UMR 7200 CNRS, Therapeutic Innovation Laboratory, Faculty of Pharmacy, University of Strasbourg, 64701 Illkirch, France.
Mar Drugs. 2013 Feb 26;11(3):599-610. doi: 10.3390/md11030599.
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).
20 种法国海藻的有机提取物已被筛选用于对抗引起昏睡病的寄生虫——罗氏利什曼原虫的无鞭毛体。这些提取物先前在体外对恶性疟原虫和杜氏利什曼原虫显示出很强的抗原生动物活性。通过在哺乳动物 L6 细胞系上测试细胞毒性，还评估了提取物的选择性。褐藻 Bifurcaria bifurcata 的乙酸乙酯提取物具有很强的杀锥虫活性，选择性指数较低（IC50 = 0.53 µg/mL；选择性指数（SI）= 11.6）。生物导向的分级分离导致分离出该物种的主要二萜类化合物 eleganolone。Eleganolone 对乙酸乙酯提取物的杀锥虫活性贡献不大（IC50 = 45.0 µM，SI = 4.0）。然而，体外已经突出显示出对恶性疟原虫红细胞阶段的选择性活性（IC50 = 7.9 µM，SI = 21.6）。
