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

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

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1
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, UK. a.l.harvey@strath.ac.uk

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.

PMID:
21798331
DOI:
10.1016/j.jep.2011.07.035
[Indexed for MEDLINE]
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