Abstract
Serum deprivation-induced neuronal-like PC12 cell apoptosis was used as an ischemic/hypoxic model to screen neuroprotective compounds from the rhizomes of Gastrodia elata, a traditional Chinese medicine. Two active compounds, bis(4-hydroxybenzyl)sulfide (1) and N6-(4-hydroxybenzyl)adenine riboside (2), together with 15 known compounds were obtained from the active fraction. Compound 2 was further elucidated by chemical synthesis. Compounds 1 and 2 potently prevented PC12 cell apoptosis in concentration-dependent manners with EC50 values of 7.20 microM and 3.7 x 10-8 M, respectively, and IC50 values of 42.90 microM (Ki 24.10 microM) and 4.660 microM (Ki 2.620 microM), respectively, in an adenosine A2A receptor binding assay.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine / analogs & derivatives*
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Adenosine / chemistry
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Adenosine / isolation & purification
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Adenosine / pharmacology
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Animals
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Apoptosis / drug effects
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Disease Models, Animal
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Drugs, Chinese Herbal / chemistry
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Drugs, Chinese Herbal / isolation & purification
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Drugs, Chinese Herbal / pharmacology*
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Gastrodia / chemistry*
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Molecular Structure
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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 / drug effects
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Plants, Medicinal / chemistry*
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Rats
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Receptor, Adenosine A2A / drug effects
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Serum / metabolism
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Sulfides / chemistry
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Sulfides / isolation & purification
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Sulfides / pharmacology*
Substances
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Drugs, Chinese Herbal
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N6-(4-hydroxybenzyl)adenine riboside
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Neuroprotective Agents
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Receptor, Adenosine A2A
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Sulfides
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bis(4-hydroxybenzyl)sulfide
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Adenosine