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负载熊果酸和人参皂苷Rg3的脂质体治疗肝细胞癌

Liposomes co-loaded with ursolic acid and ginsenoside Rg3 in the treatment of hepatocellular carcinoma.

作者信息

Wang Bin, Xu Qiaoqiao, Zhou Chenjian, Lin Yu

机构信息

Department of Pharmaceutical, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325000, China.

Department of Pharmaceutical, Wenzhou Central Hospital, Wenzhou, Zhejiang 325000, China.

出版信息

Acta Biochim Pol. 2021 Nov 3;68(4):711-715. doi: 10.18388/abp.2020_5608.

Abstract

OBJECTIVE

Liposomes co-loaded with ursolic acid and ginsenoside Rg3 (UA+Rg3-LIP) were prepared to study their effects on the proliferation, apoptosis and cell cycle of hepatocellular carcinoma (HCC) cells.

METHODS

Liposomes were prepared by reverse evaporation, and then UA+Rg3-LIP were prepared by the pH gradient method, and followed by liposome characterization. Next, the effects of UA+Rg3-LIP on the proliferation, apoptosis and cell cycle of HepG2 cells were investigated by MTT method and flow cytometry at the cell level.

RESULTS

The entrapment efficiency of UA in UA+Rg3-LIP was 78.52% and that of Rg3 was 71.68%, as assayed by low-temperature ultracentrifugation. The in vitro release rates of UA+Rg3-LIP and UA+Rg3 detected by the dialysis membrane method were 1-10 h. The release rate of UA+Rg3 was close to 100%; that of UA+Rg3-LIP was decreased after 10 h and approached 100% after 24 h. It was further confirmed by cell experiments that UA+Rg3-LIP could significantly reduce cells viability while at the same time increase their apoptosis rate and raise the proportion of cells in the G0/G1 phase.

CONCLUSION

Liposomes co-loaded with ursolic acid and ginsenoside Rg3 could affect cell proliferation, apoptosis and cell cycle, thus slowing down the in vitro drug release ability of HCC.

摘要

目的

制备同时负载熊果酸和人参皂苷Rg3的脂质体(UA+Rg3-LIP),研究其对肝癌(HCC)细胞增殖、凋亡及细胞周期的影响。

方法

采用逆相蒸发法制备脂质体,然后通过pH梯度法制备UA+Rg3-LIP,并对脂质体进行表征。接下来,在细胞水平上通过MTT法和流式细胞术研究UA+Rg3-LIP对HepG2细胞增殖、凋亡及细胞周期的影响。

结果

通过低温超速离心法测定,UA+Rg3-LIP中UA的包封率为78.52%,Rg3的包封率为71.68%。采用透析膜法检测,UA+Rg3-LIP和UA+Rg3的体外释放时间为1-10小时。UA+Rg3的释放率接近100%;UA+Rg3-LIP在10小时后释放率下降,24小时后接近100%。细胞实验进一步证实,UA+Rg3-LIP可显著降低细胞活力,同时提高其凋亡率,并增加处于G0/G1期的细胞比例。

结论

同时负载熊果酸和人参皂苷Rg3的脂质体可影响细胞增殖、凋亡及细胞周期,从而减缓肝癌细胞的体外药物释放能力。

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