Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/17329
ชื่อเรื่อง: Novel multifunctional ascorbic triazole derivatives for amyloidogenic pathway inhibition, anti-inflammation, and neuroprotection
ผู้แต่ง: Jiaranaikulwanitch J.
Pandith H.
Tadtong S.
Thammarat P.
Jiranusornkul S.
Chauthong N.
Nilkosol S.
Vajragupta O.
Keywords: amyloid beta protein
amyloid protein
antiinflammatory agent
ascorbic acid
cyclooxygenase 2
inducible nitric oxide synthase
neuroprotective agent
Nos2 protein, mouse
Ptgs2 protein, mouse
SLC23A2 protein, human
sodium ascorbic acid cotransporter
triazole derivative
Alzheimer disease
animal
binding site
blood brain barrier
cell culture
chemical structure
chemistry
computer simulation
drug effect
gene expression
genetics
human
metabolism
molecular docking
mouse
RAW 264.7 cell line
structure activity relation
synthesis
Alzheimer Disease
Amyloid beta-Peptides
Amyloidogenic Proteins
Animals
Anti-Inflammatory Agents
Ascorbic Acid
Binding Sites
Blood-Brain Barrier
Cells, Cultured
Computer Simulation
Cyclooxygenase 2
Gene Expression
Humans
Mice
Molecular Docking Simulation
Molecular Structure
Neuroprotective Agents
Nitric Oxide Synthase Type II
RAW 264.7 Cells
Sodium-Coupled Vitamin C Transporters
Structure-Activity Relationship
Triazoles
วันที่เผยแพร่: 2021
บทคัดย่อ: Alzheimer’s disease (AD) is a common neurodegenerative disorder. The number of patients with AD is projected to reach 152 million by 2050. Donepezil, rivastigmine, galantamine, and memantine are the only four drugs currently approved by the United States Food and Drug Administration for AD treatment. However, these drugs can only alleviate AD symptoms. Thus, this research focuses on the discovery of novel lead compounds that possess multitarget regulation of AD etiopathology relating to amyloid cascade. The ascorbic acid structure has been designated as a core functional domain due to several characteristics, including antioxidant activities, amyloid aggregation inhibition, and the ability to be transported to the brain and neurons. Multifunctional ascorbic derivatives were synthesized by copper (I)-catalyzed azide–alkyne cycloaddition reaction (click chemistry). The in vitro and cell-based assays showed that compounds 2c and 5c exhibited prominent multifunctional activities as beta-secretase 1 inhibitors, amyloid aggregation inhibitors, and antioxidant, neuroprotectant, and anti-inflammatory agents. Significant changes in activities promoting neuroprotection and anti-inflammation were observed at a considerably low concentration at a nanomolar level. Moreover, an in silico study showed that compounds 2c and 5c were capable of being permeated across the blood–brain barrier by sodium-dependent vitamin C transporter-2. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
URI: https://ir.swu.ac.th/jspui/handle/123456789/17329
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85103862243&doi=10.3390%2fmolecules26061562&partnerID=40&md5=578da1c9e03ec2a5f32c0abc0c08662e
ISSN: 14203049
Appears in Collections:Scopus 1983-2021

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