Department of Bioengineering, University of Washington, Box 355061, Seattle, WA 98195, USA.
Invest New Drugs. 2013 Feb;31(1):230-46. doi: 10.1007/s10637-012-9873-z. Epub 2012 Aug 31.
Artemisinin contains an endoperoxide moiety that can react with iron to form cytotoxic free radicals. Cancer cells contain significantly more intracellular free iron than normal cells and it has been shown that artemisinin and its analogs selectively cause apoptosis in many cancer cell lines. In addition, artemisinin compounds have been shown to have anti-angiogenic, anti-inflammatory, anti-metastasis, and growth inhibition effects. These properties make artemisinin compounds attractive cancer chemotherapeutic drug candidates. However, simple artemisinin analogs are less potent than traditional cancer chemotherapeutic agents and have short plasma half-lives, and would require high dosage and frequent administration to be effective for cancer treatment. More potent and target-selective artemisinin-compounds are being developed. These include artemisinin dimers and trimers, artemisinin hybrid compounds, and tagging of artemisinin compounds to molecules that are involved in the intracellular iron-delivery mechanism. These compounds are promising potent anticancer compounds that produce significantly less side effect than traditional chemotherapeutic agents.
青蒿素含有一个内过氧化物部分，可以与铁反应形成细胞毒性自由基。癌细胞内的游离铁含量明显高于正常细胞，已证明青蒿素及其类似物能选择性地导致许多癌细胞系凋亡。此外，青蒿素化合物已被证明具有抗血管生成、抗炎、抗转移和生长抑制作用。这些特性使青蒿素化合物成为有吸引力的癌症化学治疗候选药物。然而，简单的青蒿素类似物的效力不如传统的癌症化学治疗药物，并且血浆半衰期短，为了对癌症治疗有效，需要高剂量和频繁给药。更有效和靶向选择性的青蒿素化合物正在开发中。这些包括青蒿素二聚体和三聚体、青蒿素杂合化合物，以及将青蒿素化合物标记到参与细胞内铁输送机制的分子上。这些化合物是很有前途的强效抗癌化合物，与传统化学治疗药物相比，产生的副作用明显更少。
