Abstract
Bioassay-guided fractionation of the EtOAc-soluble extract of Pueraria lobata based on the inhibition of Aβ-induced toxicity in PC12 cells resulted in the isolation of four known active compounds, genistein (8), biochanin A (9), sissotrin (10), and puerol B (11). Of these, genistein (8) and biochanin A (9) exhibited potent neuroprotective effects with ED(50) values of 33.7 and 27.8 μM, respectively. In addition, a new coumestan, 2-(α,α-dimethylallyl)coumestrol (1) was isolated and characterized, but proved to be inactive, as were additional seven known compounds. The structure of new compound 1 was determined using spectroscopic techniques.
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 / prevention & control
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Amyloid beta-Peptides / metabolism*
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Animals
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Cell Survival / drug effects
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Coumestrol / analogs & derivatives
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Coumestrol / chemistry
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Coumestrol / isolation & purification
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Coumestrol / pharmacology
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Drug Discovery
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Flavonoids / chemistry
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Flavonoids / isolation & purification*
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Flavonoids / pharmacology*
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Genistein / chemistry
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Genistein / isolation & purification
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Genistein / pharmacology
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Medicine, East Asian Traditional
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Molecular Structure
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Neurons / drug effects*
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / isolation & purification*
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Neuroprotective Agents / pharmacology*
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PC12 Cells
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Phenols / chemistry
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Phenols / isolation & purification*
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Phenols / pharmacology*
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Plant Extracts / chemistry
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Plant Extracts / pharmacology
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Plant Roots / chemistry
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Polyphenols
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Pueraria / chemistry*
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Rats
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Spectrometry, Mass, Electrospray Ionization
Substances
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Amyloid beta-Peptides
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Flavonoids
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Neuroprotective Agents
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Phenols
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Plant Extracts
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Polyphenols
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Genistein
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biochanin A
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Coumestrol