Geary T G, Jensen J B
J Parasitol. 1983 Feb;69(1):97-105.
The potencies of 10 quinoline-containing antimalarials, including chloroquine, amodiaquine, CM-2,999-2K, quinine, mefloquine, SN-6911, SN-11875, SN-12108, SN-12308, and SN-12309, were determined in vitro against five strains of Plasmodium falciparum characterized in vivo and in vitro by various degrees of sensitivity to chloroquine. These strains included the chloroquine-sensitive strains Honduras and FCC1, and R1-resistant line FCR3TC, and the R3-resistant strains FCR1 and Viet Nam Smith (VNS). The potency of chloroquine varied 100-fold in these strains, with minimum inhibitory concentrations (MIC) ranging from 3.2 X 10(-9) M in FCC1 to 3.2 X 10(-7) M in FCR1. The other drugs had different patterns; SN-12108 had an MIC of 3.2 X 10(-9) M in FCC1, Honduras, and FCR1, and 3.2 X 10(-8) M in VNS. However, SN-6911 (3-methylchloroquine), amodiaquine, and mefloquine showed little or no variation in potency among these strains. There was no correlation between sensitivity to chloroquine and any other drug. This lack of cross-resistance in vitro must be taken into account in consideration of theories of chloroquine action in these parasites.
测定了10种含喹啉的抗疟药的效力，包括氯喹、氨酚喹、CM - 2,999 - 2K、奎宁、甲氟喹、SN - 6911、SN - 11875、SN - 12108、SN - 12308和SN - 12309，它们在体外对5株恶性疟原虫的效力，这些菌株在体内和体外对氯喹具有不同程度的敏感性。这些菌株包括氯喹敏感株洪都拉斯株和FCC1株，R1抗性株FCR3TC，以及R3抗性株FCR1和越南史密斯株（VNS）。氯喹在这些菌株中的效力相差100倍，最低抑菌浓度（MIC）范围从FCC1株中的3.2×10⁻⁹ M到FCR1株中的3.2×10⁻⁷ M。其他药物有不同的模式；SN - 12108在FCC1株、洪都拉斯株和FCR1株中的MIC为3.2×10⁻⁹ M，在VNS株中的MIC为3.2×10⁻⁸ M。然而，SN - 6911（3 - 甲基氯喹）、氨酚喹和甲氟喹在这些菌株中的效力几乎没有变化或没有变化。对氯喹的敏感性与任何其他药物之间没有相关性。在考虑氯喹对这些寄生虫的作用理论时，必须考虑到这种体外缺乏交叉抗性的情况。
