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 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Targeting Interleukin (IL) 5 for Asthma and Hypereosinophilic Diseases
Recent Patents on Inflammation & Allergy Drug Discovery Angiotensin II, Cell Proliferation and Angiogenesis Regulator: Biologic and Therapeutic Implications in Cancer
Current Vascular Pharmacology Natural Flora and Anticancer Regime: Milestones and Roadmap
Anti-Cancer Agents in Medicinal Chemistry Current and Experimental Antibody-Based Therapeutics: Insights, Breakthroughs, Setbacks and Future Directions
Current Molecular Medicine Immunomodulation in Inflammatory Neuropathies: Rationale and Safety
Current Drug Safety On Therapeutic Drug Monitoring of Thiopurines in Inflammatory Bowel Disease; Pharmacology, Pharmacogenomics, Drug Intolerance and Clinical Relevance
Current Drug Metabolism Medicolegal Aspects of Disclosure of Side Effects of Biologic Drugs in Rheumatology: A Pilot Study
New Emirates Medical Journal What is the Optimal Treatment for Anemia in Inflammatory Bowel Disease?
Current Drug Delivery Polyglandular Autoimmune Syndromes
Current Immunology Reviews (Discontinued) A Pathogenetic Approach to Autoimmune Skin Disease Therapy: Psoriasis and Biological Drugs, Unresolved Issues, and Future Directions
Current Pharmaceutical Design Use of Toll-Like Receptor 3 Agonists Against Respiratory Viral Infections
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cyclooxygenase and Neuroinflammation in Parkinsons Disease Neurodegeneration
Current Neuropharmacology Signal Transduction Pathways of Inflammatory Gene Expressions and Therapeutic Implications
Current Pharmaceutical Design Editorial (Thematic Issue: Chemistry Bordering Biology: Highlights from the XXXIV Biennial Meeting of the RSEQ)
Current Topics in Medicinal Chemistry Therapeutic Potential of Targeting TREM-1 in Inflammatory Diseases and Cancer
Current Pharmaceutical Design Pulmonary Arterial Hypertension: Need to Treat
Inflammation & Allergy - Drug Targets (Discontinued) Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery A Review of Natural and Synthetic Antioxidants Important for Health and Longevity
Current Medicinal Chemistry Chemometrics-assisted Spectrofluorimetric Determination of Two Co-administered Drugs of Major Interaction, Methotrexate and Aspirin, in Human Urine Following Acid-induced Hydrolysis
Combinatorial Chemistry & High Throughput Screening COVID-19: Role of Robotics, Artificial Intelligence and Machine Learning During the Pandemic
Current Medical Imaging