Assessment of Dual Life Stage Antiplasmodial Activity of British Seaweeds

被引:18
作者
Spavieri, Jasmine [1 ]
Allmendinger, Andrea [1 ]
Kaiser, Marcel [2 ,3 ]
Itoe, Maurice Ayamba [4 ]
Blunden, Gerald [5 ]
Mota, Maria M. [4 ]
Tasdemir, Deniz [1 ,6 ]
机构
[1] Univ London, Sch Pharm, Dept Pharmaceut & Biol Chem, London WC1N 1AX, England
[2] Swiss Trop & Publ Hlth Inst, Dept Med Parasitol & Infect Biol, CH-4002 Basel, Switzerland
[3] Univ Basel, CH-4003 Basel, Switzerland
[4] Univ Lisbon, Inst Med Mol, P-1649028 Lisbon, Portugal
[5] Univ Portsmouth, Sch Pharm & Biomed Sci, Portsmouth PO1 2DT, Hants, England
[6] Natl Univ Ireland, Sch Chem, Galway, Ireland
来源
MARINE DRUGS | 2013年 / 11卷 / 10期
基金
欧盟地平线“2020”;
关键词
seaweed; marine alga; malaria; Plasmodium; malaria prophylaxis; fatty acid biosynthesis; liver stage; blood stage; PARASITE PLASMODIUM-FALCIPARUM; FATTY-ACID BIOSYNTHESIS; IN-VITRO GROWTH; LIVER-STAGE; MALARIA PARASITES; ANTIPROTOZOAL; ANTIMYCOBACTERIAL; INHIBIT; TRICLOSAN; PROTEINS;
D O I
10.3390/md11104019
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 g/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 g/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.
引用
收藏
页码:4019 / 4034
页数:16
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