S1 PfCRT cannot be a channel for un-protonated chloroquine CQ S2 Membrane equilibrium equation S3 The expression for the Cellular Accumulation Ratio of chloroquine S4 Chloroquine concentration is equal in the external buffer and inside the erythrocyte S5 CAR expressions in the case of chloroquine-HM binding in linear regime (hypothesis H1) S6 Proof that [CQ]DV,D = [CQ]e in the hypothesis PfCRT ...

Sulfadoxine/pyrimethamine (SP) is increasingly used against malaria in sub-Saharan Africa because of chloroquine resistance. However, chloroquine may have a beneficial antipyretic effect. We therefore compared the combination of SP plus chloroquine, chloroquine alone, SP alone, and SP plus paracetamol in the treatment of uncomplicated Plasmodium falciparum malaria in 175 Tanzanian children (1-4...

Chloroquine began as a first-line antimalarial in 1946, the same year that the rock star Cher was born. Similar to Cher, chloroquine peaked in popularity in the early 1960s. Cher has famously made several major comebacks. Is it now chloroquine’s turn? For decades, chloroquine was a remarkably effective, safe, and inexpensive antimalarial. Optimism about effectiveness of chloroquine led public h...

BACKGROUND Treatment failure of chloroquine for P. vivax infections has reached high levels in the eastern provinces of Indonesia, however, in vitro characterization of chloroquine resistance and its associated molecular profile have yet to be determined. METHODS Using a modified schizont maturation assay we investigated the in vitro chloroquine susceptibility profile and molecular polymorphi...

Cepharanthin is a proprietary extract of Stephania cepharantha, widely used in Japan for the treatment of inflammatory diseases. Cephranthin, its component alkaloids, and the standard resistance modulator verapamil were tested against Plasmodium falciparum for capacity to modulate sensitivity to chloroquine. Cepharanthin enhanced the activity of chloroquine against resistant clones by a factor ...

Mutations in the Plasmodium falciparum chloroquine resistance transporter (pfcrt) gene were examined to assess their associations with chloroquine resistance in clinical samples from Armopa (Papua) and Papua New Guinea. In Papua, two of the five pfcrt haplotypes found were new: SVIET from Armopa and CVIKT from an isolate in Timika. There was also a strong association (P < 0.0001) between the pf...

BACKGROUND The return of chloroquine-sensitive Plasmodium falciparum to the limited area of Blantyre, Malawi, has been well demonstrated in several studies. METHODS To characterize chloroquine susceptibility over a wide geographic area, infants and children aged 6-59 months were selected using 2-stage cluster sampling in 8 Malawian districts. Pyrosequencing of the pfcrt gene codon 76 region w...

The basal activity of Ca2+-ATPase in two isolates (NL56, UNC) and two clones (D6, W2) of P.falciparum was assessed. The effects of various concentrations of chloroquine phosphate and toxic concentrations of lead acetate were also evaluated in the clones and strains of P.falciparum. The Ca2+-ATPase activity was measured by monitoring the rate of release of inorganic phosphate from the gamma-posi...

BACKGROUND Chloroquine-resistant Plasmodium falciparum malaria is a major health problem, particularly in sub-Saharan Africa. Chloroquine resistance has been associated in vitro with point mutations in two genes, pfcrt and pfmdr 1, which encode the P. falciparum digestive-vacuole transmembrane proteins PfCRT and Pgh1, respectively. METHODS To assess the value of these mutations as markers for...

K1 strain of Plasmdoium falciparum is resistant in vitro to chloroquine, pyrimethamine and sulfadoxine. Response of this strain to combinations of antimalarial drugs in the in vitro hypoxanthine incorporation test was coupled with that of a line of strain NF54 relatively sensitive to chloroquine and fully sensitive to other antimalarials. Pyrimethamine and sulfadoxine showed potentiative synerg...