The Traditional Medicine Spilanthes acmella, and the Alkylamides Spilanthol and Undeca-2E-ene-8,10-diynoic Acid Isobutylamide, Demonstrate In Vitro and In Vivo Antimalarial Activity

Kevin Spelman (1) , Delphine Depoix (2) , Megan Mccray (3) , Elisabeth Mouray (2) , Philippe Grellier (2)

1 NIH - National Institutes of Health [Bethesda]
2 MCAM - Molécules de Communication et Adaptation des Micro-organismes
3 UNCG - University of North Carolina [Greensboro]

Spilanthes spp. are used as traditional herbal medicines in Africa and India to treat malaria. Yet, to date, there is no data on active constituents or most effective extraction methods for this indication. The isolated alkylamides, spilanthol and undeca-2E-ene-8,10-diynoic acid isobutylamide, found in S. acmella Murr., were shown to have IC50s of 16.5 μg/mL and 41.4 μg/ mL on Plasmodium falciparum strain PFB and IC50s of 5.8 μg/mL and 16.3 μg/mL for the chloroquine resistant P. falciparum K1 strain, respectively. Further investigations revealed that at relatively low concentrations, spilanthol and the water extract of S. acmella reduced the parasitemia 59% and 53% in mice infected with P. yoelii yoelii 17XNL at 5 mg/kg and 50 mg/kg, respectively. Unexpectedly, the 95% ethanol extract of S. acmella was less effective (36% reduction in parasitemia) at 50 mg/kg. These results provide the first evidence supporting S. acmella against malaria and demonstrating active constituents in S. acmella against P. falciparum.

Keywords: Plasmodium falciparum; alkylamides; deca-2E 6Z 8E-trienoic acid isobutylamide; malaria; traditional medicine; phytotherapy

Domains: Chemical Sciences; Microbiology and Parasitology

Kevin Spelman, Delphine Depoix, Megan Mccray, Elisabeth Mouray, Philippe Grellier. The Traditional Medicine Spilanthes acmella, and the Alkylamides Spilanthol and Undeca-2E-ene-8,10-diynoic Acid Isobutylamide, Demonstrate In Vitro and In Vivo Antimalarial Activity. Phytotherapy Research, 2011, 25 (7), pp.1098-1101. ⟨10.1002/ptr.3395⟩. ⟨mnhn-02070067⟩