ArticleAntimicrobial agents and chemotherapy2013
Cytostatic versus cytocidal activities of chloroquine analogues and inhibition of hemozoin crystal growth.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 52 citations in OpenAlex.
- Antiplasmodial peptaibols act through membrane directed mechanisms.Cell chemical biology · 2024Article
- Biological evaluation of novel side chain containing CQTrICh-analogs as antimalarials and their development asHeliyon · 2024Article
- Target-Based Virtual Screening of Natural Compounds Identifies a Potent Antimalarial With Selective Falcipain-2 Inhibitory Activity.Frontiers in pharmacology · 2022Article
- Artemisinin-Based Drugs Target the Plasmodium falciparum Heme Detoxification Pathway.Antimicrobial agents and chemotherapy · 2021Article
- Repurposing Chloroquine Against Multiple Diseases With Special Attention to SARS-CoV-2 and Associated Toxicity.Frontiers in pharmacology · 2021Review
- Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.Journal of medicinal chemistry · 2020Article
- Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, AgainstMolecular & cellular proteomics : MCP · 2020Article
- Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development ofRSC advances · 2019Article
- Highly Sensitive and Rapid Characterization of the Development of Synchronized Blood Stage Malaria Parasites Via Magneto-Optical Hemozoin Quantification.Biomolecules · 2019Article
- Artesunate Activation by Heme in an Aqueous Medium.Inorganica chimica acta · 2019Article
- High-Content Screening of the Medicines for Malaria Venture Pathogen Box for Plasmodium falciparum Digestive Vacuole-Disrupting Molecules Reveals Valuable Starting Points for Drug Discovery.Antimicrobial agents and chemotherapy · 2018Article
- Antimalarial Activity of Small-Molecule Benzothiazole Hydrazones.Antimicrobial agents and chemotherapy · 2016Article
- Mechanisms of hematin crystallization and inhibition by the antimalarial drug chloroquine.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Syntheses and biological studies of marine terpenoids derived from inorganic cyanide.Natural product reports · 2015Review
- Targeting the cell stress response of Plasmodium falciparum to overcome artemisinin resistance.PLoS biology · 2015Article
- Determination of the cytostatic and cytocidal activities of antimalarial compounds and their combination interactions.Current protocols in chemical biology · 2014Article
- Malarial hemozoin: from target to tool.Biochimica et biophysica acta · 2014Review
- To kill or not to kill, that is the question: cytocidal antimalarial drug resistance.Trends in parasitology · 2014Article
- Article
- Cytostatic versus cytocidal profiling of quinoline drug combinations via modified fixed-ratio isobologram analysis.Malaria journal · 2013Article
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Authors and funding
8 authors at 1 institution in 1 country.
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Abstract
We report an improved, nonhazardous, high-throughput assay for in vitro quantification of antimalarial drug inhibition of β-hematin (hemozoin) crystallization performed under conditions that are more physiological relative to previous assays. The assay uses the differential detergent solubility of crystalline and noncrystalline forms of heme and is optimized via the use of lipid catalyst. Using this assay, we quantify the effect of pH on the crystal growth-inhibitory activities of current quinoline antimalarials, evaluate the catalytic efficiencies of different lipids, and test for a possible correlation between hemozoin inhibition by drugs versus their antiplasmodial activity. Consistent with several previous reports, we found a good correlation between hemozoin inhibition potency versus cytostatic antiplasmodial potency (50% inhibitory concentration) for a series of chloroquine (CQ) analogues. However, we found no correlation between hemozoin inhibition potency and cytocidal antiplasmodial potency (50% lethal dose) for the same drugs, suggesting that cellular targets for these two layers of 4-aminoquinoline drug activity differ. This important concept is also explored further for QN and its stereoisomers in the accompanying paper (A. P. Gorka, K. S. Sherlach, A. C. de Dios, and P. D. Roepe, Antimicrob. Agents Chemother. 57:365-374, 2013).
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