Chloroquine resistance in the malaria parasite Plasmodium falciparum has made malaria increasingly difficult to control. Chloroquine-resistant parasites accumulate less chloroquine than their chloroquine-sensitive counterparts; however, the mechanism underlying this remains unclear. The primary site of accumulation and antimalarial action of chloroquine is the internal acidic digestive vacuole ...

The saturable uptake of chloroquine by parasites of Plasmodium falciparum has been attributed to specific carrier-mediated transport of chloroquine. It is suggested that chloroquine is transported in exchange for protons by the parasite membrane Na+/H+ exchanger [J Biol Chem 272:2652-2658 (1997)]. Once inside the parasite, it is proposed that chloroquine inhibits the polymerization of hematin, ...

antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs, chloroquine (cq) and amodiaquine (aq), have been used to prevent and treat malaria for many years. the importance of these drugs is related to their simple usage, high efficacy, affordability, and cost-effectiveness of their synthesis. in recent years, with the spread of parasite resistance to cq and cross-resist...

In this article, we are collectively presenting case reports of 15 patients who developed pigmentary changes of the skin and mucus membrane during the course of chloroquine therapy for connective tissue disorders. These female patients developed hyper pigmentation of the skin, largely on the exposed parts of the body. The pigmentary changes varied from brownish/ grayish/ bluish-black in color, ...

the children aged under 5 years from vast african areas badly suffer from falciparum malaria and many of them die of this disease. therapeutic efficacy of anti-malaria drugs, especially pyrimethamine-sulfadoxine (ps) and chloroquine (cq) to falciparum malaria is frequently evaluated and reported in recent 10 years. unfortunately, to date, these widespread materials and researches have not been ...

The in vitro activities of new organometallic chloroquine analogs, based on 4-amino-quinoleine compounds bound to a molecule of ferrocene, were evaluated against chloroquine-susceptible, chloroquine-intermediate, and chloroquine-resistant, culture-adapted Plasmodium falciparum lineages by a proliferation test. One of the ferrocene analogs totally restored the activity of chloroquine against chl...

Spironolactone has produced beneficial effects in animal models of neurodegenerative disorders. However, the underlying mechanisms of this agent on neurons and glia are mostly unknown. Therefore, we aimed to show the effects of spironolactone and fludrocortisone, a mineralocorticosteroid receptor agonist, on neuronal and glial toxicity induced by N-methyl-D-aspartate (NMDA) activation and chlor...

In the studies reported here, we examined the inoculum effect observed with chloroquine and Plasmodium falciparum. The 50% effective doses observed with both chloroquine-susceptible and -resistant parasites increased five- to sevenfold from their baseline values as the inoculum was increased from 2 X 10(5) to 2 X 10(7) parasitized erythrocytes per ml (parasitemias of 0.1 to 10% with a hematocri...