1. Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production.
- Author
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Pham TA, Che H, Phan PT, Lee JW, Kim SS, and Park H
- Subjects
- Acetophenones chemistry, Aldehydes chemistry, Animals, Anti-Anxiety Agents pharmacology, Cell Line, Transformed, Flavanones pharmacology, Flavonoids pharmacology, Lipopolysaccharides pharmacology, Macrophages cytology, Macrophages drug effects, Mice, Microglia cytology, Microglia drug effects, Nitric Oxide biosynthesis, Nitric Oxide Synthase Type II metabolism, Nitrophenols chemistry, Anti-Anxiety Agents chemical synthesis, Flavonoids chemical synthesis, Nitric Oxide antagonists & inhibitors, Nitric Oxide Synthase Type II antagonists & inhibitors
- 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.)
- Published
- 2012
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