HPLC-based activity profiling for GABA(A) receptor modulators: a new dihydroisocoumarin from Haloxylon scoparium

J Nat Prod. 2010 Apr 23;73(4):768-70. doi: 10.1021/np900803w.

Abstract

A new dihydroisocoumarin was isolated from a dichloromethane extract of Haloxylon scoparium with the aid of a functional assay with Xenopus oocytes transiently expressing GABA(A) receptors of defined subunit composition (alpha(1)beta(2)gamma(2S)). Compound 1 induced a maximum potentiation of the chloride currents by 144.6 +/- 35.3% with an EC(50) of 140.2 +/- 51.2 muM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amaranthaceae / chemistry*
  • Animals
  • Chloride Channels / drug effects
  • Chromatography, High Pressure Liquid
  • GABA Modulators / pharmacology
  • Isocoumarins / chemistry
  • Isocoumarins / isolation & purification*
  • Isocoumarins / pharmacology*
  • Molecular Structure
  • Morocco
  • Oocytes / metabolism
  • Plant Roots / chemistry
  • Plants, Medicinal / chemistry*
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-A / metabolism
  • Receptors, GABA-A / physiology
  • Xenopus laevis / metabolism

Substances

  • (S)-4-methoxy-7-phenyl-7,8-dihydro(1,3)dioxolo(4,5-g)isochromen-5-one
  • Chloride Channels
  • GABA Modulators
  • Isocoumarins
  • Receptors, GABA-A