目的 制备靶向熊果酸脂质体，并评价其对宫颈癌HeLa细胞的体外靶向性。方法 采用化学合成方法制备新型的靶向性功能材料叶酸-CONH-聚乙二醇-NH-胆固醇，以薄膜分散法制备靶向熊果酸脂质体；构建以钙黄绿素为荧光探针标记物的脂质体，用荧光共聚焦倒置显微镜观察靶向脂质体对HeLa细胞的穿透能力；以流式细胞术考察靶向脂质体的摄取效率。同时，考察靶向熊果酸脂质体对HeLa细胞的生长抑制作用。结果 薄膜分散法制备的靶向熊果酸脂质体对HeLa细胞具有明显的靶向作用，并且具有显著的细胞增殖抑制作用。结论 靶向熊果酸脂质体可有效穿透HeLa细胞，且具有较强的杀伤宫颈癌细胞活性的作用。

Objective To prepare the targeted ursolic acid liposome and evaluate its targeting and inhibitory effects on HeLa cells in vitro. Methods Using folate receptors as cell targets, the new functional targeted material Folate-CONH-PEG-NH-Cholesterol conjugate was synthesized chemically. Ursolic acid liposome was developed by modifying Folate-CONH-PEG-NH-Cholesterol using film dispersed method. The liposome was constructed with calcein as a fluorescent probe marker, and the penetrating ability of targeted liposome on HeLa cells was observed by fluorescence confocal microscopy. The uptake efficiency of targeted liposome was investigated by flow cytometry. Meanwhile, the growth inhibitory effect of ursolic acid liposome on HeLa cells was investigated. Results The targeted ursolic acid liposome prepared by thin dispersion method had obvious targeting effect on HeLa cells and have significant anti-proliferative effect. Conclusion The targeted ursolic acid liposome can effectively penetrate HeLa cells with great killing power on the activity of cervical cancer cells.

博士资助项目科研启动经费032号