管花蒲公英中抗肿瘤活性化合物的快速筛选研究

目的: 应用肿瘤细胞提取和色谱联用分析技术快速预测管花蒲公英中潜在的抗肿瘤活性化合物。 方法: 使用管花蒲公英醇提取物与人子宫颈癌细胞株(Hela)以及人胃腺癌细胞株(MK-1)孵育培养,HPLC-ESI-MS/MS及NMR技术分析和鉴定肿瘤细胞破碎液中化合物。 结果: Hela细胞破碎液中检测到10个活性化合物,MK-1细胞破碎液中检测到5个活性化合物。 结论: 活性化合物可特异性地与靶细胞膜结合或进入靶细胞内,采用肿瘤细胞提取结合色谱联用分析技术,发现管花蒲公英中10个化合物(没食子酸,咖啡酰基酒石酸,绿原酸,4-O-咖啡酰基奎宁酸,槲皮素-3-O-α-D-吡喃阿拉伯糖苷,槲皮素-3-O-β-D-吡喃葡萄糖苷,槲皮素-3-O-α-D-呋喃阿拉伯糖苷,槲皮素-3-O-α-L-鼠李糖苷,槲皮素,木犀草素)可与Hela细胞结合,5个化合物(没食子酸,没食子酸甲酯,咖啡酸,槲皮素,木犀草素)可与MK-1细胞结合,该研究方法可预测中药提取中潜在的抗肿瘤活性成分。

Objective: The tumor cells extraction coupled with HPLC-ESI-MS/MS analysis has been applied to fast screen potential antitumor compounds from Neo-Taraxacum siphonathum. Method: Hela and MK-1 were incubated with the ethanol extract of Neo-Taraxacum siphonathum,and then the potential active compounds in cells desorption eluate were analyzed and elucidated by HPLC-ESI-MS/MS and NMR experiments. Results: Ten compounds were found to combine with Hela,while five compounds were found to combine with MK-1. Conclusion: After cells were incubated with the extraction,potential bioactive compounds should selectively combine with the cells.Ten compounds(gallic acid,caftaric acid,chlorogenic acid,4-O-caffeoylquinic acid,quercetin-3-O-α-D-arabinopyranoside,quercetin-3-O-β-D-glucopyranoside,quercetin-3-O-α-D-arabinofuranoside,quercetin-3-O-α-L-rhamnoside,quercetin and luteolin)were found to selectively bound to Hela cell,while five compounds(gallic acid,gallicin,caffeic acid,quercetin and luteolin)were found to selectively bound to MK-1 cell.The results displayed that the study could be applied to screen potent active compounds from complex mixtures.