青蒿素类衍生物抗肿瘤研究进展

青蒿素类药物是很好的抗疟药物,近年来大量体内、外研究显示青蒿素具有良好的抗肿瘤活性。大多数肿瘤细胞表面有高浓度的转铁蛋白受体,因此与正常细胞相比,细胞内含有更多的亚铁离子,青蒿素与亚铁离子反应生成自由基,可以选择性的杀伤肿瘤细胞。G1期细胞的转铁蛋白受体表达和铁离子摄入都显著增多,青蒿素类药物在此期诱导细胞凋亡,其具体作用靶点和机制还有待进一步研究,青蒿素衍生物还具有抗肿瘤血管生成活性。将青蒿素类药物与转铁蛋白上的糖基共价结合的复合体,可以将铁离子和青蒿素同时摄入肿瘤细胞,增强了青蒿素的高效性和靶向性。

Current status of artemisinin derivatives anticancer properties

Artemisinin and its derivatives are well known antimalaria drugs.In recent years,there are a lot of reports of artemisinins about it’s anticancer activities in vitro and in vivo,and it have had some experiences in clininal.There are more transferrin receptors on tumor cell surface than normal l human cells,so there are more iron in the tumor cells.artemisinins react with iron to generate free radicals,and free radicals kills the tumor cells.Transferrin receptors express more and uptake more iron during the G1 phase,so artemisinins induces apoptosis mainly during this phase,it also has the antiangiogenic effect.Tagging artemisinin to transferrin,both iron and artemisinin would be transported into cancer cells in one package.This would enhance the toxicity and selectivity of artemisinin towards cancer cells.