title: HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root).
abstract: An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABA(A) receptors with subunit composition, α (1) β (2) γ (2S). HPLC-based activity profiling of the extract led to the identification of 8-lavandulyl flavonoids, kushenol I, sophoraflavanone G, (-)-kurarinone, and kuraridine as GABA(A) receptor modulators. In addition, a series of inactive structurally related flavonoids were characterized. Among these, kushenol Y (4) was identified as a new natural product. The 8-lavandulyl flavonoids are first representatives of a novel scaffold for the target.
authors.affiliation: Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland.
authors.forename: Xinzhou
authors.initials: X
authors.lastname: Yang
authors.forename: Igor
authors.initials: I
authors.lastname: Baburin
authors.forename: Inken
authors.initials: I
authors.lastname: Plitzko
authors.forename: Steffen
authors.initials: S
authors.lastname: Hering
authors.forename: Matthias
authors.initials: M
authors.lastname: Hamburger
mesh_terms: D001681:Biological Assay; D001688:Biological Products / Q000737:chemistry / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000235:genetics / Q000378:metabolism*; D012107:Research Design; D013329:Structure-Activity Relationship
chemical_list: D001688:Biological Products; D004365:Drugs, Chinese Herbal; D011963:Receptors, GABA-A; C494416:kushen