title: Convulsion-related activities of Scutellaria flavones are related to the 5,7-dihydroxyl structures.
abstract: We screened the major bioactive flavones isolated from Scutellaria baicalensis (baicalin, baicalein and oroxylin A) for their convulsion related activities. In electrogenic response score system and the pentylenetetrazole seizure model, baicalein but not oroxylin A and baicalin exhibited anticonvulsant effects. In vitro studies also revealed that baicalein induced intracellular Cl(-) influx, whereas oroxylin A blocked muscimol- and baicalein-induced intracellular Cl(-) influx. The anticonvulsant effect of baicalein was inhibited by flumazenil, a benzodiazepine(BZD) receptor antagonist. Therefore, anticonvulsive effect of baicalein was mediated by the BZD binding site of GABA(A) receptor. The 5, 7-dihydroxyl group is present in the structure of the three flavones. It is postulated that this group played a key role in inducing convulsion-related activities.
authors: Department of Pharmacology, College of Pharmacy, Seoul National University, Seoul 139-742, Republic of Korea.
authors: Seo Young
authors: SY
authors: Yoon
authors: Ike Campomayor
authors: IC
authors: dela Peña
authors: Chan Young
authors: CY
authors: Shin
authors: Kun Ho
authors: KH
authors: Son
authors: Yong Soo
authors: YS
authors: Lee
authors: Jong Hoon
authors: JH
authors: Ryu
authors: Jae Hoon
authors: JH
authors: Cheong
authors: Kwang Ho
authors: KH
authors: Ko
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D002712:Chlorides / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D004597:Electroshock; D047309:Flavones / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D006878:Hydroxides / Q000737:chemistry*; D042541:Intracellular Space / Q000187:drug effects / Q000378:metabolism; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D031364:Scutellaria baicalensis / Q000737:chemistry*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology / Q000503:physiopathology; D013329:Structure-Activity Relationship; D013331:Strychnine / Q000494:pharmacology
chemical_list: D000927:Anticonvulsants; D002712:Chlorides; D047309:Flavones; D006878:Hydroxides; C031356:hydroxide ion; D013331:Strychnine; D010433:Pentylenetetrazole