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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
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Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.

机译：螺-和二螺-1,2,4-三氧戊环抗疟药的抗疟活性和血红素烷基化之间的关系。

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摘要

The reaction of spiro- and dispiro-1,2,4-trioxolane antimalarials with heme has been investigated to provide further insight into the mechanism of action for this important class of antimalarials. A series of trioxolanes with various antimalarial potencies was found to be unreactive in the presence of Fe(III) hemin, but all were rapidly degraded by reduced Fe(II) heme. The major reaction product from the heme-mediated degradation of biologically active trioxolanes was an alkylated heme adduct resulting from addition of a radical intermediate. Under standardized reaction conditions, a correlation (R2 = 0.88) was found between the extent of heme alkylation and in vitro antimalarial activity, suggesting that heme alkylation may be related to the mechanism of action for these trioxolanes. Significantly less heme alkylation was observed for the clinically utilized artemisinin derivatives compared to the equipotent trioxolanes included in this study.
机译：已对螺-和螺-1,2,4-三氧戊环抗疟药与血红素的反应进行了研究，以进一步了解这一重要抗疟药的作用机理。发现在具有Fe（III）血红素的情况下，一系列具有不同抗疟疾效力的三氧戊环不具有反应性，但均被还原的Fe（II）血红素迅速降解。来自血红素介导的生物活性三氧杂环戊烷降解的主要反应产物是烷基化血红素加合物，其是通过添加自由基中间体而产生的。在标准化反应条件下，血红素烷基化程度与体外抗疟活性之间存在相关性（R2 = 0.88），这表明血红素烷基化可能与这些三氧戊酮的作用机理有关。与本研究中包括的等价三氧戊环相比，临床上使用的青蒿素衍生物的血红素烷基化显着减少。

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