Ndounga M, Basco L K, Ringwald P
Laboratoire de pharmacologie, Centre d'études sur les ressources végétales (CERVE), Brazzaville, Congo.
Bull Soc Pathol Exot. 1999 Dec;92(5):313-6.
The in vitro activity of proguanil, cycloguanil (active metabolite of proguanil), pyrimethamine, and chloroquine was determined for 14 isolates of Plasmodium falciparum and the chloroquine-resistant W2 clone. In vitro assays were performed by using different types of RPMI 1640 culture medium and incubation period. The use of the standard RPMI medium or RPMI medium containing low concentrations of folate and para-aminobenzoic acid increases the 50% inhibitory concentrations of cycloguanil and pyrimethamine, as compared with the use of folate- and para-aminobenzoic acid-free RPMI medium. The concentrations of folate and para-aminobenzoic acid did not affect the in vitro activity of proguanil and chloroquine. However, prolongation of the incubation period from 42 to 66 hours decreased the 50% inhibitory concentrations of all test compounds. The weak antagonism in vitro between chloroquine and proguanil or cycloguanil does not seem to have any repercussion on the in vivo efficacy of chloroquine-proguanil combination.
测定了氯胍、环氯胍（氯胍的活性代谢产物）、乙胺嘧啶和氯喹对14株恶性疟原虫分离株及耐氯喹的W2克隆株的体外活性。采用不同类型的RPMI 1640培养基并设置不同孵育期进行体外试验。与使用不含叶酸和对氨基苯甲酸的RPMI培养基相比，使用标准RPMI培养基或含有低浓度叶酸和对氨基苯甲酸的RPMI培养基会提高环氯胍和乙胺嘧啶的50%抑制浓度。叶酸和对氨基苯甲酸的浓度不影响氯胍和氯喹的体外活性。然而，将孵育期从42小时延长至66小时会降低所有受试化合物的50%抑制浓度。氯喹与氯胍或环氯胍之间的体外弱拮抗作用似乎对氯喹-氯胍联合用药的体内疗效没有任何影响。
