Interactions of Magnolia and Ziziphus extracts with selected central nervous system receptors

J Ethnopharmacol. 2009 Jul 30;124(3):421-5. doi: 10.1016/j.jep.2009.05.040. Epub 2009 Jun 6.

Abstract

Ethnopharmacological relevance: Magnolia officinalis Rehder and Wilson [Magnoliaceae] bark and Ziziphus spinosa (Buhge) Hu ex. Chen. [Fam. Rhamnaceae] seed have a history of use in traditional Asian medicine for mild anxiety, nervousness and sleep-related problems.

Aim of the study: To identify pharmacological targets, extracts of Magnolia officinalis (ME), Ziziphus spinosa (ZE), and a proprietary fixed combination (MZE) were tested for affinity with central nervous system receptors associated with relaxation and sleep.

Methods: In vitro radioligand binding and cellular functional assays were conducted on: adenosine A(1), dopamine (transporter, D(1), D(2S), D(3), D(4.4) and D(5)), serotonin (transporter, 5-HT(1A), 5-HT(1B), 5-HT(4e), 5-HT(6) and 5-HT(7)) and the GABA benzodiazepine receptor.

Results: Interactions were demonstrated with the adenosine A(1) receptor, dopamine transporter and dopamine D(5) receptor (antagonist activity), serotonin receptors (5-HT(1B) and 5-HT(6) antagonist activity) and the GABA benzodiazepine receptor at a concentration of 100 microg/ml or lower. ME had an affinity with adenosine A(1) (K(i) of 9.2+/-1.1 microg/ml) and potentiated the GABA activated chloride current at the benzodiazepine subunits of the GABA receptor (maximum effect at 50 microg/ml). ME had a modest antagonist action with 5-HT(6) and ZE with the 5-HT(1B) receptor.

Conclusion: The interactions in the receptor binding models are consistent with the traditional anxiolytic and sleep-inducing activities of Magnolia officinalis bark and Ziziphus spinosa seed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / metabolism
  • Central Nervous System / drug effects*
  • Dopamine / metabolism
  • Dopamine Plasma Membrane Transport Proteins / drug effects
  • Dopamine Plasma Membrane Transport Proteins / metabolism
  • Drug Combinations
  • Humans
  • Hypnotics and Sedatives / chemistry*
  • Hypnotics and Sedatives / pharmacology*
  • Magnolia / chemistry*
  • Medicine, East Asian Traditional
  • Muscle Relaxants, Central / pharmacology
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Radioligand Assay
  • Receptor, Adenosine A1 / drug effects
  • Receptors, Dopamine / drug effects
  • Receptors, GABA-A / drug effects
  • Receptors, Neurotransmitter / drug effects*
  • Receptors, Serotonin / drug effects
  • Serotonin / metabolism
  • Serotonin Plasma Membrane Transport Proteins / drug effects
  • Serotonin Plasma Membrane Transport Proteins / metabolism
  • Sleep / drug effects
  • Ziziphus / chemistry*
  • gamma-Aminobutyric Acid / metabolism

Substances

  • Dopamine Plasma Membrane Transport Proteins
  • Drug Combinations
  • Hypnotics and Sedatives
  • Muscle Relaxants, Central
  • Plant Extracts
  • Receptor, Adenosine A1
  • Receptors, Dopamine
  • Receptors, GABA-A
  • Receptors, Neurotransmitter
  • Receptors, Serotonin
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin
  • gamma-Aminobutyric Acid
  • Adenosine
  • Dopamine