jaceosidin and 5-7-dihydroxy-6-methoxy-2-phenylchromen-4-one

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).

Topics: Acetophenones; Aldehydes; Animals; Anti-Anxiety Agents; Cell Line, Transformed; Flavanones; Flavonoids; Lipopolysaccharides; Macrophages; Mice; Microglia; Nitric Oxide; Nitric Oxide Synthase Type II; Nitrophenols