Abstract
A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2'-hydroxy-4,5,6-trimethoxyacetophenone and aldehydes in 3 steps. Among the tested compounds, several analogs (3b, 3c, 3d, 3f) exhibited strong inhibitory activities. Especially, the analog with 4-nitrophenyl group (3b) showed stronger inhibitory activity (IC(50)=4.73 μM) than that of wogonin (IC(50)=7.80 μM).
Copyright © 2012. Published by Elsevier Ltd.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetophenones / chemistry
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Aldehydes / chemistry
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Animals
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Anti-Anxiety Agents / chemical synthesis*
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Anti-Anxiety Agents / pharmacology
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Cell Line, Transformed
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Flavanones / pharmacology
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Flavonoids / chemical synthesis*
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Flavonoids / pharmacology
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Lipopolysaccharides / pharmacology
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Macrophages / cytology
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Macrophages / drug effects
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Mice
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Microglia / cytology
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Microglia / drug effects
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Nitric Oxide / antagonists & inhibitors*
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Nitric Oxide / biosynthesis
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Nitric Oxide Synthase Type II / antagonists & inhibitors*
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Nitric Oxide Synthase Type II / metabolism
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Nitrophenols / chemistry
Substances
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2-hydroxyl-4,5,6-trimethoxyacetophenone
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Acetophenones
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Aldehydes
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Anti-Anxiety Agents
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Flavanones
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Flavonoids
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Lipopolysaccharides
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Nitrophenols
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4-nitrophenyl
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Nitric Oxide
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5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one
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Nitric Oxide Synthase Type II
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wogonin