Abstract
Aquilaria subintegra, locally known as “Gaharu”, belongs to the Thymelaeceae family. This plant’s leaves have been claimed to be effective for the treatment of Alzheimer's disease (AD) by Malay traditional practitioner in Malaysia. In this research, the chloroform extracts of the leaves and stem of A. subintegra were tested for acetylcholinesterase (AChE) inhibitory activity. The Thin Layer Chromatography (TLC) results indicated the presence of phenols, flavonoids, terpenoids, and alkaloids compounds in the extracts. Analysis of the stem chloroform extracts with LCMS/MS displayed that it contains kaempferol 3,4,7-trimethyl ether. The AChE inhibitory activity of leaves and stem chloroform extracts and kaempferol were 80%, 93% and 85.8%, respectively. The Brine Shrimp Lethality Assay (BSLA) exhibited low to moderate toxicity of the chloroform extract from leaves (LC50=531.18 ± 49.53 μg/ml), the stem chloroform extract (LC50=407.34 ± 68.05 μg/ml) and kaempferol (LC50=762.41 ± 45.09 μg/ml). The extracts and kaempferol were not cytotoxic to human umbilical vein endothelial cells (HUVEC), human normal gastric epithelial cell line (GES-1) and human normal hepatic cell line (WRL-68). The effect of leaf and stem chloroform extracts and kaempferol were determined in the Radial Arm Maze (RAM) after administration by oral gavage to ICR male and female mice with valium-impaired memory. Administration of kaempferol to the mice significantly reduced the number of repeated entries into the arms of maze in males and females. In conclusion, the inhibition of AChE by leaf and stem chloroform extracts of A. subintegra could be due to the presence of kaempferol. This extract is safe for use as a natural AChE inhibitor as an alternative to berberine for the treatment of AD.
Keywords: Acetylcholinesterase, Alzheimer's disease, Aquilaria subintegra, kaempferol.
Current Alzheimer Research
Title:Isolation and Characterisation of Acetylcholinesterase Inhibitors from Aquilaria subintegra for the Treatment of Alzheimer’s Disease (AD)
Volume: 11 Issue: 2
Author(s): Hirbod Bahrani, Jamaludin Mohamad, Mohammadjavad Paydar and Hussin A. Rothan
Affiliation:
Keywords: Acetylcholinesterase, Alzheimer's disease, Aquilaria subintegra, kaempferol.
Abstract: Aquilaria subintegra, locally known as “Gaharu”, belongs to the Thymelaeceae family. This plant’s leaves have been claimed to be effective for the treatment of Alzheimer's disease (AD) by Malay traditional practitioner in Malaysia. In this research, the chloroform extracts of the leaves and stem of A. subintegra were tested for acetylcholinesterase (AChE) inhibitory activity. The Thin Layer Chromatography (TLC) results indicated the presence of phenols, flavonoids, terpenoids, and alkaloids compounds in the extracts. Analysis of the stem chloroform extracts with LCMS/MS displayed that it contains kaempferol 3,4,7-trimethyl ether. The AChE inhibitory activity of leaves and stem chloroform extracts and kaempferol were 80%, 93% and 85.8%, respectively. The Brine Shrimp Lethality Assay (BSLA) exhibited low to moderate toxicity of the chloroform extract from leaves (LC50=531.18 ± 49.53 μg/ml), the stem chloroform extract (LC50=407.34 ± 68.05 μg/ml) and kaempferol (LC50=762.41 ± 45.09 μg/ml). The extracts and kaempferol were not cytotoxic to human umbilical vein endothelial cells (HUVEC), human normal gastric epithelial cell line (GES-1) and human normal hepatic cell line (WRL-68). The effect of leaf and stem chloroform extracts and kaempferol were determined in the Radial Arm Maze (RAM) after administration by oral gavage to ICR male and female mice with valium-impaired memory. Administration of kaempferol to the mice significantly reduced the number of repeated entries into the arms of maze in males and females. In conclusion, the inhibition of AChE by leaf and stem chloroform extracts of A. subintegra could be due to the presence of kaempferol. This extract is safe for use as a natural AChE inhibitor as an alternative to berberine for the treatment of AD.
Export Options
About this article
Cite this article as:
Bahrani Hirbod, Mohamad Jamaludin, Paydar Mohammadjavad and Rothan A. Hussin, Isolation and Characterisation of Acetylcholinesterase Inhibitors from Aquilaria subintegra for the Treatment of Alzheimer’s Disease (AD), Current Alzheimer Research 2014; 11 (2) . https://dx.doi.org/10.2174/1567205011666140130151344
DOI https://dx.doi.org/10.2174/1567205011666140130151344 |
Print ISSN 1567-2050 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5828 |
Call for Papers in Thematic Issues
New Advances in the Prevention, Diagnosis, Treatment, and Rehabilitation of Alzheimer's Disease
Aims and Scope: Introduction: Alzheimer's disease (AD) poses a significant global health challenge, with an increasing prevalence that demands concerted efforts to advance our understanding and strategies for prevention, diagnosis, treatment, and rehabilitation. This thematic issue aims to bring together cutting-edge research and innovative approaches from multidisciplinary perspectives to address ...read more
Current updates on the Role of Neuroinflammation in Neurodegenerative Disorders
Neuroinflammation is an invariable hallmark of chronic and acute neurodegenerative disorders and has long been considered a potential drug target for Alzheimer?s disease (AD) and dementia. Significant evidence of inflammatory processes as a feature of AD is provided by the presence of inflammatory markers in plasma, CSF and postmortem brain ...read more
Deep Learning for Advancing Alzheimer's Disease Research
Alzheimer's disease (AD) poses a significant global health challenge, with an increasing number of individuals affected yearly. Deep learning, a subfield of artificial intelligence, has shown immense potential in various domains, including healthcare. This thematic issue of Current Alzheimer Research explores the application of deep learning techniques in advancing our ...read more
Diagnostic and therapeutic biomarkers of dementia
Dementia affects 18 million people worldwide. Dementia is a syndrome of symptoms caused by brain disease, usually chronic or progressive, clinically characterized by multiple impairments of higher cortical functions such as memory, thinking, orientation, and learning. In addition, in the course of dementia, cognitive deficits are observed, which often hinder ...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
-
Formaldehyde as a trigger for protein aggregation and potential target for mitigation of age-related, progressive cognitive impairment
Current Topics in Medicinal Chemistry Recent Trends in the Management of Alzheimer’s Disease: Current Therapeutic Options and Drug Repurposing Approaches
Current Neuropharmacology Cardiotoxicity of Molecularly Targeted Agents
Current Cardiology Reviews Cellular Mechanisms of the Protective Effect of Polyphenols on the Neurovascular Unit in Strokes
Cardiovascular & Hematological Agents in Medicinal Chemistry Editorial: Pain in Dementia: A Distressing Combination of Several Factors
Current Alzheimer Research Conference Report: 12<sup>th</sup> International Congress on Neuroprotective Agents (ICNA), Charlottesville, VA, USA September 28, 2014-Ocobert 01, 2014
CNS & Neurological Disorders - Drug Targets Current View from Alzheimer Disease to Type 2 Diabetes Mellitus
CNS & Neurological Disorders - Drug Targets Modulation of Monoaminergic Transporters by Choline-Containing Phospholipids in Rat Brain
CNS & Neurological Disorders - Drug Targets Pharmacological Inhibition of Protein Tyrosine Phosphatase 1B: A Promising Strategy for the Treatment of Obesity and Type 2 Diabetes Mellitus
Current Medicinal Chemistry Omega-3 Fatty Acids in the Management of Epilepsy
Current Topics in Medicinal Chemistry Subject Index to Volume 11
Protein & Peptide Letters Recent Multi-target Approaches on the Development of Anti- Alzheimer's Agents Integrating Metal Chelation Activity
Current Medicinal Chemistry Platelet Alpha- and Beta- Secretase Activities are not Significantly Affected by Dementia or Mild Cognitive Impairment in Swedish Patients
Current Alzheimer Research Vitamin D and Stroke: Promise for Prevention and Better Outcome
Current Vascular Pharmacology Drug Development of Small-Molecule Inhibitors of AD-Relevant Kinases as Novel Perspective Multitargeted Approach
Current Alzheimer Research Nitric Oxide-Derived Oxidants with a Focus on Peroxynitrite: Molecular Targets,Cellular Responses and Therapeutic Implications
Current Pharmaceutical Design The Immunoproteasome: An Emerging Therapeutic Target
Current Topics in Medicinal Chemistry Aligning Animal Models of Clinical Germinal Matrix Hemorrhage, From Basic Correlation to Therapeutic Approach
Current Drug Targets Inhibitors of the 5-Lipoxygenase Pathway in Atherosclerosis
Current Pharmaceutical Design Need for Nutritious Convenience Foods for the Elderly Population: A Review
Current Nutrition & Food Science