青蒿素及其衍生物的抗肿瘤研究进展

Progress of anti-tumor activities of artemisinin and its derivatives

青蒿素及其半合成衍生物(ARTs)是一类有效的抗疟药物。最近研究显示,ARTs具有抗癌作用,其主要机制是产生活性氧、诱导细胞凋亡、抑制血管生成和阻滞细胞周期等。ARTs能抑制实体肿瘤的生长,表明其可用于抗肿瘤新辅助疗法中。双氢青蒿素和青蒿琥酯在体内实验中对乳腺、肺、胰腺和神经胶质瘤癌细胞有很好的化疗效果,提示其可用于联合抗癌疗法中。现就ARTs的抗癌机制以及其作为抗癌剂的疗效、安全性和剂量范围等方面做一总结。

Artemisinin and its derivatives(ARTs) are a group of effective antimalarial drugs. Recent studies have shown that artemisinin and its derivatives(ARTs) have anti-cancer effects through the production of reactive oxygen species, induction of apoptosis, inhibition of angiogenesis and cell cycle. ARTs can inhibit the growth of solid tumors, suggesting their application in a neoadjuvant therapy. Dihydroartemisinin and artesunate exhibit chemosensitizing effects in vivo on cancer cells of breast, lung, pancreas and glioma, suggesting the use of ARTs in combination anticancer therapy. This article summarizes the anti-cancer mechanism of ARTs and its efficacy, safety and dose range.