青蒿素与抗疟内过氧化物：从草药疗法到靶向化疗
Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy.
作者信息
Meshnick S R, Taylor T E, Kamchonwongpaisan S
机构信息
Department of Epidemiology, University of Michigan School of Public Health, Ann Arbor 48109-2029, USA.
出版信息
Microbiol Rev. 1996 Jun;60(2):301-15. doi: 10.1128/mr.60.2.301-315.1996.
Abstract
Artemisinin and its derivatives are endoperoxide-containing compounds which represent a promising new class of antimalarial drugs. In the presence of intraparasitic iron, these drugs are converted into free radicals and other electrophilic intermediates which then alkylate specific malaria target proteins. Combinations of available derivatives and other antimalarial agents show promise both as first-line agents and in the treatment of severe disease.
摘要
青蒿素及其衍生物是含内过氧化物的化合物，是一类很有前景的新型抗疟药物。在疟原虫体内铁的存在下，这些药物会转化为自由基和其他亲电中间体，然后使特定的疟疾靶蛋白烷基化。现有衍生物与其他抗疟药物的联合使用，作为一线药物以及用于重症疾病的治疗都显示出前景。
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本文引用的文献
1
Protection against malaria by thalassaemia and haemoglobin variants.
Parasitol Today. 1993 Jul;9(7):241-5. doi: 10.1016/0169-4758(93)90065-n.
2
The chemotherapy of rodent malaria. L. The activities of some synthetic 1,2,4-trioxanes against chloroquine-sensitive and chloroquine-resistant parasites. Part 3: Observations on 'Fenozan-50F', a difluorinated 3,3'-spirocyclopentane 1,2,4-trioxane.啮齿动物疟疾的化疗。L. 某些合成1,2,4-三恶烷对氯喹敏感和氯喹抗性寄生虫的活性。第3部分：对二氟化3,3'-螺环戊烷1,2,4-三恶烷“Fenozan-50F”的观察
Ann Trop Med Parasitol. 1993 Apr;87(2):111-23. doi: 10.1080/00034983.1993.11812745.
3
Syntheses and antimalarial activities of N-substituted 11-azaartemisinins.N-取代11-氮杂青蒿素的合成及其抗疟活性
J Med Chem. 1995 Dec 22;38(26):5045-50. doi: 10.1021/jm00026a012.
4
Molecular modeling studies of the artemisinin (qinghaosu)-hemin interaction: docking between the antimalarial agent and its putative receptor.青蒿素（青蒿琥酯）与血红素相互作用的分子模拟研究：抗疟药物与其假定受体之间的对接
J Mol Graph. 1995 Aug;13(4):215-22. doi: 10.1016/0263-7855(94)00001-9.
5
Iron-dependent free radical generation from the antimalarial agent artemisinin (qinghaosu).抗疟药物青蒿素（青蒿琥酯）产生的铁依赖性自由基生成。
Antimicrob Agents Chemother. 1993 May;37(5):1108-14. doi: 10.1128/AAC.37.5.1108.
6
Effects of qinghaosu (artemisinin) and its derivatives on experimental cutaneous leishmaniasis.青蒿素及其衍生物对实验性皮肤利什曼病的影响。
Parasitology. 1993 Jan;106 ( Pt 1):7-11. doi: 10.1017/s0031182000074758.
7
Treatment of malaria in Vietnam with oral artemisinin.
Am J Trop Med Hyg. 1993 Mar;48(3):398-402.
8
Plasmodium falciparum: in vitro studies of the pharmacodynamic properties of drugs used for the treatment of severe malaria.恶性疟原虫：用于治疗重症疟疾的药物的药效学特性的体外研究
Exp Parasitol. 1993 Feb;76(1):85-95. doi: 10.1006/expr.1993.1010.
9
In vitro activity of artemisinin derivatives against African isolates and clones of Plasmodium falciparum.青蒿素衍生物对恶性疟原虫非洲分离株和克隆株的体外活性。
Am J Trop Med Hyg. 1993 Sep;49(3):301-7. doi: 10.4269/ajtmh.1993.49.301.
10
Studies on chemotherapy of parasitic helminths: efficacy of artemether on Japanese strain of Schistosoma japonicum in mice.寄生虫化疗研究：蒿甲醚对日本血吸虫日本株小鼠的疗效。
Southeast Asian J Trop Med Public Health. 1993 Mar;24(1):53-6.
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