三种蟾毒单体对SMMC-7721和BEL-7402人肝癌细胞生长的抑制作用

目的：探讨蟾蜍中主要蟾毒内酯类成分蟾毒灵、华蟾酥毒基、酯蟾毒配基的抗肝癌作用及机制。方法：以SMMC—7721、BEL—7402人肝癌细胞为靶细胞，以丝裂霉素为阳性对照药物，应用四甲基偶氟唑盐比色法、锥虫蓝染色和DNA染色分析法观察这3种蟾毒单体对肝癌细胞的生长抑制和诱导凋亡作用。结果：蟾毒灵和华蟾酥毒基对上述肝癌细胞具有明显生长抑制作用，华蟾酥毒基较蟾毒灵作用略弱，但两者达到相同生长抑制效果所需浓度均低于丝裂霉素，酯蟾毒配基只有在较高浓度下才显示对肝癌细胞的生长抑制作用；不同浓度蟾毒灵、华蟾酥毒基对人肝癌细胞细胞膜具有破坏作用；可使人肝癌细胞阻止于G2／M期，使处于S期的细施比例降低，并有明显诱导肝癌细胞凋亡作用。结论：蟾毒灵、华蟾酥毒基对上述人肝癌细胞具有明显生长抑制作用，具有对肝癌细胞膜的直接破坏作用和诱导凋亡作用；酯蟾毒配基抗肿瘤作用较弱。

Inhibition effects of three kinds of bufotoxins on human SMMC-7721 and BEL-7402 hepatoma cells lines

Objective: To study the effect and mechanism of bufalin, cinobufagin and resibufogenin on human hepatoma cell lines. Methods: SMMC-7721 and BEL-7402 cells were incubated with the above 3 drugs at different concentration separately. Mitomycin C was used as control drugs. The inhibitory rate was analyzed by MTT and trypan-blue staining assay. Cell DNA contents and apoptosis were analyzed by flow cytometer. Results: Bufalin and cinobufagin even at low concentration remarkably inhibited the cells growth, stopped the cells in G2/M phase and induced the cells apoptosis. High dose of bufalin and cinobufagin damaged the cells membrane effectively. Anti-tumor effects of both bufalin and cinobufagin were stronger than that of mitomycin C at the same concentration, and the effect of bufalin was stronger than that of cinobufagin. Conclusion: Bufalin and cinobufagin can efficiently depress the cancer cells growth, inducing cells apoptosis and demolishing cells membrane are 2 ways of their anti-tumor effects, while resibufogenin has weak anti-tumor effect.