Le Bras J, Deloron P, Hartmann J F, Coulanges P, Dourado H V, Larouze B
Trans R Soc Trop Med Hyg. 1984;78(4):485-8. doi: 10.1016/0035-9203(84)90068-3.
The activity of four antimalarial drugs against 66 Plasmodium falciparum isolates from 15 countries was assessed by an in vitro semi-microtest. Median inhibitory concentrations (IC50) for chloroquine were less than 120 nM in 22 isolates from patients successfully treated with chloroquine, and more than 250 nM in six isolates from patients with chloroquine-resistant malaria. 10 of 15 isolates from Brazil (Amazonia), 7 of 12 isolates from Madagascar, two from Kenya and two from Thailand had IC50 for chloroquine of more than 250 nM. None of the 35 isolates from West and Central Africa had IC50 of more than 120 nM. Very different levels of sensitivity were observed in Brazil and Madagascar. 27 of 28 isolates (including two that were chloroquine-resistant in vivo) had IC50 of less than 50 nM for dichlorquinazine, a 4-aminoquinoline. The IC50 for mefloquine was less than 160 nM in 55 isolates including ten from patients who were successfully treated with mefloquine. IC50 for quinine were between 140 and 660 nM for 30 isolates. This test has proved useful in epidemiological studies, therapeutic monitoring of clinical cases and in the evaluation of new drugs.
通过体外半微量试验评估了四种抗疟药物对来自15个国家的66株恶性疟原虫分离株的活性。来自成功接受氯喹治疗患者的22株分离株中,氯喹的半数抑制浓度(IC50)小于120 nM,而来自氯喹耐药疟疾患者的6株分离株中,IC50大于250 nM。来自巴西(亚马逊地区)的15株分离株中有10株、来自马达加斯加的12株分离株中有7株、来自肯尼亚的2株以及来自泰国的2株,其氯喹的IC50大于250 nM。来自西非和中非的35株分离株中,没有一株的IC50大于120 nM。在巴西和马达加斯加观察到了非常不同的敏感性水平。28株分离株中的27株(包括两株体内对氯喹耐药的分离株)对4-氨基喹啉二氯喹嗪的IC50小于50 nM。包括10株来自成功接受甲氟喹治疗患者的分离株在内,55株分离株中甲氟喹的IC50小于160 nM。30株分离株中奎宁的IC50在140至660 nM之间。该试验已证明在流行病学研究、临床病例的治疗监测以及新药评估中有用。