咯萘啶、甲氟喹和奎宁对青蒿琥酯敏感株与抗性株恶性疟原虫的体外作用

EFFECT OF PYRONARIDINE, MEFLOQUINE AND QUININE ON ARTESUNATE-SENSITIVE AND ARTESUNATE-RESISTANT PLASMODIUM FALCIPARUM

[目的 ]比较青蒿琥酯敏感株与抗性株恶性疟原虫对咯萘啶、甲氟喹和奎宁的敏感性 ;了解这 3种药物与青蒿琥酯伍用对抗青蒿琥酯恶性疟原虫的体外抗疟作用。 [方法 ]应用Rieckmann体外微量法测定敏感株与抗性株原虫对上述 4种药物的敏感性 ,同时测定青蒿琥酯分别与咯萘啶、甲氟喹、奎宁伍用对抗性株原虫的敏感性。 [结果 ]咯萘啶、甲氟喹、奎宁和青蒿琥酯对敏感株的ID5 0 分别为 5 9 0、 6 9 7、 2 83 8和 9 6nmo1/L ;对抗性株的ID5 0 依次为 170 6、 6 3 2、 2 72 4及 85 1nmo1/L。咯萘啶与青蒿琥酯伍用 ,其ID5 0 分别为两药单用组的 1/4 7(36 6 / 170 6 )和 1/ 3 7(2 2 8/ 85 1)。甲氟喹与青蒿琥酯伍用中 ,其ID95 分别为两药单用组的 1/ 4(40 / 16 0 )和 1/ 12 5 (3 2 / 40 0 )。奎宁与青蒿琥酯伍用 ,其ID95 分别为单用组的 1/ 16 (80 / 12 80 )和 1/ 12 5 (3 2 / 40 0 )。 [结论 ]抗青蒿琥酯恶性疟原虫对甲氟喹和奎宁无交叉抗性 ,这两种药物分别与青蒿琥酯伍用 ,对抗青蒿琥酯恶性疟原虫有较明显增效作用。

Objective] To compare the sensitivity of artesunate sensitive and artesunate resistant P falciparum to pyronaridine,mefloquine and quinine and to understand the effect of artesunte combined with the above mentioned 3 drugs respectively on artesunate resistant P falciparum . [Methods] Rieckmanns in vitro miorotechnique was used. [Results] The ID 50 values of pyronaride,mefloquine, quinine and artesunate were 59 0, 69 7, 283 8 and 9 6 nmol/L to artesunate sensitive P falciparum ;the ID 50 of the 4 drugs mentioned above were 170 6, 63 2, 272 4 and 85 1 nmol/L to the artesunate resistant P falciparum , respectively. In artesunate pyronaridine combinaton, the ID 50 values were 1/3 7 (22 8/85 1) and 1/4 7 (36 6/170 6) of the 2 drugs singly used.In artesunate mefloquine combinaton,the ID 95 is 1/125 (3 2/400) and 1/16 (80/128) of the 2 drugs singly used, respectively. [Conclusion] The artesunate resistant P falciparum isolate has no cross resistance to mefloquine and quinine.When artesunate was used in combination with the 2 drugs mentioned above respectively,the efficacy proved to be enhanced.