Exploiting natural resources for bioactive compounds is an attractive drug discovery strategy in search for new anti-malarial drugs with novel modes of action. Initial screening efforts in our laboratory revealed two preparations of soil-derived actinomycetes (H11809 and FH025) with potent anti-malarial activities. Both crude extracts showed GSK3β-inhibitory activities in a yeast-based kinase a...

Overcoming antigenic variation is one of the major challenges in the development of an effective vaccine against Plasmodium falciparum, a causative agent of human malaria. Inclusion of multiple Ag variants in subunit vaccine candidates is one strategy that has aimed to overcome this problem for the leading blood-stage malaria vaccine targets, that is, merozoite surface protein 1 (MSP1) and apic...

A series of novel chalcone derivatives were synthesized and investigated against the chloroquine-sensitive P. falciparum 3D7 (Pf3D7) strain chloroquine-resistant K1 to establish their structure-activity relationship. In this study, compound 7 was found most active as well less cytotoxic (IC50 = 4.12 µM 3.14 for Pf3D7 PfK1 respectively; CC50 46.18 µM). Compound studied effect on parasite growth ...

A tetrazolium-based colorimetric selective assay (MTT-based CSA) was developed to assess the selectivity of antimalarial drugs. This in vitro assay, unlike all others, measures the ability of drugs to indirectly protect red blood cells (RBCs) from Plasmodium-falciparum-induced destruction. Optimum incubation time and number of cells needed were 5 days and 23 × 10(6) RBCs per well, respectively....

Herein we describe the synthesis and evaluation of a series of novel 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones for in vitro cytotoxicity against three human cancer cell lines as well as for potential antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The title compounds were prepared via PdCl₂-mediated endo-dig cyclization of 2-aryl-8-(arylethyn...

BACKGROUND Studies have shown that the barks and roots of some Apocynaceae species have anticancer and antimalarial properties. In this study, leaf extracts of five selected species of Apocynaceae used in traditional medicine (Alstonia angustiloba, Calotropis gigantea, Dyera costulata, Kopsia fruticosa and Vallaris glabra) were assessed for antiproliferative (APF) and antiplasmodial (APM) activ...

Strain diversity may play a role in delaying development of protective immunity in endemic areas. We evaluated genetic diversity of Plasmodium falciparum infected children before being treated with Sulphadoxine Pyrimethamine (SP) and CoartemTM in Southeastern Tanzania. Allelic diversity of P. falciparum strains were determined in order to further assist in correct estimation of recrudescent and...

Plasmepsins (PMs) are thought to have an important function in hemoglobin degradation in the malarial parasite Plasmodium falciparum and have generated interest as antimalarial drug targets. Four paralogous plasmepsins reside in the food vacuole of P. falciparum. Targeted gene disruption by double crossover homologous recombination has been employed to study food vacuole plasmepsin function in ...