Woerdenbag H J, Lugt C B, Pras N
Department of Pharmacognosy, University of Groningen, The Netherlands.
Pharm Weekbl Sci. 1990 Oct 19;12(5):169-81. doi: 10.1007/BF01980041.
Artemisia annua L. contains artemisinin, an endoperoxide sesquiterpene lactone, mainly in its leaves and inflorescences. This compound and a series of derivatives have attracted attention because of their potential value as antimalarial drugs. In this review a survey of the currently available literature data is given. It includes phytochemical aspects, such as constituents of A. annua, the artemisinin content during the development of the plant and its biosynthesis, isolation, analysis and stability. Total chemical synthesis of artemisinin is referred to, as well as structure-activity relationships of derivatives and simplified analogues. Pharmacological studies are summarized, including the mechanism of action, interaction of the antimalarial activity with other drugs, possible occurrence of resistance to artemisinin, clinical results, toxicological aspects, metabolism and pharmacokinetics. Finally, plant cell biotechnology is mentioned as a possible means to obtain plants and cell cultures with higher artemisinin contents, allowing an industrial production of pharmaceuticals containing this novel drug.
黄花蒿主要在其叶片和花序中含有青蒿素，一种内过氧化物倍半萜内酯。该化合物及其一系列衍生物因其作为抗疟药物的潜在价值而受到关注。在这篇综述中，给出了对当前可用文献数据的调查。它包括植物化学方面，如黄花蒿的成分、植物生长过程中青蒿素的含量及其生物合成、分离、分析和稳定性。还提到了青蒿素的全化学合成以及衍生物和简化类似物的构效关系。总结了药理学研究，包括作用机制、抗疟活性与其他药物的相互作用、对青蒿素可能产生的耐药性、临床结果、毒理学方面、代谢和药代动力学。最后，提到了植物细胞生物技术，作为获得青蒿素含量更高的植物和细胞培养物的一种可能手段，从而实现含这种新药的药物的工业化生产。
