THE EFFECT OF ARTEMISININ, ITS DERIVATIVES AND MEFLOQUINE AGAINST CHLOROQUINE-RESISTANT STRAINS OF PLASMODIUM-FALCIPARUM INVITRO
THE EFFECT OF ARTEMISININ, ITS DERIVATIVES AND MEFLOQUINE AGAINST CHLOROQUINE-RESISTANT STRAINS OF PLASMODIUM-FALCIPARUM INVITRO
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DOI：
10.1016/0035-9203(92)90220-7
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发表时间：
1992-07-01
影响因子：
2.2
通讯作者：
ASHTON, M
中科院分区：
文献类型：
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作者：
ALIN, MH;BJORKMAN, A;ASHTON, M
用青蒿素、双氢青蒿素、蒿甲醚、甲氟喹和氯喹对3株抗氯喹恶性疟原虫泰国株K1、T996株和印度LS21株进行了48h的体外药效试验。一个S型的EM。模型适用于每种药物和菌株组合的所有体外抑制数据。菌株Ki和LS21对氯喹有很强的抗性，而T996对氯喹有部分抗性。青蒿素、双氢青蒿素和蒿甲醚对所有菌株均有抑制作用，在10~(-7)M时完全抑制生长，青蒿素和双氢青蒿素的半数有效浓度(EC50)分别为0~57~1.6 nm和0.36~3.1 nm，青蒿素对3个菌株的EC50为1.5~6.1 nm。甲氟喹的EC50值为46~185 nm。在较高浓度下，菌株K1和LS21被完全抑制，而菌株T996即使在最高浓度1.28×10~(-6)M时也不能完全抑制。
A 48 h in vitro test of the efficacy of artemisinin, dihydroartemisinin, artemether, mefloquine and chloroquine was carried out against 3 chloroquine-resistant strains of Plasmodium falciparum, strains K1 and T996 from Thailand and LS21 from India. A sigmoid Em. model was fitted to all in vitro inhibition data for each combination of drug and strain. Strains KI and LS21 were strongly resistant to chloroquine, whereas T996 was partially resistant. Artemisinin, dihydroartemisinin and artemether were active against all strains, with complete growth inhibition at 10(-7) M. Artemether and dihydroartemisinin were both more potent than artemisinin, with 50% effective (EC50) values of 0-57-1.6 nM and 0.36-3.1 nm respectively; the EC50 of artemisinin was 1.5-6.1 nm for the 3 strains. The EC50 values for mefloquine were 46-185 nM. At higher concentrations, strains K1 and LS21 were fully inhibited, while with strain T996 mefloquine did not fully inhibit even at the highest concentration, 1.28 X 10(-6) M. It is concluded that artemisinin and its derivatives were highly effective against the 3 chloroquine-resistant strains, one of which showed borderline resistance to mefloquine.