Fleck S L, Pudney M, Sinden R E
Department of Biology, Imperial College, London, UK.
Trans R Soc Trop Med Hyg. 1996 May-Jun;90(3):309-12. doi: 10.1016/s0035-9203(96)90266-7.
Atovaquone (566C80), a hydroxynaphthoquinone, was investigated for activity against Plasmodium falciparum gametocytes (NF54 strain) in vitro. After 96 h of continuous exposure to the drug at 1.4 x 10(-7) M (a concentration achievable in humans 14 d after administration of a therapeutic dose of 10 mg/kg) reductions of 75%, 54% and 20% in the number of gametocyte stages 2, 3 and 4, respectively, were achieved. A small increase (14%) in stage 5 gametocytes was seen. At the same concentration, atovaquone showed greater activity against the asexual stages of P. falciparum, reductions of 93%, 96% and 43% in the number of rings, schizonts and trophozoites, respectively, being achieved. These data are consistent with inhibition of maturation of trophozoites. The observed effect on maturation of gametocytes is similarly consistent with blockade of gametocyte recruitment from merozoites produced by the preceding schizogony, or to stasis of intraerythrocytic sexual development before the formation of stage 2 gametocytes.
阿托伐醌（566C80），一种羟基萘醌，在体外被研究对恶性疟原虫配子体（NF54株）的活性。在以1.4×10⁻⁷ M（在给予10 mg/kg治疗剂量14天后人体可达到的浓度）持续暴露于该药物96小时后，配子体2期、3期和4期的数量分别减少了75%、54%和20%。观察到5期配子体有小幅增加（14%）。在相同浓度下，阿托伐醌对恶性疟原虫无性阶段显示出更大活性，环状体、裂殖体和滋养体的数量分别减少了93%、96%和43%。这些数据与滋养体成熟受到抑制一致。观察到的对配子体成熟的影响同样与阻断前一次裂体增殖产生的裂殖子发育为配子体，或在2期配子体形成之前使红细胞内有性发育停滞一致。
