Pharmacognosie et Molécules Naturelles Bio-actives, Laboratoire d'Innovation Thérapeutique UMR CNRS 7200, Faculté de Pharmacie, Université de Strasbourg, 74 route du Rhin, 67401 Illkirch cedex, France.
Physiologie et Ecophysiologie des Mollusques Marins, UMR M IFREMER 100, Institut de Biologie Fondamentale et Appliquée (IBFA), Université de Caen Basse-Normandie, 14032 Caen cedex, France.
Mar Drugs. 2011;9(6):922-933. doi: 10.3390/md9060922. Epub 2011 May 25.
Marine macrophytes contain a variety of biologically active compounds, some reported to have antiprotozoal activity in vitro. As a part of a screening program to search for new natural antiprotozoals, we screened hydroalcoholic and ethyl acetate extracts of 20 species of seaweeds from three phyla (Rhodophyta, Heterokontophyta and Chlorophyta), sampled along the Normandy (France) coast. We tested them in vitro against the protozoa responsible for three major endemic parasitic diseases: Plasmodium falciparum, Leishmania donovani and Trypanosoma cruzi. The selectivity of the extracts was also evaluated by testing on a mammalian cell line (L6 cells). Ethyl acetate extracts were more active than hydroalcoholic ones. Activity against T. cruzi and L. donovani was non-existent to average, but almost half the extracts showed good activity against P. falciparum. The ethyl acetate extract of Mastocarpus stellatus showed the best antiplasmodial activity as well as the best selectivity index (IC(50) = 2.8 μg/mL; SI > 30). Interestingly, a red algae species, which shares phylogenetic origins with P. falciparum, showed the best antiplasmodial activity. This study is the first to report comparative antiprotozoal activity of French marine algae. Some of the species studied here have not previously been biologically evaluated.
海洋大型藻类含有多种具有生物活性的化合物,其中一些已被报道具有体外抗原生动物活性。作为寻找新型天然抗原生动物药物筛选计划的一部分,我们对来自三个门(红藻门、异鞭毛门和绿藻门)的 20 种海藻的水醇提取物和乙酸乙酯提取物进行了筛选,这些海藻均采自诺曼底(法国)海岸。我们在体外测试了它们对引起三种主要地方性寄生虫病的原生动物的活性:疟原虫、利什曼原虫和克氏锥虫。提取物的选择性也通过在哺乳动物细胞系(L6 细胞)上进行测试进行了评估。乙酸乙酯提取物比水醇提取物更具活性。对 T. cruzi 和 L. donovani 的活性平均为非活性,但近一半的提取物对 P. falciparum 表现出良好的活性。Mastocarpus stellatus 的乙酸乙酯提取物表现出最好的抗疟原虫活性和最好的选择性指数(IC50 = 2.8 μg/mL;SI > 30)。有趣的是,一种与疟原虫具有共同进化起源的红藻表现出最好的抗疟原虫活性。本研究首次报道了法国海洋藻类的比较抗原生动物活性。本研究中研究的一些物种以前没有进行过生物学评价。