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抗疟药对ICR小鼠体内伯氏疟原虫ANKA株及斯氏按蚊的配子体杀灭和子孢子杀灭活性。

Gametocytocidal and sporontocidal activity of antimalarials against Plasmodium berghei ANKA in ICR Mice and Anopheles stephensi mosquitoes.

作者信息

Coleman R E, Clavin A M, Milhous W K

机构信息

Department of Entomology, Walter Reed Army Institute of Research, Washington, DC.

出版信息

Am J Trop Med Hyg. 1992 Feb;46(2):169-82. doi: 10.4269/ajtmh.1992.46.169.

DOI:10.4269/ajtmh.1992.46.169
PMID:1539752
Abstract

The gametocytocidal and sporontocidal activity of three 8-aminoquinolines (primaquine, WR-238605, and WR-242511), three dihydroacridine-diones (floxacrine, WR-250547, and WR-250548), a 1,4-naphthoquinone (menoctone), a synthetic aminoalcohol (halofantrine), and a guanide (WR-182393) was determined against a cloned line of Plasmodium berghei ANKA. Gametocytocidal activity was assessed by treating mice with a single intraperitoneal inoculation of a given compound (25 mg base drug/kg mouse body weight) four days after the mice were infected with P. berghei. Thin blood smears were made every other day, and the percent parasitemia and macrogametocyte and microgametocyte rates were determined. Floxacrine, menoctone, WR-242511, WR-250547, and WR-250548 effectively cleared sexual and asexual parasites from the peripheral circulation within six days of drug administration. Halofantrine, primaquine, WR-182393, and WR-238605 were ineffective at clearing P. berghei ANKA from circulating erythrocytes at the doses tested; however, mice survival time increased markedly with these compounds when compared with the controls. Significant numbers of macrogametocytes and microgametocytes were present throughout the duration of the infection in mice treated with halofantrine, primaquine, WR-182393, and WR-238605. Sporontocidal activity was evaluated by allowing Anopheles stephensi mosquitoes to feed on P. berghei-infected mice 90 min after treatment with a particular drug. Halofantrine and WR-182393 exhibited no sporontocidal activity, while floxacrine, menoctone, primaquine, WR-238605, WR-242511, WR-250547, and WR-250548 exhibited significant activity. Minimum effective doses (mg base drug/kg of mouse body weight) that prevented mosquitoes from developing sporozoite-infected salivary glands were 0.1563 mg/kg for WR-250547, 0.625 mg/kg for menoctone, 1.25 mg/kg for primaquine, 10 mg/kg for floxacrine, 10 mg/kg for WR-242511, 10 mg/kg for WR-250548, and 25 mg/kg for WR-238605.

摘要

测定了三种8-氨基喹啉(伯氨喹、WR-238605和WR-242511)、三种二氢吖啶二酮(氟甲喹、WR-250547和WR-250548)、一种1,4-萘醌(甲萘醌)、一种合成氨基醇(卤泛群)和一种胍(WR-182393)对伯氏疟原虫ANKA克隆株的杀配子体和杀孢子体活性。在小鼠感染伯氏疟原虫四天后,通过腹腔注射给予单一剂量的特定化合物(25 mg碱药物/千克小鼠体重)来评估杀配子体活性。每隔一天制作薄血涂片,测定疟原虫血症百分比以及大配子体和小配子体率。氟甲喹、甲萘醌、WR-242511、WR-250547和WR-250548在给药后六天内有效清除外周循环中的有性和无性寄生虫。在所测试的剂量下,卤泛群、伯氨喹、WR-182393和WR-238605无法有效清除循环红细胞中的伯氏疟原虫ANKA;然而,与对照组相比,使用这些化合物时小鼠存活时间显著增加。在用卤泛群、伯氨喹、WR-182393和WR-238605治疗的小鼠感染期间,整个过程中都存在大量的大配子体和小配子体。通过让斯氏按蚊在使用特定药物治疗90分钟后叮咬感染伯氏疟原虫的小鼠来评估杀孢子体活性。卤泛群和WR-182393没有杀孢子体活性,而氟甲喹、甲萘醌、伯氨喹、WR-238605、WR-242511、WR-250547和WR-250548表现出显著活性。防止蚊子产生感染子孢子唾液腺的最小有效剂量(mg碱药物/千克小鼠体重),WR-250547为0.1563 mg/kg,甲萘醌为0.625 mg/kg,伯氨喹为1.25 mg/kg,氟甲喹为10 mg/kg,WR-242511为10 mg/kg,WR-250548为10 mg/kg,WR-238605为25 mg/kg。

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