Department of Pharmaceutical and Biological Chemistry, School of Pharmacy, University of London, London WC1N 1AX, UK.
Mar Drugs. 2013 Oct 22;11(10):4019-34. doi: 10.3390/md11104019.
Terrestrial plants have proven to be a prolific producer of clinically effective antimalarial drugs, but the antimalarial potential of seaweeds has been little explored. The main aim of this study was to assess the in vitro chemotherapeutical and prophylactic potential of the extracts of twenty-three seaweeds collected from the south coast of England against blood stage (BS) and liver stage (LS) Plasmodium parasites. The majority (14) of the extracts were active against BS of P. falciparum, with brown seaweeds Cystoseira tamariscifolia, C. baccata and the green seaweed Ulva lactuca being the most active (IC(50)s around 3 μg/mL). The extracts generally had high selectivity indices (>10). Eight seaweed extracts inhibited the growth of LS parasites of P. berghei without any obvious effect on the viability of the human hepatoma (Huh7) cells, and the highest potential was exerted by U. lactuca and red seaweeds Ceramium virgatum and Halopitys incurvus (IC50 values 14.9 to 28.8 μg/mL). The LS-active extracts inhibited one or more key enzymes of the malarial type-II fatty acid biosynthesis (FAS-II) pathway, a drug target specific for LS. Except for the red seaweed Halopitys incurvus, all LS-active extracts showed dual activity versus both malarial intracellular stage parasites. This is the first report of LS antiplasmodial activity and dual stage inhibitory potential of seaweeds.
陆生植物已被证明是具有临床疗效的抗疟药物的丰富生产者,但海藻的抗疟潜力尚未得到充分探索。本研究的主要目的是评估从英格兰南部海岸采集的 23 种海藻的提取物对血期(BS)和肝期(LS)疟原虫寄生虫的体外化学治疗和预防潜力。大多数(14)提取物对 BS 的 P. falciparum 具有活性,棕色海藻 Cystoseira tamariscifolia、C. baccata 和绿海藻 Ulva lactuca 最为活跃(IC(50)约为 3 μg/mL)。提取物通常具有较高的选择性指数(>10)。八种海藻提取物抑制 LS 的 P. berghei 寄生虫的生长,而对人肝癌(Huh7)细胞的活力没有明显影响,U. lactuca 和红海藻 Ceramium virgatum 和 Halopitys incurvus 的潜力最高(IC(50)值为 14.9 至 28.8 μg/mL)。LS 活性提取物抑制疟原虫 II 型脂肪酸生物合成(FAS-II)途径的一种或多种关键酶,这是 LS 的特定药物靶标。除了红海藻 Halopitys incurvus 之外,所有 LS 活性提取物对两种疟原虫内寄生虫均具有双重活性。这是首次报道海藻的 LS 抗疟活性和双重阶段抑制潜力。