Bioactivity Comments

The interaction table below provides data from an evaluation of the antimalarial (asexual blood stage) activity of arteflene, using a panel of culture-adapted P. falciparum strains, with no evidence of reduced potency against drug resistant strains being observed.

Whole organism assay data
Key to terms and symbols	Click on species/strain names for details	Click column headers to sort
MOA/likely target Sp. Assay description Type Action Value Parameter Concentration range (M) Reference Unknown MOA PfFCR3 Plasmodium falciparum FCR3 P. falciparum strain FCR3 (PfFCR3) was originally isolated from a patient in The Gambia, West Africa in 1976. PfFCR3 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4). Differences in sensitivity of PfFCR3 clones to chloroquine have been reported, with the original isolate that was chloroquine sensitive rapidly acquiring resistance in culture (PMID: 7031656, PMID: 51801). ✖ Parasite growth inhibition assay - - 7.6 – 7.7 pIC50 - 3 ⤷ pIC50 7.7 (IC50 2.23x10-8 M) [3H]-hypoxanthine incorporation, measured after 72 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) pIC50 7.6 (IC50 2.27x10-8 M) [3H]-hypoxanthine incorporation, measured after 48 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Unknown MOA PfW2 Plasmodium falciparum W2 P. falciparum strain W2 (PfW2) was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfW2 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine and susceptible to mefloquine. ✖ Parasite growth inhibition assay - - 7.5 – 7.7 pIC50 - 3 ⤷ pIC50 7.7 (IC50 2.11x10-8 M) [3H]-hypoxanthine incorporation, measured after 48 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) pIC50 7.5 (IC50 3.25x10-8 M) [3H]-hypoxanthine incorporation, measured after 72 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Unknown MOA PfK1 Plasmodium falciparum K1 P. falciparum strain K1 (PfK1) was isolated in Kanchanaburi, Thailand in 1979. PfK1 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be a multidrug-resistant strain. ✖ Parasite growth inhibition assay - - 7.5 – 7.5 pIC50 - 3 ⤷ pIC50 7.5 (IC50 3.1x10-8 M) [3H]-hypoxanthine incorporation, measured after 48 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) pIC50 7.5 (IC50 3.24x10-8 M) [3H]-hypoxanthine incorporation, measured after 72 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Unknown MOA PfHB3 Plasmodium falciparum HB3 P. falciparum strain HB3 (PfHB3) was cloned from the Honduras I/CDC strain, originally isolated from a patient in Choluteca, Honduras, during an outbreak of urban malaria in January 1980. PfHB3 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be chloroquine sensitive. ✖ Parasite growth inhibition assay - - 7.4 – 7.5 pIC50 - 3 ⤷ pIC50 7.5 (IC50 3.15x10-8 M) [3H]-hypoxanthine incorporation, measured after 48 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) pIC50 7.4 (IC50 4.36x10-8 M) [3H]-hypoxanthine incorporation, measured after 72 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Unknown MOA PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖ Parasite growth inhibition assay - - 7.3 – 7.3 pIC50 - 3 ⤷ pIC50 7.3 (IC50 4.42x10-8 M) [3H]-hypoxanthine incorporation, measured after 48 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) pIC50 7.3 (IC50 4.6x10-8 M) [3H]-hypoxanthine incorporation, measured after 72 hours in culture [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)