Abstract
We studied in vitro effects of three different drugs (ibuprofen, meloxicam and methotrexate) which are often used in rheumatoid arthritis (RA) treatment on human serum paraoxanase1 (PON1) enzyme activity. The drugs used in RA treatment decreased the in vitro PON1 activity. The inhibition mechanism of ibuprofen and methotrexate were noncompetitive whereas meloxicam was a competitive inhibitor. The IC50 values for ibuprofen, meloxicam and methotrexate were calculated to be 0.35 mM, 0.10 mM, and 0.18 mM, respectively, and the Ki constants were calculated to be 0.890 mM, 0.125 mM, and 0.260 mM, respectively. The IC50 and Ki values showed the maximum inhibition of meloxicam drugs. We propose a prediction scheme for the interaction of meloxicam with the PON1 active site because we thought that meloxicam interacts with the amino acids which are in the PON1 enzyme active site. The results we found showed that these drugs which are often used in RA treatment in vitro inhibit the activity of the enzyme with different inhibition mechanisms at low doses.
Keywords: Ibuprofen, inhibition, meloxicam, methotrexate. paraoxonase1.
Protein & Peptide Letters
Title:In Vitro Inhibition Of Three Different Drugs Used In Rheumatoid Arthritis Treatment On Human Serum Paraoxanase 1 Enzyme Activity
Volume: 23 Issue: 1
Author(s): Esra Dilek and M. Fatih Polat
Affiliation:
Keywords: Ibuprofen, inhibition, meloxicam, methotrexate. paraoxonase1.
Abstract: We studied in vitro effects of three different drugs (ibuprofen, meloxicam and methotrexate) which are often used in rheumatoid arthritis (RA) treatment on human serum paraoxanase1 (PON1) enzyme activity. The drugs used in RA treatment decreased the in vitro PON1 activity. The inhibition mechanism of ibuprofen and methotrexate were noncompetitive whereas meloxicam was a competitive inhibitor. The IC50 values for ibuprofen, meloxicam and methotrexate were calculated to be 0.35 mM, 0.10 mM, and 0.18 mM, respectively, and the Ki constants were calculated to be 0.890 mM, 0.125 mM, and 0.260 mM, respectively. The IC50 and Ki values showed the maximum inhibition of meloxicam drugs. We propose a prediction scheme for the interaction of meloxicam with the PON1 active site because we thought that meloxicam interacts with the amino acids which are in the PON1 enzyme active site. The results we found showed that these drugs which are often used in RA treatment in vitro inhibit the activity of the enzyme with different inhibition mechanisms at low doses.
Export Options
About this article
Cite this article as:
Dilek Esra and Polat Fatih M., In Vitro Inhibition Of Three Different Drugs Used In Rheumatoid Arthritis Treatment On Human Serum Paraoxanase 1 Enzyme Activity, Protein & Peptide Letters 2016; 23 (1) . https://dx.doi.org/10.2174/0929866522666151013130102
DOI https://dx.doi.org/10.2174/0929866522666151013130102 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
The Oral Administration Effect of Drug Mannuronic Acid (M2000) on Gene Expression of Matrix and Tissue Inhibitor of Metalloproteinases in Rheumatoid Arthritis Patients
Current Drug Discovery Technologies Satisfaction with Social Roles and Physical Function in Immune-mediated Inflammatory Diseases: A Cross-Sectional Study
Reviews on Recent Clinical Trials Irreversible Kinase Inhibitors Targeting Cysteine Residues and their Applications in Cancer Therapy
Mini-Reviews in Medicinal Chemistry Chemical Instability Determines the Biological Action of the Artemisinins
Current Medicinal Chemistry Phage Display Derived Therapeutic Antibodies
Current Pharmaceutical Biotechnology Bhasma: Indian Perspective of Nanomedicinal Technology
Recent Patents on Nanomedicine Chemokine Receptors as Targets for Cancer Therapy
Current Pharmaceutical Design Synthesis and Biological Activity of a New Class of Azetidinones Compounds as Potential HLE Inhibitors
Letters in Drug Design & Discovery Identification of Candidate Genetic Markers and a Novel 4-genes Diagnostic Model in Osteoarthritis through Integrating Multiple Microarray Data
Combinatorial Chemistry & High Throughput Screening Strychni Semen Combined with Atractylodes Macrocephala Koidz Attenuates Rheumatoid Arthritis by Regulating Apoptosis
Current Computer-Aided Drug Design Integrated Network Pharmacology and Cellular Assay to Explore the Mechanisms of Selenized Tripterine Phytosomes (Se@Tri-PTs) Alleviating Podocyte Injury in Diabetic Nephropathy
Current Pharmaceutical Design A Single Fas Gene Mutation Changes Lupus Onset, Severity, Location, and Molecular Abnormalities in Mice
Current Molecular Medicine Integrin Antagonists: A Special Emphasis on Structural Requirements of N-benzoyl-L-biphenylalanines as α4β7 and α4β1 Antagonists
Current Signal Transduction Therapy Modern Therapeutic Strategies for Autoimmune Diseases
Current Pharmaceutical Design Treatment of Large Vessel Vasculitis
Current Immunology Reviews (Discontinued) Drug-Induced Aseptic Meningitis
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Central Nervous System-Related
Current Bioactive Compounds Right Ventricle and Autoimmune Diseases
Current Rheumatology Reviews Drug Discovery and Protein Tyrosine Phosphatases
Current Medicinal Chemistry VEGF Inhibitors in Cancer Therapy
Current Pharmaceutical Design