The hematin-targeting properties of pynacrine, an acridine analog of the schizontocidal antimalarial drug, pyronaridine, were evaluated to probe the role of the latter’s benzonaphthyridine moiety. Pynacrine was as active as pyronaridine in inhibiting glutathione-induced hematin degradation and in enhancing hematin-mediated membrane lysis. It formed a 1:2 complex with hematin but was 50-fold less effective in inhibiting β-hematin formation. However, pynacrine was as potent as pyronaridine in inhibiting intra-erythrocytic Plasmodium falciparum growth in culture, suggesting that it has other off-target(s) effects.
All Keywords
【저자키워드】 pyronaridine, Plasmodium falciparum, antiplasmodial, Hematin, 9-Aminoacridine, Pynacrine,
【저자키워드】 pyronaridine, Plasmodium falciparum, antiplasmodial, Hematin, 9-Aminoacridine, Pynacrine,