Basco L K, Bickii J, Ringwald P
Institut Français de Recherche Scientifique pour le Développement en Coopération (ORSTOM)- Organisation de Coordination pour la lutte contre les Endémies en Afrique.
Antimicrob Agents Chemother. 1998 Sep;42(9):2347-51. doi: 10.1128/AAC.42.9.2347.
The in vitro antimalarial activity of the new Chinese synthetic drug, lumefantrine, also known as benflumetol (a fluorene derivative belonging to the aminoalcohol class), was determined by an isotopic microtest against 61 fresh clinical isolates of Plasmodium falciparum and compared with that of other established antimalarial agents. The geometric mean 50% inhibitory concentration of lumefantrine was 11.9 nmol/liter (95% confidence intervals, 10.4 to 13.6 nmol/liter; range, 3.3 to 25.6 nmol/liter). The in vitro activities of lumefantrine against the chloroquine-sensitive and the chloroquine-resistant isolates did not differ (P > 0.05). There was a significant positive correlation of responses between lumefantrine and two other aminoalcohols studied, mefloquine (r = 0.688) and halofantrine (r = 0.677), and between lumefantrine and artesunate (r = 0.420), suggesting a potential for in vitro cross-resistance. Our data suggest high in vitro activity of lumefantrine, comparable to that of mefloquine, and are in agreement with the promising results of preliminary clinical trials.
新型中国合成药物本芴醇（又称氯氟菲醇，属于氨基醇类的芴衍生物）的体外抗疟活性，通过同位素微量试验针对61株恶性疟原虫新鲜临床分离株进行了测定，并与其他既定抗疟药物的活性进行了比较。本芴醇的几何平均50%抑制浓度为11.9纳摩尔/升（95%置信区间为10.4至13.6纳摩尔/升；范围为3.3至25.6纳摩尔/升）。本芴醇对氯喹敏感和氯喹耐药分离株的体外活性没有差异（P>0.05）。本芴醇与另外两种研究的氨基醇甲氟喹（r=0.688）和卤泛群（r=0.677）之间，以及本芴醇与青蒿琥酯（r=0.420）之间的反应存在显著正相关，表明存在体外交叉耐药的可能性。我们的数据表明本芴醇具有较高的体外活性，与甲氟喹相当，并且与初步临床试验的良好结果一致。
