Teklehaimanot A, Nguyen-Dinh P, Collins W E, Barber A M, Campbell C C
Am J Trop Med Hyg. 1985 May;34(3):429-34. doi: 10.4269/ajtmh.1985.34.429.
A test system that uses infective gametocytes from in vitro cultures was developed for evaluating the sporontocidal activity of antimalarial compounds. In evaluating the system, pyrimethamine and cycloguanil (dihydrofolate reductase inhibitors) and primaquine (8-aminoquinoline) were tested against pyrimethamine-sensitive and pyrimethamine-resistant strains of Plasmodium falciparum. The drugs were administered to Anopheles either in a blood meal containing infective gametocytes or in a noninfective meal 2-4 days later. The mosquitoes were dissected 9-10 days after they received the infective blood meal, and the sporontocidal effect of the drugs was evaluated by the number of oocysts found in the gut. Both cycloguanil and pyrimethamine had marked sporontocidal activity. The susceptibility pattern of the strains to the sporontocidal effect of pyrimethamine and cycloguanil was similar to the susceptibility of their asexual blood stages in vitro to the schizontocidal effect of the compounds. The sporontocidal effect was observed only when the compounds were administered at the same time as the infective blood meal, but not when they were given 2-4 days later. No sporontocidal activity was observed with primaquine. This system permits more reliable quantitative observations than have been possible with previous methods.
开发了一种使用体外培养的感染性配子体的测试系统，用于评估抗疟化合物的杀孢子体活性。在评估该系统时，对乙胺嘧啶和环氯胍（二氢叶酸还原酶抑制剂）以及伯氨喹（8-氨基喹啉）针对恶性疟原虫的乙胺嘧啶敏感和耐药菌株进行了测试。将药物通过含有感染性配子体的血餐或在2-4天后通过非感染性餐喂给按蚊。在按蚊接受感染性血餐后9-10天进行解剖，并通过在肠道中发现的卵囊数量评估药物的杀孢子体效果。环氯胍和乙胺嘧啶均具有显著的杀孢子体活性。这些菌株对乙胺嘧啶和环氯胍杀孢子体作用的敏感性模式与其体外无性血液阶段对这些化合物裂殖体杀灭作用的敏感性相似。仅当化合物与感染性血餐同时给药时才观察到杀孢子体效果，而在2-4天后给药时则未观察到。未观察到伯氨喹的杀孢子体活性。该系统比以前的方法能够进行更可靠的定量观察。
