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啮齿动物疟疾的化疗。LVI. 对天然和合成内过氧化物耐药性发展的研究。

The chemotherapy of rodent malaria. LVI. Studies on the development of resistance to natural and synthetic endoperoxides.

作者信息

Peters W, Robinson B L

机构信息

CABI Bioscience, St. Albans, U.K.

出版信息

Ann Trop Med Parasitol. 1999 Jun;93(4):325-9. doi: 10.1080/00034989958320.

DOI:10.1080/00034989958320
PMID:10656034
Abstract

Chloroquine-sensitive Plasmodium berghei N and chloroquine-resistant P. yoelii ssp. NS were exposed to selection pressure, in the '2% relapse technique', from artemisinin, artesunate, a bicyclic, synthetic endoperoxide Ro 41-3823 (an analogue of arteflene) or Fenozan B07, a synthetic 1,2,4-trioxane endoperoxide. Whereas resistance against artemisinin did develop to a moderate level in both parasites, only a low level of resistance or none developed to the other compounds, and resistant parasites readily lost resistance once drug-selection pressure was withdrawn. The relevance of these observations and the experience of other investigators are discussed in relation to the possible risk that resistance may be developed in nature once endoperoxides are deployed widely against multidrug-resistant P. falciparum.

摘要

对氯喹敏感的伯氏疟原虫N株和对氯喹耐药的约氏疟原虫NS株,在“2%复发技术”中受到来自青蒿素、青蒿琥酯、一种双环合成内过氧化物Ro 41 - 3823(蒿甲醚的类似物)或芬诺赞B07(一种合成的1,2,4 - 三恶烷内过氧化物)的选择压力。虽然两种寄生虫对青蒿素都产生了一定程度的耐药性,但对其他化合物仅产生了低水平的耐药性或未产生耐药性,而且一旦撤去药物选择压力,耐药寄生虫很容易失去耐药性。结合一旦内过氧化物广泛用于对抗多重耐药恶性疟原虫可能在自然界产生耐药性的潜在风险,讨论了这些观察结果及其他研究者经验的相关性。

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