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柬埔寨恶性疟原虫分离株对卤泛群、咯萘啶和青蒿素衍生物的体外敏感性

In vitro susceptibility of Cambodian isolates of Plasmodium falciparum to halofantrine, pyronaridine and artemisinin derivatives.

作者信息

Basco L K, Le Bras J

机构信息

Centre National de Référence pour la Chimiosensibilité du Paludisme, Hôpital Bichat-Claude Bernard, Paris, France.

出版信息

Ann Trop Med Parasitol. 1994 Apr;88(2):137-44. doi: 10.1080/00034983.1994.11812851.

DOI:10.1080/00034983.1994.11812851
PMID:8067809
Abstract

Multidrug-resistant Plasmodium falciparum is widespread in Cambodia. The in vitro susceptibilities of 14 Cambodian isolates to chloroquine, quinine, mefloquine, halofantrine, pyrimethamine, cycloguanil, pyronaridine, artemisinin, arteether, artemether and artelinate were studied using a semi-microtest on day 0 and after 15-30 days of culture. The culture-adapted isolates were all resistant to chloroquine, pyrimethamine and cycloguanil. The susceptibility to quinine was generally low. Three isolates were resistant to mefloquine. A comparison of susceptibility to cycloguanil, quinine, and mefloquine prior to and after culture adaptation showed a trend toward a higher resistance level in some isolates. Halofantrine, pyronaridine and artemisinin derivatives were highly active against the multidrug-resistant Cambodian isolates, with very similar 50% inhibitory concentrations (IC50). These results confirm the presence of multidrug-resistant P. falciparum isolates in Cambodia and indicate that quinine- and mefloquine-resistant populations of the parasite may already exist in the field. The high in vitro activities of halofantrine, pyronaridine and artemisinin derivatives indicate their potential usefulness for the treatment of multidrug-resistant malaria.

摘要

耐多药恶性疟原虫在柬埔寨广泛存在。采用半微量试验,研究了14株柬埔寨分离株在培养第0天以及培养15 - 30天后对氯喹、奎宁、甲氟喹、卤泛群、乙胺嘧啶、环氯胍、咯萘啶、青蒿素、蒿乙醚、蒿甲醚和青蒿琥酯的体外敏感性。适应培养后的分离株均对氯喹、乙胺嘧啶和环氯胍耐药。对奎宁的敏感性普遍较低。3株分离株对甲氟喹耐药。比较培养适应前后对环氯胍、奎宁和甲氟喹的敏感性发现,部分分离株有耐药水平升高的趋势。卤泛群、咯萘啶和青蒿素衍生物对耐多药柬埔寨分离株具有高活性,50%抑制浓度(IC50)非常相似。这些结果证实柬埔寨存在耐多药恶性疟原虫分离株,并表明该寄生虫的耐奎宁和耐甲氟喹群体可能已在野外存在。卤泛群、咯萘啶和青蒿素衍生物的高体外活性表明它们在治疗耐多药疟疾方面具有潜在用途。

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