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与标准抗疟药物相比,蒿甲醚对恶性疟原虫非洲分离株(塞内加尔)的体外活性。

In vitro activity of artemether against African isolates (Senegal) of Plasmodium falciparum in comparison with standard antimalarial drugs.

作者信息

Pradines B, Rogier C, Fusai T, Tall A, Trape J F, Doury J C

机构信息

Unite de Parasitologie, Institut de Medecine Tropicale du Service de Sante des Armees, Marseille, France.

出版信息

Am J Trop Med Hyg. 1998 Mar;58(3):354-7. doi: 10.4269/ajtmh.1998.58.354.

Abstract

The in vitro activity of artemether against 56 African isolates of Plasmodium falciparum from Senegal was evaluated using an isotope-based drug susceptibility semi-microtest. The 50% inhibitory concentration (IC50) values for artemether were in a narrow range from 0.8 to 15.2 nM (mean IC50 = 3.43 nM) and the 95% confidence interval (CI) was 2.50-4.36 nM. Artemether was equally effective on chloroquine-sensitive and chloroquine-resistant isolates (mean IC50 = 346 nM, 95% CI = 2.08-4.84 nM versus mean IC50 = 2.80 nM, 95% CI = 2.00-3.60 nM). There was a significant positive correlation between responses to artemether and mefloquine (r2 = 0.36, P < 0.001), artemether and quinine (r2 = 0.085, P < 0.05), artemether and halofantrine (r2 = 0.075, P < 0.05), quinine and mefloquine (r2 = 0.205, P < 0.01), quinine and halofantrine (r2 = 0.124, P < 0.05), and mefloquine and halofantrine (r2 = 0.801, P < 0.001). A positive correlation between these drugs suggests in vitro cross-resistance or at least in vitro cross-susceptibility.

摘要

采用基于同位素的药物敏感性半微量试验,评估了蒿甲醚对来自塞内加尔的56株非洲恶性疟原虫分离株的体外活性。蒿甲醚的50%抑制浓度(IC50)值在0.8至15.2 nM的狭窄范围内(平均IC50 = 3.43 nM),95%置信区间(CI)为2.50 - 4.36 nM。蒿甲醚对氯喹敏感和氯喹耐药分离株同样有效(平均IC50 = 346 nM,95% CI = 2.08 - 4.84 nM,对比平均IC50 = 2.80 nM,95% CI = 2.00 - 3.60 nM)。蒿甲醚与甲氟喹(r2 = 0.36,P < 0.001)、蒿甲醚与奎宁(r2 = 0.085,P < 0.05)、蒿甲醚与卤泛群(r2 = 0.075,P < 0.05)、奎宁与甲氟喹(r2 = 0.205,P < 0.01)、奎宁与卤泛群(r2 = 0.124,P < 0.05)以及甲氟喹与卤泛群(r2 = 0.801,P < 0.001)之间存在显著正相关。这些药物之间的正相关表明存在体外交叉耐药性或至少存在体外交叉敏感性。

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