title: Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production.
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).
authors.affiliation: College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
authors.forename: Tuan-Ahn N
authors.initials: TA
authors.lastname: Pham
authors.forename: Haiyan
authors.initials: H
authors.lastname: Che
authors.forename: Phuong-Thuy T
authors.initials: PT
authors.lastname: Phan
authors.forename: Jae-Won
authors.initials: JW
authors.lastname: Lee
authors.forename: Sung-Soo
authors.initials: SS
authors.lastname: Kim
authors.forename: Haeil
authors.initials: H
authors.lastname: Park
mesh_terms: D000098:Acetophenones / Q000737:chemistry; D000447:Aldehydes / Q000737:chemistry; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002461:Cell Line, Transformed; D044950:Flavanones / Q000494:pharmacology; D005419:Flavonoids / Q000138:chemical synthesis* / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000166:cytology / Q000187:drug effects; D051379:Mice; D017628:Microglia / Q000166:cytology / Q000187:drug effects; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009596:Nitrophenols / Q000737:chemistry
chemical_list: C504842:2-hydroxyl-4,5,6-trimethoxyacetophenone; D000098:Acetophenones; D000447:Aldehydes; D014151:Anti-Anxiety Agents; D044950:Flavanones; D005419:Flavonoids; D008070:Lipopolysaccharides; D009596:Nitrophenols; C024719:4-nitrophenyl; D009569:Nitric Oxide; C080669:5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one; D052247:Nitric Oxide Synthase Type II; C085514:wogonin