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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.JE

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.

Authors+Show Affiliations

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, UK. a.l.harvey@strath.ac.ukNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21798331

Citation

Harvey, Alan L., et al. "Pharmacological Actions of the South African Medicinal and Functional Food Plant Sceletium Tortuosum and Its Principal Alkaloids." Journal of Ethnopharmacology, vol. 137, no. 3, 2011, pp. 1124-9.
Harvey AL, Young LC, Viljoen AM, et al. Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids. J Ethnopharmacol. 2011;137(3):1124-9.
Harvey, A. L., Young, L. C., Viljoen, A. M., & Gericke, N. P. (2011). Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids. Journal of Ethnopharmacology, 137(3), 1124-9. https://doi.org/10.1016/j.jep.2011.07.035
Harvey AL, et al. 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. PubMed PMID: 21798331.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids. AU - Harvey,Alan L, AU - Young,Louise C, AU - Viljoen,Alvaro M, AU - Gericke,Nigel P, Y1 - 2011/07/20/ PY - 2011/03/01/received PY - 2011/06/14/revised PY - 2011/07/11/accepted PY - 2011/7/30/entrez PY - 2011/7/30/pubmed PY - 2012/2/15/medline SP - 1124 EP - 9 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 137 IS - 3 N2 - 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. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/21798331/Pharmacological_actions_of_the_South_African_medicinal_and_functional_food_plant_Sceletium_tortuosum_and_its_principal_alkaloids_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(11)00511-3 DB - PRIME DP - Unbound Medicine ER -