目的 对比研究青蒿素及其衍生物青蒿琥酯对人乳腺癌 MCF-7细胞增殖的影响并探讨其作用机制。方法采用体外培养的人乳腺癌 MCF-7细胞株，利用 SRB法测定青蒿素和青蒿琥酯对 MCF-7细胞增殖的影响，FCM法测定细胞周期的变化，亚 G₁ 期含量测定和 DAPI荧光染色法观察细胞凋亡。结果 10 μmol/L 青蒿素和 1μmol/L青蒿琥酯能明显改变 MCF-7细胞的细胞周期，使 S期细胞显著减少，G₀+G₁ 期细胞明显增加。青蒿素对 MCF-7细胞增殖仅有微弱抑制作用，但其衍生物青蒿琥酯却有显著的抑制作用，IC₅₀ 为 0.31μmol/L。同样，1μmol/L 青蒿琥酯引起 MCF-7细胞的凋亡和直接的细胞毒作用明显强于 10μm ol/L青蒿素的作用。结论 体外研究表明，对肿瘤细胞增殖的抑制青蒿琥酯比青蒿素作用强。

Object To study the effects of artemisinin and its analogue artemisunate on the proliferation of human breast cancer MCF-7 cell line, as well as their mechanism comparatively. Methods The inhibition of cell proliferation was determined by SRB method. Cell cycle was determined by flow cytometry (FCM) analysis. Apoptosis was confirmed by sub-G₁ cells content and DAPI method. Results The cell cycle of MCF-7 was changed greatly when treated 24 h with either 10 μmol/L artemisinin or 1 μmol/L artemisunate, the distribution of MCF-7 cells among S phase was reduced greatly, while inereased during G₀+G₁. However, artemisinin had weaker effect on the proliferation of MCF-7 cell, while artemisunate effectively inhibited the proliferation of MCF-7, the IC₅₀ was 0.31 μmol/L. Apoptosis induced by 1 μmol/L artemisunate was stronger than that by 10 μmol/L artemisinin, too. Conclusion The inhibitory effect of artemisunate on the proliferation of tumor cell is stronger than that of artemisinin in vitro.