Pradines B, Tall A, Rogier C, Spiegel A, Mosnier J, Marrama L, Fusai T, Millet P, Panconi E, Trape J F, Parzy D
Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Le Pharo, Marseille, France.
Trop Med Int Health. 2002 Mar;7(3):265-70. doi: 10.1046/j.1365-3156.2002.00848.x.
The in vitro activities of ferrochloroquine, chloroquine, quinine, mefloquine, halofantrine, amodiaquine, artesunate, atovaquone, cycloguanil and pyrimethamine were evaluated against Plasmodium falciparum isolates from Senegal (Dielmo, Ndiop), using an isotopic micro-drug susceptibility test. The IC50 values for ferrochloroquine ranged from 0.55 to 28.2 nM and the geometric mean IC50 for the 55 isolates was 7.9 nM (95% CI, 6.5-9.7 nM). Ferrochloroquine was 35 times more active than chloroquine (35-fold greater against chloroquine-resistant isolates), quinine, mefloquine, amodiaquine, cycloguanil and pyrimethamine. Weak positive correlations were observed between the responses to ferrochloroquine and that to chloroquine, quinine, and amodiaquine, but not compulsorily predictive of cross-resistance. There was no significant correlation between the response to ferrochloroquine and that to mefloquine, halofantrine, artesunate, atovaquone, cycloguanil and pyrimethamine. Ferrochloroquine may be an important alternative drug for the treatment of chloroquine-resistant malaria.
使用同位素微量药物敏感性试验，评估了铁氯喹、氯喹、奎宁、甲氟喹、卤泛群、阿莫地喹、青蒿琥酯、阿托伐醌、环氯胍和乙胺嘧啶对来自塞内加尔（迪耶尔莫、恩迪奥普）的恶性疟原虫分离株的体外活性。铁氯喹的IC50值范围为0.55至28.2 nM，55株分离株的几何平均IC50为7.9 nM（95%置信区间，6.5 - 9.7 nM）。铁氯喹的活性比氯喹、奎宁、甲氟喹、阿莫地喹、环氯胍和乙胺嘧啶高35倍（对氯喹耐药分离株的活性高35倍）。观察到铁氯喹与氯喹、奎宁和阿莫地喹的反应之间存在弱正相关，但并非必然预示交叉耐药性。铁氯喹与甲氟喹、卤泛群、青蒿琥酯、阿托伐醌、环氯胍和乙胺嘧啶的反应之间没有显著相关性。铁氯喹可能是治疗氯喹耐药疟疾的一种重要替代药物。
