蟾酥中蟾毒配基类成分的分离纯化及其体外抗肿瘤活性的研究

Isolation and antitumor activity in vitro of three kinds of bufadienolides

目的:研究蟾酥中蟾毒配基类成分的分离纯化方法,并初步考察其体外抗肿瘤活性。方法:采用硅胶柱层析法纯化蟾酥药材粗提物,高效液相法测定三种蟾毒配基含量,以此确定最佳纯化工艺;MTT比色法测定药物对肿瘤细胞的生长抑制作用。结果:用优化工艺制备得到的纯化产物蟾毒配基类成分平均含量为95.98%;纯化产物具有显著的抑制肿瘤细胞生长作用,在0.001～100μg/mL的浓度范围内,药物对人乳腺癌MDA-MB-435细胞和人肺癌A549细胞有很强的抑制作用。结论:硅胶柱层析法适合于蟾酥中蟾毒配基类成分:脂蟾毒配基、华蟾毒基、蟾毒灵的制备,且纯化产物体外抗肿瘤作用显著。

AIM： To isolate three kinds of bufadienolides composition from Venenum bufonis in order to investigate their antitumor activity in vitro.METHODS： Alcohol extraction and isolation by Silica gel colume were employed in this study.Their antitumor activities in vitro were evaluated by MTT colorimetric method.RESULTS： With such methods,three kinds of bufadienolides,including Bufalin,cinobufagin,and resibufogenin with purity above 90% were prepared.The in-vitro results showed that three kinds of bufadienolides had prominent inhibition effect on human lung cancer A549 cells,human breast cancer MDA-MB-435 cells in the range of 0.001 μg/mL ～ 100 μg/mL.CONCLUSION： Isolation by Silica gel colume can be used to separate three kinds of bufadienolides from Venenum bufonis and its constituents has prominent anti-cancer effects.