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高铁原卟啉IX与抗疟内过氧化物青蒿琥酯之间的反应产生了一种具有增强氧化还原催化活性的中间物种。

Reaction between ferriprotoporphyrin IX and the antimalarial endoperoxide artesunate gives an intermediate species with enhanced redox catalytic activity.

作者信息

Adams P A, Berman P A

机构信息

Department of Chemical Pathology, University of Cape Town Medical School, South Africa.

出版信息

J Pharm Pharmacol. 1996 Feb;48(2):183-7. doi: 10.1111/j.2042-7158.1996.tb07119.x.

Abstract

The kinetics of the reaction between ferri(Fe(III) protoporphyrin IX (haemin) and the potent sesquiterpene endoperoxide antimalarial artesunate are shown to be consistent with a three-step, two-intermediate mechanism, with the final product possessing a degraded tetrapyrrole ring system. Microscopic rate constants for the mechanism have been evaluated. The redox catalytic capability of the haem artesunate complex is shown to be approximately fourfold that of haemin alone, suggesting a possible mechanism of action of the drug.

摘要

已表明,高铁(Fe(III))原卟啉IX(血红素)与强效倍半萜内过氧化物抗疟药青蒿琥酯之间反应的动力学符合一个包含三个步骤、两个中间体的机制,最终产物具有降解的四吡咯环系统。已评估了该机制的微观速率常数。血红素青蒿琥酯复合物的氧化还原催化能力约为单独血红素的四倍,这表明了该药物可能的作用机制。

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