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第 7 期 孙建瑞，等: 铁棒锤中 3-乙酰乌头碱和宋果灵抗肿瘤活性
乙酰乌头碱能阻滞 HepG2 细胞于细胞增殖周期的
G1 期，而不能进入 S 期。G1 期是决定细胞增殖状
态的关键阶段，存在调节细胞增殖周期的检测点（R
点），它可以接受多种环境信号的调节，控制着细胞
增殖活动的进程，是细胞增殖与否的转折点
点可阻止受损伤的细胞进入 S 期，从而导致细胞增
殖的抑制，可见 3-乙酰乌头碱以某种抑制机制抑制
了 HepG2 细胞周期的进程，从而使细胞周期阻滞，
抑制肿瘤细胞的增殖。
图 10 HepG2 在不同质量浓度的 3-乙酰乌头碱处理的细
胞的周期时相分布
Fig. 10 Cell cycle phase of HepG2 cells treated by
3-acetylaconitine with different concentration
3 结论
本研究从铁棒锤中分离得到 3-乙酰乌头碱和宋
果灵两个化合物，用倒置显微镜和 LSCM 观察 3-乙
酰乌头碱和宋果灵对 HepG2 细胞形态的影响，用
MTT 法和流式细胞仪法对两种化合物的抗肝癌活
性及促进癌细胞凋亡能力进行了考察。随着 3-乙酰
乌头碱和宋果灵浓度的增加及作用时间的延长，其
抗肿瘤效果逐步增强，最高分别达到 93.56%和
98.48%，具有明显的时间-效应和剂量-效应关系。
3-乙酰乌头碱和宋果灵作用于人肝癌细胞后，使细
胞出现聚集、脱壁，进而死亡，细胞增殖能力减低，
使细胞发生早期凋亡和晚期凋亡的比率增大，3-乙
酰乌头碱使早期细胞凋亡率上升至 58.32%，晚期凋
亡率增至 13.81%；宋果灵使早期细胞凋亡率上升至
41.02%，晚期凋亡率增至 28.78%。随给药组处理时
间的延长 G1 期细胞逐渐增多，G2 期和 S 期细胞逐
渐减少，可见 3-乙酰乌头碱以某种机制抑制了细胞
的增殖活动。因此，3-乙酰乌头碱和宋果灵是对抗
肝癌的一个很好的候选治疗剂，值得进一步探索其
抗肿瘤机制，并且为研发新型乌头属抗肿瘤药物的
研究提供参考。
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