Abstract
Alzheimer's disease is a neurodegenerative disorder that results in progressive and irreversible central nervous system impairment, which has become one of the severe issues recently. The most successful approach of Alzheimer’s treatment is the administration of cholinesterase inhibitors to prevent the hydrolysis of acetylcholine and subsequently improve cholinergic postsynaptic transmission. This review highlights a class of heterocycles, namely xanthone, and its remarkable acetylcholinesterase inhibitory activities. Naturally occurring xanthones, including oxygenated, prenylated, pyrano, and glycosylated xanthones, exhibited promising inhibition effects towards acetylcholinesterase. Interestingly, synthetic xanthone derivatives with complex substituents such as alkyl, pyrrolidine, piperidine, and morpholine have shown greater acetylcholinesterase inhibition activities. The structure-activity relationship of xanthones revealed that the type and position of the substituent(s) attached to the xanthone moiety influenced acetylcholinesterase inhibition activities where hydrophobic moiety will lead to an improved activity by contributing to the π-π interactions, as well as the hydroxy substituent(s) by forming hydrogen-bond interactions. Thus, further studies, including quantitative structure-activity relationship, in vivo and clinical validation studies are crucial for the development of xanthones into novel anti-Alzheimer's disease drugs.
Keywords: Enzyme kinetic, hydrogen bonding, hydrophobic interaction, structure-activity relationship (SAR), synthesis, Alzheimer's disease.
Mini-Reviews in Medicinal Chemistry
Title:Xanthone: Potential Acetylcholinesterase Inhibitor for Alzheimer's Disease Treatment
Volume: 21 Issue: 17
Author(s): Vincentsia Vienna Vanessa and Siau Hui Mah*
Affiliation:
- School of Biosciences, Faculty of Health and Medical Sciences, Taylor’s University Lakeside Campus, Subang Jaya,Malaysia
Keywords: Enzyme kinetic, hydrogen bonding, hydrophobic interaction, structure-activity relationship (SAR), synthesis, Alzheimer's disease.
Abstract: Alzheimer's disease is a neurodegenerative disorder that results in progressive and irreversible central nervous system impairment, which has become one of the severe issues recently. The most successful approach of Alzheimer’s treatment is the administration of cholinesterase inhibitors to prevent the hydrolysis of acetylcholine and subsequently improve cholinergic postsynaptic transmission. This review highlights a class of heterocycles, namely xanthone, and its remarkable acetylcholinesterase inhibitory activities. Naturally occurring xanthones, including oxygenated, prenylated, pyrano, and glycosylated xanthones, exhibited promising inhibition effects towards acetylcholinesterase. Interestingly, synthetic xanthone derivatives with complex substituents such as alkyl, pyrrolidine, piperidine, and morpholine have shown greater acetylcholinesterase inhibition activities. The structure-activity relationship of xanthones revealed that the type and position of the substituent(s) attached to the xanthone moiety influenced acetylcholinesterase inhibition activities where hydrophobic moiety will lead to an improved activity by contributing to the π-π interactions, as well as the hydroxy substituent(s) by forming hydrogen-bond interactions. Thus, further studies, including quantitative structure-activity relationship, in vivo and clinical validation studies are crucial for the development of xanthones into novel anti-Alzheimer's disease drugs.
Export Options
About this article
Cite this article as:
Vanessa Vienna Vincentsia and Mah Hui Siau *, Xanthone: Potential Acetylcholinesterase Inhibitor for Alzheimer's Disease Treatment, Mini-Reviews in Medicinal Chemistry 2021; 21 (17) . https://dx.doi.org/10.2174/1389557521666210212152514
DOI https://dx.doi.org/10.2174/1389557521666210212152514 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
Vascular Endothelial Growth Factor in Central Nervous System Injuries – A Vascular Growth Factor Getting Nervous?
Current Neurovascular Research Transgenic Mice as a Model for Alzheimers Disease
Current Alzheimer Research Dimerization of C-terminal Truncations of α-synuclein and its Effect on the Aggregation Propensity: A Potential of Mean Force Study
Current Chemical Biology Stem Cell-Mediated Gene Delivering for the Treatment of Cerebral Ischemia: Progress and Prospectives
Current Drug Targets Patterns of Self-Medication with Medicinal Plants and Related Adverse Events - A South American Survey
Current Drug Safety Transforming Cytosolic Proteins into “Insoluble” and Membrane-toxic Forms Triggering Diseases/Aging by Genetic, Pathological or Environmental Factors
Protein & Peptide Letters Structural Characterization of Amyloid β17-42 Dimer by Potential of Mean Force Analysis: Insights from Molecular Dynamics Simulations
Protein & Peptide Letters Meet Our Editorial Board Member
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Commentary: Neurorestoratology: A Concept and Emerging Discipline in the Treatment of Neurological Disorders
CNS & Neurological Disorders - Drug Targets Editorial - Progress and Vision for ‘Current Aging Science’
Current Aging Science Can't Always Get What you Want? Try an Indirect Route you Just Might Get What you Need: A Study on Access to Genetic Data by Canadian Life Insurers
Current Pharmacogenomics and Personalized Medicine Reversible and Irreversible Aggregation of Proteins from the FET Family: Influence of Repeats in Protein Chain on Its Aggregation Capacity
Current Protein & Peptide Science Neuroglobin and Estrogen Receptors: A New Pathway of Cell Survival and Cell Death Balance
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Selective Modulation of Aβ42 Production in Alzheimers Disease: Non-Steroidal Anti-Inflammatory Drugs and Beyond
Current Pharmaceutical Design Erythropoietin Requires NF-κB and its Nuclear Translocation to Prevent Early and Late Apoptotic Neuronal Injury During β-Amyloid Toxicity
Current Neurovascular Research Neuroprotective Effects of Tetracyclines: Molecular Targets, Animal Models and Human Disease
CNS & Neurological Disorders - Drug Targets Chitosan Formulations as Carriers for Therapeutic Proteins
Current Drug Discovery Technologies A Systematic Review on Donepezil-based Derivatives as Potential Cholinesterase Inhibitors for Alzheimer’s Disease
Current Medicinal Chemistry Contrasting Roles of the Galectin-3 in the Schizophrenia Onset, Clinical Presentation, and Somatic Comorbidity
Current Topics in Medicinal Chemistry Recent Advances in Medicinal Chemistry and Pharmaceutical Technology- Strategies for Drug Delivery to the Brain
Current Topics in Medicinal Chemistry