铁棒锤中3-乙酰乌头碱和宋果灵抗肿瘤活性

Anti-tumor Activity of 3-Acetylaconitine and Songorine from Aconitum szechenyianum Gay.

从铁棒锤总生物碱中提取分离得到了3-乙酰乌头碱和宋果灵,采用四唑盐（MTT）比色法考察了药物的细胞毒性,电子显微镜及激光共聚焦显微镜观察了细胞形态,流式细胞术分析了细胞凋亡和细胞周期。抗肿瘤活性研究表明：随着3-乙酰乌头碱和宋果灵浓度的增加,抗肿瘤效果逐步增强,当质量浓度均为64 mg/L时,对HepG2细胞的抑制率分别最高达到93.56%和98.48%。药物作用于人肝癌细胞后,能明显抑制HepG2细胞的生长,并且使细胞发生早期凋亡和晚期凋亡的比率增大,质量浓度为100 mg/L 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%;质量浓度为120 mg/L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。

3-Acetylaconitine and songorine were extracted and separated from the total alkaloids of Aconitum szechenyianum Gay., and cytotoxicity of drugs were studied by MTT method using human liver cancer cells（HepG2）. Morphological changes of carcinoma cells were also investigated by using inverted microscope and laser scanning confocal microscope（LSCM）. Cell apoptosis and cell cycle were analyzed by flow cytometry. The antitumor experiments showed that the antitumor effects were gradually enhanced with the increase of the concentration of 3-acetylaconitine and songorine, and the highest level was 93.56% and 98.48%, respectively, when mass concentration were all 64 mg/L. The growth of Hep G2 cells was inhibited significantly after the drugs acted on Hep G2, and the ratio of cell early apoptosis and late apoptosis increased. 3-Acetylaconitine increased early cell apoptosis rate to 58.32% and late apoptosis rate to 13.81%, when mass concentration was 100 mg/L, while songorine made early cell apoptosis rate and late apoptosis rate increased to 41.02% and 28.78%,when mass concentration was 120 mg/L. With the prolonging of treatment time, the G1 phase cells gradually increased, but G2 and S phase cells gradually decreased.