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).
Eleganolone, a diterpene from the French marine alga Bifurcaria bifurcata inhibits growth of the human pathogens Trypanosoma brucei and Plasmodium falciparum.
来自法国海洋藻类 Bifurcaria bifurcata 的二萜类化合物 Eleganolone 可抑制人类病原体锥虫(Trypanosoma brucei)和恶性疟原虫(Plasmodium falciparum)的生长
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作者:Gallé Jean-Baptiste, Attioua Barthélémy, Kaiser Marcel, Rusig Anne-Marie, Lobstein Annelise, Vonthron-Sénécheau Catherine
| 期刊: | Marine Drugs | 影响因子: | 5.400 |
| 时间: | 2013 | 起止号: | 2013 Feb 26; 11(3):599-610 |
| doi: | 10.3390/md11030599 | 种属: | Human |
| 研究方向: | 信号转导 | ||
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