Abstract
Three new acylphloroglucinols (1-3) and four known biosynthetically related analogs (4-7) were isolated from the ethanol extract of a brown alga Sargassum nigrifoloides. Structures for 1-7 were characterized via detailed spectroscopic analyses especially 2D NMR data. Screening of these compounds in Alzheimer's diseases-related bioassays revealed moderate inhibitory activities against two therapeutically important kinases, CDK5 and GSK3β. A preliminary structure-activity relationship was also discussed.
Keywords:
Alzheimer’s diseases; CDK5; GSK3β; acylphloroglucinols.
MeSH terms
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Alzheimer Disease / drug therapy
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Alzheimer Disease / enzymology
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Cyclin-Dependent Kinase 5 / antagonists & inhibitors
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Glycogen Synthase Kinase 3 / antagonists & inhibitors
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Phloroglucinol / analogs & derivatives*
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Phloroglucinol / chemical synthesis*
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Phloroglucinol / pharmacology
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology
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Sargassum / chemistry*
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Spectrometry, Mass, Electrospray Ionization
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Structure-Activity Relationship
Substances
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Protein Kinase Inhibitors
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Phloroglucinol
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Cyclin-Dependent Kinase 5
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CDK5 protein, human
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Glycogen Synthase Kinase 3