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Assessment of Dual Life Stage Antiplasmodial Activity of British Seaweeds
Department of Pharmaceutical and Biological Chemistry, School of Pharmacy, University of London, London WC1N 1AX, UK
Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel CH-4002, Switzerland
University of Basel, Petersplatz 1, Basel CH-4003, Switzerland
Instituto de Medicina Molecular, Universidade de Lisboa, Lisbon 1649-028, Portugal
School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth PO1 2DT, UK
School of Chemistry, National University of Ireland, Galway, Ireland
These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 13 August 2013; in revised form: 8 October 2013 / Accepted: 11 October 2013 / Published: 22 October 2013
Abstract: 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 (IC50s 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.
Keywords: seaweed; marine alga; malaria; Plasmodium; malaria prophylaxis; fatty acid biosynthesis; liver stage; blood stage
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Spavieri, J.; Allmendinger, A.; Kaiser, M.; Itoe, M.A.; Blunden, G.; Mota, M.M.; Tasdemir, D. Assessment of Dual Life Stage Antiplasmodial Activity of British Seaweeds. Mar. Drugs 2013, 11, 4019-4034.
Spavieri J, Allmendinger A, Kaiser M, Itoe MA, Blunden G, Mota MM, Tasdemir D. Assessment of Dual Life Stage Antiplasmodial Activity of British Seaweeds. Marine Drugs. 2013; 11(10):4019-4034.
Spavieri, Jasmine; Allmendinger, Andrea; Kaiser, Marcel; Itoe, Maurice A.; Blunden, Gerald; Mota, Maria M.; Tasdemir, Deniz. 2013. "Assessment of Dual Life Stage Antiplasmodial Activity of British Seaweeds." Mar. Drugs 11, no. 10: 4019-4034.