青蒿素（青蒿琥酯）：细胞内血红素在其抗疟作用机制中的作用。

Artemisinin (qinghaosu): the role of intracellular hemin in its mechanism of antimalarial action.

作者信息

Meshnick S R, Thomas A, Ranz A, Xu C M, Pan H Z

机构信息

Department of Microbiology, City University of New York Medical School, City College, New York 10031.

出版信息

Mol Biochem Parasitol. 1991 Dec;49(2):181-9. doi: 10.1016/0166-6851(91)90062-b.

DOI:10.1016/0166-6851(91)90062-b

PMID:1775162

Abstract

Artemisinin (qinghaosu), is a promising new antimalarial drug derived from an ancient Chinese herbal remedy. When [13-14C]artemisinin is added to cultures of Plasmodium falciparum, it is converted into a product with different solubility and chromatographic properties than the parent drug. Artemisinin reacts with hemin in aqueous solution to form an adduct with an apparent molecular weight of 914 which has identical chromatographic, solubility, and electrophoretic behavior to the parasite-derived product. The reaction between artemisinin and hemin, when carried out in the presence of red cell membranes, leads to the oxidation of protein thiols. Malarial parasites are rich in hemin; artemisinin's reactivity toward hemin may explain its selective toxicity to malarial parasites.

摘要

青蒿素（青蒿琥酯）是一种有前景的新型抗疟药物，源自一种古老的中国草药疗法。当将[13 - 14C]青蒿素添加到恶性疟原虫培养物中时，它会转化为一种与母体药物相比具有不同溶解度和色谱性质的产物。青蒿素在水溶液中与血红素反应形成一种表观分子量为914的加合物，该加合物具有与寄生虫衍生产物相同的色谱、溶解度和电泳行为。当在红细胞膜存在的情况下进行青蒿素与血红素之间的反应时，会导致蛋白质硫醇的氧化。疟原虫富含血红素；青蒿素对血红素的反应性可能解释了其对疟原虫的选择性毒性。