青蒿素类化合物是一类重要的抗疟疾药物，对大部分肿瘤细胞也有抑制作用，但对人正常组织细胞影响较小。研究表明，青蒿素作为前药被激活后的抗肿瘤效果更好。关于青蒿素的激活因素，目前的研究主要围绕亚铁离子、血红素和线粒体，但仍存在争议，不确定的激活因子使青蒿素在抗肿瘤方面的研究陷入瓶颈。总结了青蒿素类化合物在肿瘤细胞内相关激活因子的研究进展，包括对激活因子组成和功能的介绍，为深入研究青蒿素抗肿瘤作用机制提供依据和借鉴。

Artemisinin compounds are an important class of antimalarial drug showing significant antitumor activity with little side effect on normal cells in human. Studies have shown that artemisinin presents an increased antitumor effect after being activated as a prodrug. Regarding to the activation factor of artemisinin, the majority of current studies are focusing on Fe²⁺, heme and mitochondria. However, controversies still existed. The uncertain activation factors obstacle the development and further antitumor research of artemisinin. The activation factors of artemisinin in tumor cells, including the introduction of their composition and function are summarized in this article, which provide basis and reference for in-depth study of the anti-tumor mechanism of artemisinin.

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