Basco Leonardo K, Ringwald Pascal
Unité de Recherche Paludologie Afro-tropicale, Institut de Recherche pour le Développement (IRD), Organisation de Coordination pour la lutte contre les Endémies en Afrique Centrale (OCEAC), Yaoundé, Cameroon.
Antimicrob Agents Chemother. 2003 Apr;47(4):1391-4. doi: 10.1128/AAC.47.4.1391-1394.2003.
The spread of chloroquine-resistant Plasmodium falciparum calls for a constant search for new drugs. The in vitro activity of piperaquine, a new Chinese synthetic drug belonging to the bisquinolines, was evaluated in 103 fresh clinical isolates of P. falciparum in Cameroon, Central Africa, and compared with that of other 4-aminoquinoline and Mannich base derivatives and dihydroartemisinin. Piperaquine was highly active (geometric mean 50% inhibitory concentration, 38.9 nmol/liter; range, 7.76 to 78.3 nmol/liter) and equally active (P > 0.05) against the chloroquine-sensitive and the chloroquine-resistant isolates. There was a significant but low correlation of response between chloroquine and piperaquine (r = 0.257, P < 0.05). These results suggest that further development of piperaquine, in combination with dihydroartemisinin, holds promise for use in chloroquine-resistant regions of endemicity.
耐氯喹恶性疟原虫的传播促使人们不断寻找新药。哌喹是一种新的中国合成双喹啉类药物，对来自中非喀麦隆的103株新鲜恶性疟原虫临床分离株进行了体外活性评估，并与其他4-氨基喹啉、曼尼希碱衍生物及双氢青蒿素进行了比较。哌喹活性很高（几何平均半数抑制浓度为38.9纳摩尔/升；范围为7.76至78.3纳摩尔/升），对氯喹敏感及耐氯喹的分离株活性相同（P>0.05）。氯喹与哌喹之间存在显著但较低的反应相关性（r = 0.257，P<0.05）。这些结果表明，哌喹与双氢青蒿素联合用药的进一步研发有望用于疟疾流行的耐氯喹地区。
