Abstract
Oxidative stress is implicated in the pathogenesis of different human diseases: Alzheimer, Parkinson, Huntington, amyotrophic lateral sclerosis (Lou Gehrig's disease), Down’s syndrome, atherosclerosis, vascular disease, cancer, diabetes mellitus type 1 and type 2, age – related macular degeneration, psoriatic arthritis. The aim of current study is to summarize the scientific evidences for the antioxidant and neuroprotective activity of Galantamine and some of its derivatives. Galantamine is a scavenger of reactive oxygen species and causes neuroprotective effect by lowering the oxidative neuronal damage, through the following pathways: 1) prevention of the activation of P2X7 receptors; 2) protection of mitochondrial membrane potential; 3) pre – vention of the membrane fluidity disturbances. Another mechanism is the decreasing of the overproduction of reactive oxygen species, a result from the increasing of acetylcholine level due to: 1) acethylcholinesterase inhibition; 2) allosteric potentiation of α7 – subtype of nicotinic acetylcholine receptors. A close relationship between acethylcholinesterase inhibition and reduced oxidative injury is observed. Through allosteric potentiation of the α7 – subtype of nicotinic acetylcholine receptors, the drug leads to induction of phosphorylation of serine – threonine protein kinase, stimulates phosphoinositide 3 – kinase and elevates the expression of protective protein Bcl – 2. By activation of these important neuroprotective cascades, Galantamine exerts neuroprotection against a variety of cytotoxic agents (β – amyloid peptide, glutamate, hydrogen peroxide, oxygen and glucose deprivation). The new trend in therapy of Alzheimer's disease will be the investigation and application of compounds such as Galantamine derivatives, which possess acethylcholinesterase and γ – secretase inhibitory activity and antioxidant properties.
Keywords: Antioxidant activity, derivatives, galantamine, oxidative stress, neurodegeneration.
Current Medicinal Chemistry
Title:Antioxidant Activity of Galantamine and Some of its Derivatives
Volume: 20 Issue: 36
Author(s): D. Tsvetkova, D. Obreshkova, D. Zheleva – Dimitrova and L. Saso
Affiliation:
Keywords: Antioxidant activity, derivatives, galantamine, oxidative stress, neurodegeneration.
Abstract: Oxidative stress is implicated in the pathogenesis of different human diseases: Alzheimer, Parkinson, Huntington, amyotrophic lateral sclerosis (Lou Gehrig's disease), Down’s syndrome, atherosclerosis, vascular disease, cancer, diabetes mellitus type 1 and type 2, age – related macular degeneration, psoriatic arthritis. The aim of current study is to summarize the scientific evidences for the antioxidant and neuroprotective activity of Galantamine and some of its derivatives. Galantamine is a scavenger of reactive oxygen species and causes neuroprotective effect by lowering the oxidative neuronal damage, through the following pathways: 1) prevention of the activation of P2X7 receptors; 2) protection of mitochondrial membrane potential; 3) pre – vention of the membrane fluidity disturbances. Another mechanism is the decreasing of the overproduction of reactive oxygen species, a result from the increasing of acetylcholine level due to: 1) acethylcholinesterase inhibition; 2) allosteric potentiation of α7 – subtype of nicotinic acetylcholine receptors. A close relationship between acethylcholinesterase inhibition and reduced oxidative injury is observed. Through allosteric potentiation of the α7 – subtype of nicotinic acetylcholine receptors, the drug leads to induction of phosphorylation of serine – threonine protein kinase, stimulates phosphoinositide 3 – kinase and elevates the expression of protective protein Bcl – 2. By activation of these important neuroprotective cascades, Galantamine exerts neuroprotection against a variety of cytotoxic agents (β – amyloid peptide, glutamate, hydrogen peroxide, oxygen and glucose deprivation). The new trend in therapy of Alzheimer's disease will be the investigation and application of compounds such as Galantamine derivatives, which possess acethylcholinesterase and γ – secretase inhibitory activity and antioxidant properties.
Export Options
About this article
Cite this article as:
Tsvetkova D., Obreshkova D., Zheleva – Dimitrova D. and Saso L., Antioxidant Activity of Galantamine and Some of its Derivatives, Current Medicinal Chemistry 2013; 20 (36) . https://dx.doi.org/10.2174/09298673113209990148
DOI https://dx.doi.org/10.2174/09298673113209990148 |
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
-
Cannabinoids and Neurodegenerative Diseases
CNS & Neurological Disorders - Drug Targets A Single Pill to Treat Postmenopausal Hypertension? Not Yet
Current Topics in Medicinal Chemistry Adverse Effects of Statins - Mechanisms and Consequences
Current Drug Safety Emerging Role of Stem Cells - Derived Exosomes as Valuable Tools for Cardiovascular Therapy
Current Stem Cell Research & Therapy Pharmacological manipulation of peripheral vascular resistance in special clinical situations after pediatric cardiac surgery
Current Vascular Pharmacology Differential Modulation of Autophagy Contributes to the Protective Effects of Resveratrol and Co-Enzyme Q10 in Photoaged Mice
Current Molecular Pharmacology Interactive Effect of Cigarette Smoking and Gene Variants for Predisposing to Cardiovascular Disease
Current Pharmaceutical Design Lipid Based Nanosystems for Curcumin: Past, Present and Future
Current Pharmaceutical Design Aging is Neuroprotective During Global Ischemia but Leads to Increased Caspase-3 and Apoptotic Activity in Hippocampal Neurons
Current Neurovascular Research Vasoactive Factors and Diabetic Retinopathy: Vascular Endothelial Growth Factor, Cycoloxygenase-2 and Nitric Oxide
Current Pharmaceutical Design Cardioprotection Against Ischemia/Reperfusion Injury and Chromogranin ADerived Peptides
Current Medicinal Chemistry Role of Netrin-1 Beyond the Brain: From Biomarker of Tissue Injury to Therapy for Inflammatory Diseases
Recent Patents on Biomarkers Autophagy Fails to Alter Withaferin A-Mediated Lethality in Human Breast Cancer Cells
Current Cancer Drug Targets Heme Oxygenase in Regulation of Renal Function and Blood Pressure
Current Hypertension Reviews High Sensitivity Troponin in Cardiovascular Disease. Is There More Than a Marker of Myocardial Death?
Current Topics in Medicinal Chemistry Inhibition of Cytochrome P450 1A2-Mediated Metabolism and Production of Reactive Oxygen Species by Heme Oxygenase-1 in Rat Liver Microsomes
Drug Metabolism Letters Critical Role of the Endocannabinoid System in the Regulation of Food Intake and Energy Metabolism, with Phylogenetic, Developmental, and Pathophysiological Implications
Endocrine, Metabolic & Immune Disorders - Drug Targets Conantokins: Peptide Antagonists of NMDA Receptors
Current Medicinal Chemistry Pharmaceutical Aspects of Hemoglobin-Based Oxygen Carriers
Current Drug Delivery Cellular Mechanisms of the Protective Effect of Polyphenols on the Neurovascular Unit in Strokes
Cardiovascular & Hematological Agents in Medicinal Chemistry