title: Eleganolone, a diterpene from the French marine alga Bifurcaria bifurcata inhibits growth of the human pathogens Trypanosoma brucei and Plasmodium falciparum.
abstract: Organic extracts of 20 species of French seaweed have been screened against Trypanosoma brucei rhodesiense trypomastigotes, the parasite responsible for sleeping sickness. These extracts have previously shown potent antiprotozoal activities in vitro against Plasmodium falciparum and Leishmania donovani. The selectivity of the extracts was also evaluated by testing cytotoxicity on a mammalian L6 cell line. The ethyl acetate extract of the brown seaweed, Bifurcaria bifurcata, showed strong trypanocidal activity with a mild selectivity index (IC(50) = 0.53 µg/mL; selectivity index (SI) = 11.6). Bio-guided fractionation led to the isolation of eleganolone, the main diterpenoid isolated from this species. Eleganolone contributes only mildly to the trypanocidal activity of the ethyl acetate extract (IC(50) = 45.0 µM, SI = 4.0). However, a selective activity against P. falciparum erythrocytic stages in vitro has been highlighted (IC(50) = 7.9 µM, SI = 21.6).
authors: UMR 7200 CNRS, Therapeutic Innovation Laboratory, Faculty of Pharmacy, University of Strasbourg, 64701 Illkirch, France. vonthron@unistra.fr
authors: Jean-Baptiste
authors: JB
authors: Gallé
authors: Barthélémy
authors: B
authors: Attioua
authors: Marcel
authors: M
authors: Kaiser
authors: Anne-Marie
authors: AM
authors: Rusig
authors: Annelise
authors: A
authors: Lobstein
authors: Catherine
authors: C
authors: Vonthron-Sénécheau
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D002460:Cell Line; D004224:Diterpenes / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D005602:France; D006801:Humans; D020128:Inhibitory Concentration 50; D000459:Phaeophyceae / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000187:drug effects*; D051381:Rats; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D004224:Diterpenes; D014344:Trypanocidal Agents; C027930:eleganolone