polyunsaturated Fatty Acids and Immune-Mediated Diseases: Inflammatory Bowel Disease and Rheumatoid Arthritis
Current Pharmaceutical Design Strategies of Functional Foods Promote Sleep in Human Being
Current Signal Transduction Therapy The Role of Synovial Fibroblasts in Mediating Joint Destruction in Rheumatoid Arthritis
Current Pharmaceutical Design Potential Targets for Anti-Inflammatory and Anti-Allergic Activities of Marine Algae: An Overview
Inflammation & Allergy - Drug Targets (Discontinued) Monoclonal Antibody-based Genetic Immunotherapy
Current Gene Therapy IL-1 Cytokines in Cardiovascular Disease: Diagnostic, Prognostic and Therapeutic Implications
Cardiovascular & Hematological Agents in Medicinal Chemistry Update on the Use of Biologics in Vasculitides
Current Pharmaceutical Biotechnology Flow Cytometric Analysis of Protein Aggregates
Protein & Peptide Letters Gene Therapy Approaches for Cartilage Injury and Osteoarthritis
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents