Abstract
EtOAc extracts from two batches of Morus alba root bark (Sang bai pi) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes, which transiently expressed GABA (A) receptors of the subunit composition α₁β₂γ(2S). With the aid of HPLC-based activity profiling of the extract from the first batch, activity was traced to a peak subsequently identified as sanggenon G (3). The second batch had a different phytochemical profile, and HPLC-based activity profiling led to the identification of sanggenon C (4) and a stereoisomer of sanggenon D (2) as positive GABA (A) receptor modulators. The structurally related compound kuwanon L (1) was inactive. The sanggenons represent a new scaffold of positive GABA (A) receptor modulators.
© Georg Thieme Verlag KG Stuttgart · New York.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Benzofurans / chemistry
-
Benzofurans / isolation & purification
-
Benzofurans / pharmacology*
-
Chromatography, High Pressure Liquid
-
Chromones / chemistry
-
Chromones / isolation & purification
-
Chromones / pharmacology*
-
Dose-Response Relationship, Drug
-
Drugs, Chinese Herbal / chemistry
-
Drugs, Chinese Herbal / isolation & purification
-
Drugs, Chinese Herbal / pharmacology*
-
GABA Modulators / chemistry
-
GABA Modulators / isolation & purification
-
GABA Modulators / pharmacology*
-
Medicine, Chinese Traditional
-
Molecular Structure
-
Morus / chemistry*
-
Oocytes
-
Plant Bark / chemistry
-
Plant Roots / chemistry
-
Plants, Medicinal / chemistry
-
Receptors, GABA-A / drug effects*
-
Receptors, GABA-A / metabolism
-
Xenopus laevis
-
gamma-Aminobutyric Acid / pharmacology
Substances
-
Benzofurans
-
Chromones
-
Drugs, Chinese Herbal
-
GABA Modulators
-
Receptors, GABA-A
-
sanggenon G
-
gamma-Aminobutyric Acid
-
sanggenone C