Coleman R E, Nath A K, Schneider I, Song G H, Klein T A, Milhous W K
Department of Entomology, Walter Reed Army Institute of Research, Washington, District of Columbia.
Am J Trop Med Hyg. 1994 May;50(5):646-53. doi: 10.4269/ajtmh.1994.50.646.
The sporontocidal activity of three 8-aminoquinolines, a 1,4-naphthoquinone, and three dihydroacridine-diones was determined against the ANKA clone of Plasmodium berghei and both chloroquine-sensitive (NF54) and chloroquine-resistant (7G8) P. falciparum. Anopheles stephensi mosquitoes previously fed on P. berghei--infected mice or P. falciparum--infected cultures were refed on uninfected mice treated previously with a given drug. Sporontocidal activity was determined by assessing both oocyst and sporozoite development. Neither primaquine nor menoctone exhibited sporontocidal activity against P. berghei or either strain of P. falciparum at a dose of 100 mg base drug/kg mouse body weight, whereas the other five compounds each effectively interrupted the sporogonic development of all three parasite strains at this dose. These data clearly demonstrate that experimental dihydroacridine-diones and 8-aminoquinolines are capable of interrupting the sporogonic development of P. berghei and chloroquine-sensitive and chloroquine-resistant P. falciparum. These data also suggest that the P. berghei model may be used to accurately predict sporontocidal activity against P. falciparum.
测定了三种8-氨基喹啉、一种1,4-萘醌和三种二氢吖啶二酮对伯氏疟原虫ANKA克隆株以及氯喹敏感（NF54）和氯喹耐药（7G8）恶性疟原虫的杀配子体活性。先前吸食过感染伯氏疟原虫的小鼠或感染恶性疟原虫培养物的斯氏按蚊，再吸食先前用特定药物处理过的未感染小鼠。通过评估卵囊和子孢子发育来确定杀配子体活性。在剂量为100mg碱基药物/千克小鼠体重时，伯氨喹和甲萘醌对伯氏疟原虫或任何一种恶性疟原虫菌株均未表现出杀配子体活性，而其他五种化合物在此剂量下均有效阻断了所有三种寄生虫菌株的孢子生殖发育。这些数据清楚地表明，实验性二氢吖啶二酮和8-氨基喹啉能够阻断伯氏疟原虫以及氯喹敏感和氯喹耐药恶性疟原虫的孢子生殖发育。这些数据还表明，伯氏疟原虫模型可用于准确预测对恶性疟原虫的杀配子体活性。
