Abstract
BackgroundIron is an essential micronutrient required by all living organisms including malaria parasites (Plasmodium spp.) for many biochemical reactions, especially growth and multiplication processes. Therefore, malaria parasite needs to take up the iron from outside or/and inside the parasitized red blood cells (PRBC). Iron chelators are widely used for the treatment of thalassaemia-related iron overload and also inhibit parasite growth at levels that are non-toxic to mammalian cells.MethodsInhibitory effect of 1-(N-acetyl-6-aminohexyl)-3-hydroxy-2-methylpyridin-4-one (CM1) and green tea extract (GTE) on the growth of malaria parasite Plasmodium falciparum was compared with standard chelators including desferrioxamine (DFO), deferiprone (DFP) and deferasirox (DFX). A flow cytometric technique was used to enumerate PRBC stained with SYBR Green I fluorescent dye. The labile iron pool (LIP) was assayed using the calcein-acetoxymethyl fluorescent method.ResultsThe IC50 values of DFO, GTE, CM1, DFX and DFP against P. falciparum were 14.09, 21.11, 35.14, 44.71 and 58.25 µM, respectively. Importantly, CM1 was more effective in reducing LIP levels in the P. falciparum culture than DFP (p < 0.05).ConclusionsCM1 and GTE exhibit anti-malarial activity. They could interfere with uptake of exogenous iron or deplete the intracellular labile iron pool in malaria parasites, leading to inhibition of their growth.
Highlights
Iron is an essential micronutrient required by all living organisms including malaria parasites (Plasmodium spp.) for many biochemical reactions, especially growth and multiplication processes
Artemisinin found in the Chinese medicinal plant (Artemisia annua) binds iron to form ferric-dihydroartemisinin complex, resulting in reactive oxygen species (ROS)-mediated potent antimalarial activity against ring and late stage of CQ-resistant P. falciparum malaria parasites [5]
The PYR-Green tea extract (GTE) synergy seemed to be greater than the PYR-compounds 1‐(N‐Acetyl‐6‐aminohexyl)‐3‐hydroxy‐2‐methylpyridin‐4‐one (CM1)
Summary
Iron is an essential micronutrient required by all living organisms including malaria parasites (Plasmodium spp.) for many biochemical reactions, especially growth and multiplication processes. Plasmodial malaria parasites essentially obtain iron from their hosts for their growth and development, while. Widespread multiple drug resistance in human malaria has intensified the search for new antimalarial compounds, iron chelators. The chelators exert their effects by sequestering iron from multiple sources, including transferrin as well as intracellular and extracellular iron [4]. Artemisinin found in the Chinese medicinal plant (Artemisia annua) binds iron to form ferric-dihydroartemisinin complex, resulting in reactive oxygen species (ROS)-mediated potent antimalarial activity against ring and late stage of CQ-resistant P. falciparum malaria parasites [5]
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