目的:研究异叶败酱提取物对白血病细胞体外增殖的毒性抑制作用。方法:提取异叶败酱浸膏,通过硅胶柱分离纯化异叶败酱中的单体化合物,选择白血病细胞株HL-60、K562、Jurkat为实验对象,与不同浓度的异叶败酱提取物及分离得到的单体化合物共同培养,采用CCK-8法检测其对白血病细胞体外增殖的影响,并通过流式细胞仪检测化合物3对K562细胞凋亡和周期的影响。结果:异叶败酱提取物和单体化合物均对白血病细胞有一定的毒性抑制作用,并且抑制作用与药物浓度有依赖关系。当不同浓度的化合物3作用于K562细胞后,K562细胞出现不同程度的凋亡,细胞早期凋亡率明显上升,与对照组相比具有显著性差异(P〈0.01);细胞周期G_0/G_1期所占比率由42.34%增至59.48%和64.72%,与对照组相比具有显著性差异(P〈0.01)。结论:异叶败酱提取物对白血病细胞具有明显的体外增殖毒性抑制作用,从中分离得到的环烯醚萜类化合物3能够诱导K562细胞的凋亡,并且将细胞周期阻滞在G0/G1期。异叶败酱提取物发挥抗肿瘤药理作用的物质基础很可能与其中的环烯醚萜类成分有关。
Objective: To study the inhibitory effect of extract from Patrinia heterophylla Bunge on the proliferation of leukemic cells in vitro. Methods: Isolated compounds were obtained from the whole plant Patrinia heterophylla Bunge through the means of chromatographic separation. The leukemic cells HL-60, K562 and Jurkat were cultured with different concentrations of extract from Patrinia extracts and compounds. CCK-8 assay was used to detect the inhibition of those extracts and compounds on human leukemic cell HL-60, K562 and Jurkat. And the effect of compound 3 on K562 cell cycle and apoptosis were detected by flow cytometry. Results: Both extracts and monomeric compounds had a certain dose-dependent inhibitory effect on the proliferation of leukemic cells. Different concentration of compound 3 could induce different degree of apoptosis of K562 cells. The early apoptosis rate was signifcantly higher than that of the control group (P 〈 0.01). The percentage of cells in G0/G1 phase increased from 42.34% to 59.48% and 64.72%, which was signifcantly different from that of the control group (P 〈 0.01). Conclusion: The Patrinia heterophylla Bunge has obvious inhibitory effect on the proliferation of leukemic cells in vitro. Compound 3 can induce the apoptosis of K562 cells and block the cell cycle in G0/G1 phase. The basis of antitumor pharmacological effects is likely to be related to the iridoid components.