荭草抗肿瘤活性提取物质量标志物的初步研究

目的基于质量标志物(Q-marker)理论,分析具有抗肿瘤活性的荭草醋酸乙酯提取物的成分,研究其质量控制方法。方法首先使用UPLC-ESI-HRMS对该提取物进行成分鉴定;再使用HPLC进行成分的定量测定,同时建立其定量测定方法,并对鉴定出的化合物进行药理作用分析,初步预测Q-marker;最后采用人非小细胞肺癌A549细胞模型,研究荭草醋酸乙酯提取物及6种候选成分混合物对A549肿瘤细胞生长及迁移的影响。结果通过UPLC-ESI-HRMS结果指认出12个化合物,其中,HPLC未检出原儿茶酸、儿茶素、山柰素和芹菜素,异牡荆素和木犀草素质量分数低于0.01mg/g,不纳入Q-marker候选物之列。结合药理作用分析,最终选择了6种成分没食子酸、异荭草苷、荭草苷、牡荆素、木犀草苷和槲皮苷作为其潜在Q-marker。各样品中均能检测出这6个成分,且6个成分总量超过10%。荭草醋酸乙酯提取物及等剂量6成分混合物均能显著抑制A549细胞的增殖与迁移,并诱导其凋亡,且两组之间效果无显著性差异。结论没食子酸、异荭草苷、荭草苷、牡荆素、木犀草苷和槲皮苷作为具有抗肿瘤活性的荭草醋酸乙酯提取物中的潜在Q-...

Preliminary study on Q-markers of anti-tumor activity extracts of Polygonum orientale

Objective Based on the concept of quality marker (Q-marker), the components and the quality of the ethyl acetate extract of Polygonum orientale (POEa) was analyzed and studied. Methods Firstly, the components of POEa were identified using the UPLC-ESI-HRMS method and standard compounds. Secondly, the main active compounds were determined by HPLC. Antitumor activities of these compounds were reviewed and its Q-marker was predicted. Finally, we evaluated the effects of POEa and the compound of gallic acid, isoquercetin, valerin, vitexin, luteolin, and quercetin on proliferation, apoptosis and migration of A549 cells. Results A new quality method for simultaneous determining these six compounds of POEa was established. The six chemical ingredients were detected in each sample and the total content was more than 10%. The number of apoptotic cells in A549 cells treated with POEa and six chemical mixtures were all substantial increased, and the migration amount were significantly decreased. Tow groups showed no significantly differeances. Conclusion The six components are scientific and reasonable to be considered as potential Q-marker represented the anti-tumor activity of POEa. The HPLC method can be used as accurate and stable quality control strategy of POEa.