染料木素MePEG-PLGA共聚物胶束体内外抗肿瘤作用

Anti-tumor Effect of Genistein MePEG-PLGA Copolymer Micelles in Vitro and in Vivo

目的探讨染料木素MePEG-PLGA共聚物胶束对人肝癌SMMC-7721细胞的体内外抗肿瘤作用。方法采用MTT法、Annexin V-FITC/PI染法分别考察染料木素MePEG-PLGA共聚物胶束对人肝癌SMMC-7721细胞的细胞毒性、细胞凋亡、细胞周期的影响;通过荷肝SMMC-7721瘤裸鼠体内抗肿瘤试验,考察染料木素胶束的体内抗肿瘤效应。结果染料木素胶束对肝癌SMMC-7721细胞的抑制率均高于染料木素,最高抑制率分别可达83.26%,78.25%。流式细胞仪检测结果显示,染料木素胶束组能够提高染料木素对SMMC-7721细胞凋亡的诱导能力,并且呈浓度依赖性。5,10,20μg·mL^-1的染料木素组和染料木素胶束组药物作用于SMMC-7721细胞48 h时,染料木素胶束能够明显提高染料木素对细胞G2/M期细胞的阻滞作用,并且呈现浓度依赖性。体内抗肿瘤试验结果表明,相同浓度的染料木素胶束组的抑瘤效果显著强于染料木素乳剂组,呈浓度依赖性,最高抑瘤率可达55.41%。结论染料木素MePEG-PLGA共聚物胶束在体内和体外均有显著的抗肝癌作用。

OBJECTIVE To study the anti-tumor effect of genistein(GEN)MePEG-PLGA copolymer micelles on human hepatoma SMMC-7721 cells in vitro and in vivo.METHODS MTT assay,Annexin V-FITC/PI staining were used to investigate the effects of GEN MePEG-PLGA copolymer micelles on cytotoxicity,apoptosis and cell cycle of human hepatoma SMMC-7721 cells.The in vivo anti-tumor effect of GEN micelles was investigated in nude mice bearing hepatocellular carcinoma SMMC-7721 tumor in vivo.RESULTS The inhibitory rate of GEN micelles in SMMC-7721 cells were higher than GEN and the highest inhibition rates were 83.26%and 78.25%,respectively.The results of flow cytometry showed that the GEN micelles group could increase the ability of GEN to induce apoptosis of SMMC-7721 cells and presented a concentrationdependent manner.When the concentration of 5,10,20μg·mL^-1 GEN and GEN micelles groups acted on SMMC-7721 cells for 48 h,the GEN micelles could significantly enhance the ability of arrest cell in G2/M phase for GEN,and showing a concentration-dependent manner.In vivo anti-solid tumor experimental results showed that the same concentration of GEN micelles group had significantly better anti-tumor effect than GEN emulsion,and in a concentration-dependent manner,the highest tumor inhibition rate was 55.41%.CONCLUSION The GEN MePEG-PLGA copolymer micelles has significant anti-hepatocarcinoma effects both in vivo and in vitro.