二甲胺四环素体外抗甲氟喹、氯喹和乙胺耐药恶性疟原虫的作用

Q. Lin, K. Katakura, M. Oue, S. Kano, Mamoru Suzuki
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引用次数: 6

摘要

四环素因其安全的药物作用而被用于预防疟疾和治疗耐药恶性疟疾。我们在体外重新评估了三种四环素类药物对耐药恶性疟原虫的作用。二甲胺四环素对恶性疟原虫体外生长的抑制作用分别比四环素和强力霉素强约4倍和2倍。与多西环素相比,米诺环素对氯喹、乙胺嘧啶和甲氟喹耐药恶性疟原虫有明显的体外抑制作用。在二甲胺四环素处理的寄生虫细胞质中,电镜观察到许多具有单一膜结合的电子致密囊泡,尽管线粒体没有明显的结构改变。米诺环素可能是一种比强力霉素更好的治疗药物,强力霉素被广泛强调为标准的抗疟疾四环素。
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Effects of Minocycline against Mefloquine-, Chloroquine- and Pyrimethamine-resistant Plasmodium falciparum in vitro.
Tetracyclines are used for prophylaxis of malaria and treatment of drug-resistant falciparum malaria because of their safe drug action. We re-evaluated effects of three tetracyclines against drug-resistant Plasmodium falciparum in vitro. Minocycline was approximately 4 times and twice more potent in inhibiting the in vitro growth of falciparum parasites than tetracycline and doxycycline, respectively. Compared with doxycycline, significant inhibitory effects of minocycline to chloroquine, pyrimethamine and mefloquine resistant P. falciparum strains were affirmed by the present in vitro study. By electron microscopy a number of electron dense vesicles with a single membrane bound were observed in the cytoplasm of minocycline-treated parasites, although no distinct structural alternations of mitochondria was noted. Minocycline may be a better therapeutic drug than doxycycline which is widely accented as the standard antimalarial tetracycline.
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