SPORONTOCIDAL ACTIVITY OF THE ANTIMALARIAL WR-238605 AGAINST PLASMODIUM-BERGHEI ANKA IN ANOPHELES-STEPHENSI
SPORONTOCIDAL ACTIVITY OF THE ANTIMALARIAL WR-238605 AGAINST PLASMODIUM-BERGHEI ANKA IN ANOPHELES-STEPHENSI
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DOI：
10.4269/ajtmh.1990.42.196
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发表时间：
1990-03-01
影响因子：
3.3
通讯作者：
COLEMAN, RE
中科院分区：
文献类型：
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作者：
COLEMAN, RE
确定了 WR-238605（8-[{4-氨基-1-甲基-丁基}氨基]-2,6-二甲氧基-4-甲基-5-[3-三氟甲基苯氧基]喹啉琥珀酸酯）对伯氏疟原虫 ANKA 克隆孢子发育的影响。将史氏按蚊喂给提前 90 分钟用 25 或 50 mg WR-238605/kg 体重处理的伯氏疟原虫感染的小鼠。蚊子吸食经过药物处理的小鼠后，产生的动动子数量与喂食对照组小鼠的动动子数量相同。与对照组相比，接受药物喂养的蚊子产生的卵囊/蚊子数量较少。这些卵囊的发育速度比对照喂养的蚊子的卵囊发育得更慢。子孢子不会侵入药物喂养的蚊子的唾液腺，这些蚊子也不会将伯氏疟原虫传播给小鼠。蚊子感染伯氏疟原虫后 6 或 12 天摄入 WR-238605 对带有卵囊的蚊子的百分比或每只蚊子产生的卵囊的平均数量没有影响。感染后第 6 天摄入药物的蚊子的卵囊发育显着延迟。第 6 天或第 12 天药物喂养的蚊子随后的唾液腺子孢子感染比对照蚊子或第 18 天药物喂养的蚊子轻。这些数据表明 WR-238605 具有显着的杀孢子活性。
The influence of WR-238605 (8-[{4-amino-1-methyl-butyl} amino]-2,6-dimethoxy-4-methyl-5-[3-tri-fluoromethylphenoxy] quinoline succinate) on the sporogonic development of a Plasmodium berghei ANKA clone was determined. Anopheles stephensi were fed on P. berghei infected mice treated 90 min earlier with 25 or 50 mg WR-238605/kg body weight. Mosquitoes engorging on drug-treated mice produced the same number of ookinetes as did those fed on controls; drug-fed mosquitoes produced fewer oocysts/mosquito than did controls. These oocysts developed more slowly than did those in control-fed mosquitoes. Sporozoites did not invade the salivary glands of drug-fed mosquitoes, nor did these mosquitoes transmit P. berghei to mice. Uptake of WR-238605 6 or 12 days after mosquitoes were infected with P. berghei had no effect on the percentage of mosquitoes with oocysts or the mean number of oocysts produced per mosquito. Oocyst development was significantly retarded in mosquitoes ingesting drug on day 6 postinfection. Subsequent salivary gland sporozoite infections were lighter in mosquitoes drug-fed on day 6 or day 12 than in control mosquitoes or mosquitoes drug-fed on day 18. These data indicate that WR-238605 has significant sporontocidal activity.