Ten plants indigenous to Sudan and of common use in Sudanese folk-medicine, were examined in vitro for antimalarial activity against schizonts maturation of Plasmodium falciparum, the major human malaria parasite.
The growth inhibition of Plasmodium falciparum strains was evaluated using the measurement of lactate dehydrogenase activity.
To discover new antimalarial chemotypes, we have used a phenotypic forward chemical genetic approach to assay 309,474 chemicals. Here we disclose structures and biological activity of the entire library—many of which showed potent in vitro activity against drug-resistant P. falciparum strains—and detailed profiling of 172 representative candidates.
Antimalarial sensitivity was studied using Plasmodium falciparum and the [3H]-hypoxanthine incorporation assay. Cytotoxic effects on a T-cell leukaemia (Jurkat) cell line were determined using the tetrazolium-based cellular toxicity assay.
Four aspartyl proteases known as plasmepsins are involved in the degradation of hemoglobin by Plasmodium falciparum, which causes a large percentage of malaria deaths. The enzyme plasmepsin II (PlmII) is the most extensively studied of these aspartyl proteases and catalyzes the initial step in the breakdown of hemoglobin by the parasite.
A collaborative effort between the Global Malaria Program of the World Health Organization (WHO) and the WorldWide Antimalarial Resistance Network (WWARN) has recently been launched.
The V-type H+-ATPase is critical during the intraerythrocytic stage of the human malaria parasite Plasmodium falciparum. Our data support the disruption of parasite pH regulation through inhibition of its V-type H+-ATPase as an antimalarial approach.
The antimalarial synthetic ozonide OZ277 (RBx11160) was hydroxylated by human liver microsomes at the distal bridgehead carbon atoms of the spiroadamantane substructure to form two carbinol metabolites devoid of antimalarial activity.
Using this methodology a range of bridged tetraoxanes which display good in vitro antimalarial activity were synthesized.
The stage-specific antimalarial activities of a panel of antiretroviral protease inhibitors (PIs), including two nonpeptidic PIs (tipranavir and darunavir), were tested in vitro against Plasmodium falciparum.