The antimalarial activity of some bisbenzylisoquinoline (BBIQ) alkaloids were studied using in vitro culture of both chloroquine (CQ)-sensitive and chloroquine-resistant strains of Plasmodium falciparum. The combination of chloroquine and tetrandrine gave a 44 fold potentiation of malarial killing. Fangchinoline, hernandezine, pycnamine, berbamine and isotetrandrine had similar antimalarial act...

Antimalarial chemotherapy, globally reliant on artemisinin-based combination therapies (ACTs), is threatened by the spread of drug resistance in Plasmodium falciparum parasites. Here we use zinc-finger nucleases to genetically modify the multidrug resistance-1 transporter PfMDR1 at amino acids 86 and 184, and demonstrate that the widely prevalent N86Y mutation augments resistance to the ACT par...

Drug resistance is probably the greatest challenge to most malaria-control programs. Given the limited resources for other malarial-control measures, rational drug used is crucial. Molecular markers for parasite resistance such as pfcrt, pfmdr-1, and dhfr have the potential to be used in an integrated fashion to provide timely information that is useful to policy makers. Therefore, we evaluated...

We have investigated the contribution of drug accumulation and inhibition of heme polymerization to the in vitro activities of a series of antimalarial drugs. Only those compounds exhibiting structural relatedness to the quinolines inhibited heme polymerization. We could find no direct correlation between in vitro activity against chloroquine-susceptible or chloroquine-resistant isolates and ei...

Resistance of Plasmodium falcipanrm to chloroquine has been documented in most countries where there is transmission, over the last 2 decades (PETERS, 1987; PAYNE, 1989). Resistance to other antimalarials has followed in many countries. This article will focus on resistance occurring in chemotherapy rather than prophylaxis. Host factors, including pharmacokinetics and immunity, will not be revi...

OBJECTIVES The main objective of this study was to unravel the distribution of different Pfcrt genotypes in the central, littoral, eastern and southern regions of Cameroon and also in locations bordering Gabon and Equatorial Guinea. This is because (i) the chloroquine-resistant malaria parasite Plasmodium falciparum shows a wide occurrence in Cameroon, (ii) mutations in the 72nd to 76th amino a...

Encystation of Acanthamoeba castellanii is associated with resistance to chemotherapeutic agents. Blocking the encystation process could potentiate the efficacy of chemotherapeutic agents and biocides. During encystation, autophagy is highly stimulated and required for proper encystation of Acanthamoeba. In this study, the cytotoxic effect of chloroquine, a well-known autophagy-inhibitory drug,...

Keywords: Malaria Artemisinin resistance Fifty years ago it was becoming clear that the enormous global effort to eradicate malaria had failed. There were also an increasing number of worrying reports that the wonder drug chloroquine was not working as it should against falciparum malaria in parts of SouthEast Asia and South America. Chloroquine resistance spread slowly at first, but by 1979 it...