目的 研究β-環(huán)糊精-聚乙二醇-α-常春藤皂苷自組裝膠束的制備、溶血性和體內(nèi)外抗腫瘤活性。方法 采用自組裝方法制備了β-環(huán)糊精-聚乙二醇-α-常春藤皂苷的納米膠束，考察了膠束在大鼠全血中的溶血性，研究了膠束在不同細(xì)胞上的體外活性，以荷HT29腫瘤細(xì)胞的小鼠為模型，研究了膠束的體內(nèi)抗腫瘤活性。結(jié)果 β-環(huán)糊精-聚乙二醇-α-常春藤皂苷在水性介質(zhì)中能自組裝成粒徑較小的納米膠束。該膠束能顯著降低α-常春藤皂苷的溶血性；在體外細(xì)胞實驗中，膠束的抗腫瘤活性明顯低于α-常春藤皂苷，這可能與在體外環(huán)境中α-常春藤皂苷不能從膠束中釋放出來有關(guān)。β-環(huán)糊精-聚乙二醇-α-常春藤皂苷自組裝膠束在HT29荷瘤小鼠體內(nèi)顯示非常好的抗腫瘤活性。結(jié)論 β-環(huán)糊精-聚乙二醇-α-常春藤皂苷自組裝膠束為皂苷的減毒增效提供了一個非常好的研究模式。

Objective To prepare β-CD-PEG-α-hederin self-assembly micelle, and to study its preparation, hemolytic activity and the anti-tumor in vitro and in vivo. Methods The micelle was prepared with the self-assembly method. The hemolytic activity was studied with the rat blood. The in vitro and in vivo pharmacological activity was studied with cancer cell and tumor xenograft mice, respectively. Results The micelle was self-assembled in the aqueous solvent with small diameter. The hemolytic activity of β-CD-PEG-α-hederin micelle could be negligible when compared with α-hederin. The in vitro cytotoxicity of β-CD-PEG-α-hederin micelle was very low which may be related to the inability of α-hederin to be released from micelles in the in vitro environment. The micelle displayed a high anti-tumor activity in HT29-bearing mice. Conclusion The study of β-CD-PEG-α-hederin self-assembly micelle provides a basis for attenuation and enhancement of saponins.

R944

江西省衛(wèi)生計生委中醫(yī)藥科研課題（2017B096）