Antibiotics for prophylaxis of Plasmodium falciparum infections:: In vitro activity of doxycycline against Senegalese isolates
Antibiotics for prophylaxis of Plasmodium falciparum infections:: In vitro activity of doxycycline against Senegalese isolates
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DOI：
10.4269/ajtmh.2000.62.82
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发表时间：
2000-01-01
影响因子：
3.3
通讯作者：
Parzy, D
中科院分区：
文献类型：
--
作者：
Pradines, B;Spiegel, A;Parzy, D
多西环素，氯喹，奎宁，阿莫地喹，蒿甲醚，乙胺嘧啶，和环胍的体外活性进行了评价，对恶性疟原虫分离株从塞内加尔（Dielmo和Ndiop），使用同位素，微量，药物敏感性试验。多西环素的71个50%抑制浓度（IC_（50））值的范围为0.7 - 108.0 μ M，71个分离株的几何平均IC_（50）为11.3 μ M（95%置信区间= 9.5-13.4 μ M）。多西环素活性在氯喹敏感株和抗性株间差异不显著（P = 0.0858）。有没有在体外的反应之间的相关性，强力霉素和蒿甲醚，氯喹，奎宁，阿莫地喹，乙胺嘧啶，和环胍，这表明在体外这些药物之间没有交叉耐药。延长暴露时间可增加效力。96小时孵育。多西环素的活性比48小时温育中增加4-5倍。多西环素对多药耐药恶性疟原虫红细胞内期的体外活性、其对红细胞前型的作用、恶性疟原虫对多西环素和醚类抗疟药的体外反应之间缺乏相关性以及其最初的潜在作用位点是有利于其用作抗疟药的因素。
The in vitro activities of doxycycline, chloroquine, quinine, amodiaquine, artemether, pyrimethamine, and cycloguanil were evaluated against Plasmodium falciparum isolates from Senegal (Dielmo and Ndiop), using an isotopic, micro, drug susceptibility test. The 71 50% inhibitory concentration (IC,,) values for doxycycline ranged from 0.7 to 108.0 mu M and the geometric mean IC50 for the 71 isolates was 11.3 mu M (95% confidence interval = 9.5-13.4 mu M). The activity of doxycycline did not differ significantly (P = 0.0858) between the chloroquine-susceptible isolates and the chloroquine-resistant isolates. There was no in vitro correlation between the responses to doxycycline and those to artemether, chloroquine, quinine, amodiaquine, pyrimethamine, and cycloguanil, suggesting no in vitro cross-resistance among these drugs. Potency was increased by prolonged exposure. In 96-hr incubations. the activity of doxycycline was 4-5-fold more increased than in 48-hr incubations. The in vitro activity of doxycycline against intraerythrocytic stages of multidrug-resistant P. falciparum, its: action against the preerythrocytic forms, the lack of correlation between the responses in vitro of P. falciparum to doxycycline and the ether antimalarial drugs, and its original potential site of action are factors that favor its use as antimalarial drug.