青蒿素及其衍生物和咯萘啶对不同恶性疟原虫株的体外活性。
In vitro activity of artemisinin, its derivatives, and pyronaridine against different strains of Plasmodium falciparum.
作者信息
Alin M H, Björkman A, Ashton M
机构信息
Department of Morphology and Pathology, Faculty of Medicine, Somali National University, Mugadishu.
出版信息
Trans R Soc Trop Med Hyg. 1990 Sep-Oct;84(5):635-7. doi: 10.1016/0035-9203(90)90129-3.
The activities of artemisinin (qinghaosu), dihydroartemisinin (dihydroqinghaosu), artemether and pyronaridine were tested in a 48 h in vitro assay against 3 chloroquine-sensitive and one chloroquine-resistant strains of Plasmodium falciparum. Growth inhibition was modelled with a sigmoid Emax model. All compounds markedly inhibited the growth of all strains although, for the chloroquine-resistant strain, merozoites were detected at concentrations as high as 10(-4) M of artemisinin, dihydroartemisinin and artemether. Dihydroartemisinin, artemether and pyronaridine appeared to be more potent than artemisinin, with EC50 values of 4.7-23 nM, 0.98-6.1 nM and 4.4-18 nM respectively, while the EC50 value of artemisinin was 3-108 nM against all 4 strains.
在一项48小时的体外试验中，测试了青蒿素（青蒿素）、双氢青蒿素（双氢青蒿素）、蒿甲醚和咯萘啶对3株氯喹敏感和1株氯喹耐药的恶性疟原虫菌株的活性。用S形Emax模型模拟生长抑制情况。所有化合物均显著抑制所有菌株的生长，不过，对于氯喹耐药菌株，在青蒿素、双氢青蒿素和蒿甲醚浓度高达10(-4)M时仍检测到裂殖子。双氢青蒿素、蒿甲醚和咯萘啶似乎比青蒿素更有效，其EC50值分别为4.7 - 23 nM、0.98 - 6.1 nM和4.4 - 18 nM，而青蒿素对所有4株菌株的EC50值为3 - 108 nM。
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