Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids

J Ethnopharmacol. 2011 Oct 11;137(3):1124-9. doi: 10.1016/j.jep.2011.07.035. Epub 2011 Jul 20.

Abstract

Ethnopharmacological relevance: The South African plant Sceletium tortuosum has been known for centuries for a variety of traditional uses, and, more recently, as a possible source of anti-anxiety or anti-depressant effects. A standardised extract Zembrin(®) was used to test for pharmacological activities that might be relevant to the ethnopharmacological uses, and three of the main alkaloids were also tested.

Materials and methods: A standardised ethanolic extract was prepared from dried plant material, along with the purified alkaloids mesembrine, mesembrenone and mesembrenol. These were tested on a panel of receptors, enzymes and other drug targets, and for cytotoxic effects on mammalian cells.

Results: The extract was a potent blocker in 5-HT transporter binding assays (IC(50) 4.3 μg/ml) and had powerful inhibitory effects on phosphodiesterase 4 (PDE4) (IC(50) 8.5 μg/ml), but not other phosphodiesterases. There were no cytotoxic effects. Mesembrine was the most active alkaloid against the 5-HT transporter (K(i) 1.4 nM), while mesembrenone was active against the 5-HT transporter and PDE4 (IC(50)'s<1 μM).

Conclusions: The activity of the Sceletium tortuosum extract on the 5-HT transporter and PDE4 may explain the clinical effects of preparations made from this plant. The activities relate to the presence of alkaloids, particularly mesembrine and mesembrenone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aizoaceae* / chemistry
  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Functional Food*
  • Hep G2 Cells
  • Humans
  • Indole Alkaloids / pharmacology
  • Ion Channels / drug effects
  • Ion Channels / metabolism
  • Ligands
  • Medicine, African Traditional*
  • Phosphodiesterase 4 Inhibitors / isolation & purification
  • Phosphodiesterase 4 Inhibitors / pharmacology*
  • Plant Components, Aerial
  • Plants, Medicinal
  • Radioligand Assay
  • Serotonin Plasma Membrane Transport Proteins / drug effects
  • Serotonin Plasma Membrane Transport Proteins / metabolism
  • Serotonin Uptake Inhibitors / isolation & purification
  • Serotonin Uptake Inhibitors / pharmacology*
  • South Africa
  • U937 Cells

Substances

  • Alkaloids
  • Indole Alkaloids
  • Ion Channels
  • Ligands
  • Phosphodiesterase 4 Inhibitors
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • mesembrine