Planta Med 2011; 77 - SL44
DOI: 10.1055/s-0031-1282167

Sceletium tortuosum - an ancient treatment for modern CNS-related disorders

A Viljoen 1, E Shikanga 2, S Hamman 1, S Combrink 2, N Gericke 3
  • 1Department of Pharmaceutical Sciences, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa
  • 2Department of Chemistry, Tshwane University of Technology, Private Bag X680, Pretoria, 0001, South Africa
  • 3P.O. Box 937, Sun Valley, 7985, South Africa

Members of the genus Sceletium (Mesembryanthemaceae) have been used for millennia as masticatories, for the relief of thirst and hunger, to combat fatigue, as medicines, and for social and spiritual purposes by San hunter-gatherers (historically referred to as Bushmen) and Khoi pastoralists [1,2]. Recently, several formulations containing Sceletium have been commercialised and marketed to treat anxiety, stress and tension. In 2010 the South African Government granted the country's first ever integrated export and bioprospecting permit to a local pharmaceutical company who will market Sceletium in a joint venture with a neutraceutical company in the USA. Based on the interesting ethnobotanical information and the upsurge in commercial interest we embarked on a comprehensive biosystematic and biopharmaceutical study of S. tortuosum and its major alkaloids, mesembrenone, mesembrenol, mesembrine and mesembranol. Wild S. tortuosum (L.) N.E.Br. plants (n=150), sampled from different localities (n=31) in the south western region of South Africa, were examined for the phytochemical variability using GC-MS. The potential effect of chemotypic variation on product formulation and quality assurance protocols will be discussed. In vitro permeation studies of the alkaloids and different crude plant extracts (water, methanol and enriched alkaloid acid-base extract) across porcine buccal, sublingual and intestinal mucosa were also conducted to predict the bioavailability of the alkaloids. Absorption across intestinal mucosa was highest, but buccal and sublingual absorption contributed to overall bioavailability. In addition to results generated in our laboratory, a general overview on the botany, chemistry and ethnopharmacology of S. tortuosum will be presented.

Keywords: Sceletium tortuosum, alkaloids, bioavailability, quality control

Acknowledgement: National Research Foundation, Tshwane University of Technology, R&R abbatoir (Pretoria).

References: 1. Smith et al (1996)J Ethnopharmacol 50: 119–130

2. Gericke N, Viljoen AM (2008)J Ethnopharmacol 119: 653–663