THE INTERACTION OF ARTEMISININ WITH MALARIAL HEMOZOIN
THE INTERACTION OF ARTEMISININ WITH MALARIAL HEMOZOIN
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DOI：
10.1016/0166-6851(94)90014-0
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发表时间：
1994-01-01
影响因子：
1.5
通讯作者：
MESHNICK, SR
中科院分区：
文献类型：
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作者：
HONG, YL;YANG, YZ;MESHNICK, SR
[C-14]青蒿素在培养过程中被恶性疟原虫吸收，在血色素中被浓缩。在体外，血红素和青蒿素发生化学反应，形成两种主要产物，并通过高效液相色谱（HPLC）分离得到。两种产品的m/z值分别为856和871。从青蒿素处理过的寄生虫中分离得到的血色素的薄层色谱和高效液相色谱分析表明，大部分血色素相关的放射性与合成的加合物相结合。当[C-14]青蒿素与分离的血色素孵育时，[C-14]青蒿素以时间依赖性的方式从溶液中消失。在处理过的血色素中存在的一些放射性也与TLC上的加合物相结合。因此，在体外和原位实验中，青蒿素似乎与疟原虫色素中的血红素发生共价反应。
[C-14]Artemisinin was taken up by Plasmodium falciparum in culture and concentrated in hemozoin. In vitro, hemin and artemisinin were found to undergo a chemical reaction forming two major products which were isolated by highperformance liquid chromatography (HPLC). The m/z values of the two products were 856 and 871. Thin-layer chromatography (TLC) and HPLC of hemozoin isolated from [C-14]artemisinin-treated parasites showed that the majority of the hemozoin-associated radioactivity comigrated with the synthetic adducts. When [C-14]artemisinin was incubated with isolated hemozoin, [C-14]artemisinin disappeared from the solution in a time-dependent manner. Some of the radioactivity present in the treated hemozoin also comigrated with the adducts on TLC. Thus, artemisinin appears to react covalently with heme in malaria hemozoin both in vitro and in situ.