Abstract
Alzheimer's disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer's model. The indication of C7's effect on AD needs further study.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alzheimer Disease / drug therapy*
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Alzheimer Disease / enzymology
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Alzheimer Disease / pathology
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Animals
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Benzophenones / chemistry
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Biphenyl Compounds / metabolism
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Brain / drug effects
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Brain / enzymology
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Brain / pathology
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Chalcone / analogs & derivatives
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Chalcone / chemical synthesis*
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Chalcone / chemistry
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Chalcone / therapeutic use*
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Disease Models, Animal
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Free Radical Scavengers / pharmacology
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Free Radicals / metabolism*
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Glutathione Peroxidase / metabolism
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Hydroxylation / drug effects
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Malondialdehyde / metabolism
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Mice
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Oxidation-Reduction / drug effects
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Picrates / metabolism
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Scopolamine
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Superoxide Dismutase / metabolism
Substances
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Benzophenones
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Biphenyl Compounds
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Free Radical Scavengers
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Free Radicals
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Picrates
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exifone
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Malondialdehyde
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Chalcone
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1,1-diphenyl-2-picrylhydrazyl
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Scopolamine
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Glutathione Peroxidase
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Superoxide Dismutase