ArticleAntimicrobial agents and chemotherapy2004
Antimalarial quinolines and artemisinin inhibit endocytosis in Plasmodium falciparum.
Article in Antimicrobial agents and chemotherapy, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 100 citations in OpenAlex.
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- Endolysosome-targeted nanoparticle delivery of antiviral therapy for coronavirus infections.Life science alliance · 2025Article
- Artemisinin-resistant Plasmodium falciparum Kelch13 mutant proteins display reduced heme-binding affinity and decreased artemisinin activation.Communications biology · 2024Article
- A fast-acting inhibitor of blood-stagebioRxiv : the preprint server for biology · 2024Article
- Real-time measurements of ATP dynamics via ATeams inAntimicrobial agents and chemotherapy · 2024Article
- An In Silico and In Vitro Assessment of the Neurotoxicity of Mefloquine.Biomedicines · 2024Article
- Fluorescent Nanoparticle Uptake by Myzocytosis and Endocytosis inMicroorganisms · 2023Article
- Spirofused Tetrahydroisoquinoline-Oxindole Hybrids (Spiroquindolones) as Potential Multitarget Antimalarial Agents: Preliminary Hit Optimization and Efficacy Evaluation in Mice.Antimicrobial agents and chemotherapy · 2022Article
- Integrated human/SARS-CoV-2 metabolic models present novel treatment strategies against COVID-19.Life science alliance · 2021Article
- Fluorescence Microscopy for ATP Internalization Mediated by Macropinocytosis in Human Tumor Cells and Tumor-xenografted Mice.Journal of visualized experiments : JoVE · 2021Article
- 17-AAG-Induced Activation of the Autophagic Pathway inMicroorganisms · 2021Article
- Spirofused tetrahydroisoquinoline-oxindole hybrids as a novel class of fast acting antimalarial agents with multiple modes of action.Scientific reports · 2020Article
- Chloroquine kills hair cells in zebrafish lateral line and murine cochlear cultures: Implications for ototoxicity.Hearing research · 2020Article
- Cytotoxic and Anti-Plasmodial Activities ofMolecules (Basel, Switzerland) · 2020Article
- Artesunate: could be an alternative drug to chloroquine in COVID-19 treatment?Chinese medicine · 2020Article
- Current and Future Use of Chloroquine and Hydroxychloroquine in Infectious, Immune, Neoplastic, and Neurological Diseases: A Mini-Review.Clinical drug investigation · 2018Review
- Artemisinin Action and Resistance in Plasmodium falciparum.Trends in parasitology · 2016Review
- Current therapies and future possibilities for drug development against liver-stage malaria.The Journal of clinical investigation · 2016Review
- Amino acid efflux by asexual blood-stage Plasmodium falciparum and its utility in interrogating the kinetics of hemoglobin endocytosis and catabolism in vivo.Molecular and biochemical parasitology · 2015Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Endocytosis is a fundamental process of eukaryotic cells and fulfills numerous functions, most notably, that of macromolecular nutrient uptake. Malaria parasites invade red blood cells and during their intracellular development endocytose large amounts of host cytoplasm for digestion in a specialized lysosomal compartment, the food vacuole. In the present study we have examined the effects of artemisinin and the quinoline drugs chloroquine and mefloquine on endocytosis in Plasmodium falciparum. By using novel assays we found that mefloquine and artemisinin inhibit endocytosis of macromolecular tracers by up to 85%, while the latter drug also leads to an accumulation of undigested hemoglobin in the parasite. During 5-h incubations, chloroquine inhibited hemoglobin digestion but had no other significant effect on the endocytic pathway of the parasite, as assessed by electron microscopy, the immunofluorescence localization of hemoglobin, and the distribution of fluorescent and biotinylated dextran tracers. By contrast, when chloroquine was added to late ring stage parasites, followed by a 12-h incubation, macromolecule endocytosis was inhibited by more than 40%. Moreover, there is an accumulation of transport vesicles in the parasite cytosol, possibly due to a disruption in vacuole-vesicle fusion. This fusion block is not observed with mefloquine, artemisinin, quinine, or primaquine but is mimicked by the vacuole alkalinizing agents ammonium chloride and monensin. These results are discussed in the light of present theories regarding the mechanisms of action of the antimalarials and highlight the potential use of drugs in manipulating and studying the endocytic pathway of malaria parasites.
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