A5027858571- Polyamine Metabolism and Applications
- Malaria Research and Control
- Trypanosoma species research and implications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Computational Drug Discovery Methods
- Synthesis and Biological Evaluation
- HIV/AIDS drug development and treatment
- Cannabis and Cannabinoid Research
- Mosquito-borne diseases and control
University of Pretoria
2011-2018
A series of alkylated (bis)urea and (bis)thiourea polyamine analogues were synthesized screened for antimalarial activity against chloroquine-sensitive -resistant strains Plasmodium falciparum in vitro. All showed growth inhibitory P. at less than 3 μM, with the majority having effective IC50 values 100–650 nM range. Analogues arrested parasitic within 24 h exposure due to a block nuclear division therefore asexual development. Moreover, this effect appears be cytotoxic highly selective...
The life cycle of the malaria parasite Plasmodium falciparum is tightly regulated, oscillating between stages intense proliferation and quiescence. Cyclic 48-hour asexual replication markedly different from cell division in higher eukaryotes, mechanistically poorly understood. Here, we report tight synchronisation parasites during early phases by exposure to DL-α-difluoromethylornithine (DFMO), which results depletion polyamines. This induces an inescapable arrest G1 (~15 hours...
ABSTRACT Anthracene-polyamine conjugates inhibit the in vitro proliferation of intraerythrocytic human malaria parasite Plasmodium falciparum , with 50% inhibitory concentrations (IC 50 s) nM to μM range. The compounds are taken up into parasite, where they arrest cell cycle. Both anthracene and polyamine components play a role their antiplasmodial effect.
ABSTRACT The life cycle of the malaria parasite Plasmodium falciparum is tightly regulated, oscillating between stages intense proliferation and quiescence. Cyclic 48-hour asexual replication markedly different from cell division in higher eukaryotes, mechanistically poorly understood. Here, we report tight synchronisation parasites during early phases by exposure to DL-α-difluoromethylornithine (DFMO), which results depletion polyamines. This induces an inescapable arrest G 1 (~15 hours...