Abstract
Nine quinolone alkaloids (1-9) from the fruits of Evodia rutaecarpa were investigated for their inhibitory activity on nuclear factor of activated T cells (NFAT)-dependent transcription in comparison with nuclear factor (NF)-kappa B-dependent transcription using a reporter gene assay. These alkaloids showed inhibitory effects against NFAT activity, with IC(50) values between 0.91 microM and 15.91 microM. Of the N-methylated quinolones, the longer aliphatic side chain at the quinolone ring showed stronger inhibition of NFAT activity. These N-methylated compounds showed comparable inhibitory effects against NF-kappa B activity. However, quinolone alkaloids without the N-methyl group showed a more selective inhibition of NFAT activity.
MeSH terms
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Alkaloids / chemistry
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Alkaloids / isolation & purification
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Alkaloids / pharmacology*
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Animals
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DNA-Binding Proteins / antagonists & inhibitors*
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DNA-Binding Proteins / metabolism
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Evodia*
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Fruit
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Humans
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / isolation & purification
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Immunosuppressive Agents / pharmacology*
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Jurkat Cells
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Lymphocyte Activation
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Mice
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NFATC Transcription Factors
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Nuclear Proteins / antagonists & inhibitors*
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Nuclear Proteins / metabolism
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology
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Quinolones / chemistry
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Quinolones / isolation & purification
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Quinolones / pharmacology*
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T-Lymphocyte Subsets / metabolism
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Transcription Factors / antagonists & inhibitors*
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Transcription Factors / metabolism
Substances
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Alkaloids
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DNA-Binding Proteins
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Immunosuppressive Agents
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NFATC Transcription Factors
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Nuclear Proteins
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Plant Extracts
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Quinolones
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Transcription Factors