Basco L K, Peytavin G, Gimenez F, Genissel B, Farinotti R, Le Bras J
Department of Parasitology, Hôpital Bichat-Claude Bernard, Paris, France.
Trop Med Parasitol. 1994 Mar;45(1):45-6.
The in vitro activity of the enantiomers of N-desbutylhalofantrine, the major human metabolite of halofantrine, was compared using the semi-microtest against the multidrug-resistant Plasmodium falciparum FCM 29/Cameroon clone. The mean 50% inhibitory concentration (IC50) values (+/- standard deviation) of the enantiomers were equivalent (2.07 +/- 0.41 and 1.70 +/- 0.33 nmol/L). The enantiomers of the metabolite of halofantrine, as well as those of the parent compound, have the same antimalarial activity. Since (+)-halofantrine and enantiomer-1 of the metabolite attain higher plasma concentrations in man, our study suggests that these enantiomers may be more active in vivo.
使用半微量试验，比较了卤泛群的主要人体代谢产物N-去丁基卤泛群对多药耐药恶性疟原虫FCM 29/喀麦隆克隆株的对映体的体外活性。这些对映体的平均50%抑制浓度（IC50）值（±标准差）相当（分别为2.07±0.41和1.70±0.33 nmol/L）。卤泛群代谢产物的对映体以及母体化合物的对映体具有相同的抗疟活性。由于（+）-卤泛群及其代谢产物的对映体-1在人体中达到较高的血浆浓度，我们的研究表明这些对映体在体内可能更具活性。
