Fowler R E, Billingsley P F, Pudney M, Sinden R E
Department of Biology, Imperial College of Science, Technology and Medicine, London.
Parasitology. 1994 May;108 ( Pt 4):383-8. doi: 10.1017/s0031182000075922.
The activity of atovaquone against Plasmodium berghei ANKA during sporogonic development has been examined. Anopheles stephensi mosquitoes were fed on gametocyte infected mice which had been treated 8 h previously with atovaquone or diluent alone. Mosquito midguts were examined for oocysts, and salivary gland infections were estimated using an ELISA for the circumsporozoite protein (CSP). The number of oocysts per midgut fell by at least 97% when mosquitoes were fed on mice dosed with 0.1-10 mg atovaquone/kg body weight. This was paralleled by a decrease in the prevalence of oocyst-infected mosquitoes from 70-90% in controls to 40% or 10% respectively. No oocysts were observed at a dose of 100 mg/kg. CSP ELISA results indicated that mosquitoes fed on atovaquone failed to produce sporozoites. Mosquitoes which fed on gametocytaemic, atovaquone-treated mice (0.1-100 mg/kg) did not transmit malaria to naive mice. These results demonstrate that atovaquone has a highly potent inhibitory activity against the mosquito stages of P. berghei.
已对阿托伐醌在伯氏疟原虫ANKA孢子生殖发育过程中的活性进行了研究。用斯蒂芬斯按蚊叮咬感染了配子体的小鼠，这些小鼠在8小时前单独用阿托伐醌或稀释剂进行了处理。检查蚊中肠的卵囊，并使用针对环子孢子蛋白（CSP）的ELISA法评估唾液腺感染情况。当用0.1 - 10 mg阿托伐醌/千克体重给小鼠给药后，让蚊子叮咬这些小鼠，每个中肠的卵囊数量至少减少了97%。这伴随着卵囊感染蚊子的发生率从对照组的70 - 90%分别降至40%或10%。在100 mg/kg的剂量下未观察到卵囊。CSP ELISA结果表明，以阿托伐醌喂养的蚊子未能产生子孢子。以感染了配子体且经阿托伐醌处理（0.1 - 100 mg/kg）的小鼠为食的蚊子未将疟疾传播给未感染的小鼠。这些结果表明，阿托伐醌对伯氏疟原虫的蚊期具有高效的抑制活性。
