Abstract
In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimers Disease drug candidate.
Keywords: Alzheimer's disease, Antioxidant, Derivative, Metabolism, Scutellarein, Scutellarin, Synthesize, anti-Alzheimer's Disease drug candidate, DPPH, cytotoxicity, PC12, Alzheimer's disease (AD), pathophysiological, neuroprotection, amyloid β protein, peroxynitrate
Letters in Drug Design & Discovery
Title: Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimers Disease Candidates Based on Metabolic Mechanism
Volume: 9 Issue: 1
Author(s): Shu-Lin Song, Nian-Guang Li, Yu-Ping Tang, Zhen-Jiang Wang, Li-Hua Qian, Hao Tang and Jin-Ao Duan
Affiliation:
Keywords: Alzheimer's disease, Antioxidant, Derivative, Metabolism, Scutellarein, Scutellarin, Synthesize, anti-Alzheimer's Disease drug candidate, DPPH, cytotoxicity, PC12, Alzheimer's disease (AD), pathophysiological, neuroprotection, amyloid β protein, peroxynitrate
Abstract: In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimers Disease drug candidate.
Export Options
About this article
Cite this article as:
Song Shu-Lin, Li Nian-Guang, Tang Yu-Ping, Wang Zhen-Jiang, Qian Li-Hua, Tang Hao and Duan Jin-Ao, Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimers Disease Candidates Based on Metabolic Mechanism, Letters in Drug Design & Discovery 2012; 9 (1) . https://dx.doi.org/10.2174/157018012798192946
DOI https://dx.doi.org/10.2174/157018012798192946 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Does Semantic Memory Impairment in Amnestic MCI with Hippocampal Atrophy Conform to a Distinctive Pattern of Progression?
Current Alzheimer Research Nanoparticle-Encapsulated Bryostatin-1 Activates α-Secretase and PKC Isoforms In vitro and Facilitates Acquisition and Retention of Spatial Learning in an Alzheimer's Disease Mouse Model
Current Alzheimer Research Therapeutic Approach for Neuronal Disease by Regulating Reninangiotensin System
Current Hypertension Reviews Nanotechnology Based Delivery Systems of Drugs Currently Used to Treat Alzheimer’s Disease
Nanoscience & Nanotechnology-Asia Social Determinants, Race, and Brain Health Outcomes: Findings from the Chicago Health and Aging Project
Current Alzheimer Research Chitinases: Biomarkers for Human Diseases
Protein & Peptide Letters Memory Enhancing Effect of Black Pepper in the AlCl3 Induced Neurotoxicity Mouse Model is Mediated Through Its Active Component Chavicine
Current Pharmaceutical Biotechnology Intracellular Accumulation of Toxic Turn Amyloid-β is Associated with Endoplasmic Reticulum Stress in Alzheimer’s Disease
Current Alzheimer Research Acetylcholinesterase Inhibitors as Disease-Modifying Therapies for Alzheimers Disease
Current Medicinal Chemistry Cognition-Enhancing Drugs in Mild Cognitive Impairment (MCI) and Alzheimers Disease (AD): An Update [1]
Medicinal Chemistry Reviews - Online (Discontinued) Thermal Taste and Anti-Aspiration Drugs: A Novel Drug Discovery Against Pneumonia
Current Pharmaceutical Design Adenosine in the Central Nervous System: Effects on Neurotransmission and Neuroprotection
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) MAPKs as Mediators of Cell Fate Determination: an Approach to Neurodegenerative Diseases
Current Medicinal Chemistry Patent Selections
Recent Patents on Drug Delivery & Formulation Amyloid Beta Hypothesis in Alzheimer's Disease: Major Culprits and Recent Therapeutic Strategies
Current Drug Targets Histamine H4 Receptor: A Novel Target for Inflammation Therapy
Mini-Reviews in Medicinal Chemistry Lipoprotein-Associated Phospholipase A2: How Effective as a Risk Marker of Cardiovascular Disease and as a Therapeutic Target?
Inflammation & Allergy - Drug Targets (Discontinued) Brain Adaptation to Stressful Stimuli: A New Perspective on Potential Therapeutic Approaches Based on BDNF and NMDA Receptors
CNS & Neurological Disorders - Drug Targets Tactile Angle Discrimination Decreases due to Subjective Cognitive Decline in Alzheimer’s Disease
Current Alzheimer Research MTDL Design Strategy in the Context of Alzheimers Disease: From Lipocrine to Memoquin and Beyond
Current Pharmaceutical Design