精氨酸-甘氨酸-天冬氨酸肽修饰的脂质体雷公藤甲素靶向抗肿瘤效果  

Evaluation of antitumor efficacy of arginine-glycine-aspartic acid-modified triptolide liposomes

作　　者：熊小丽[1] 陈鹏[2] 赵东赤[3] 

机构地区：[1]武汉大学中南医院儿科,430071 武汉市儿童医院中西医结合科 [2]武汉市儿童医院中西医结合科 [3]武汉大学中南医院儿科,430071

出　　处：《中华实验外科杂志》2015年第3期505-507,共3页Chinese Journal of Experimental Surgery

基　　金：国家自然科学基金资助项目（81403434）;武汉市青年科技晨光计划资助项目（201150431082）

摘　　要：目的 制备精氨酸-甘氨酸-天冬氨酸（RGD）肽修饰的脂质体雷公藤甲素,探讨RGD肽靶向脂质体雷公藤甲素（RGD-TPL-LPs）纳米药物在小鼠移植性肝癌模型的靶向效果及药效.方法 通过成膜法制备具有靶向作用的脂质体纳米药物（RGD-TPL-LPs）,并观察细胞毒性.建立小鼠移植肝癌肿瘤模型并评价药效.结果 靶向修饰脂质体RGD-TPL-LPs的肿瘤细胞毒性明显强于无靶向脂质体（TPL-LPs）.此外,RGD靶向修饰的RGD-TPL-LPs抑瘤率为61.2％,要明显高于无靶向TPL-LPs的45.2％和游离雷公藤甲素的20.0％.结论 RGD靶向修饰的雷公藤甲素脂质体能够明显抑制肿瘤的生长,具有显著的抗肿瘤效果.Objective To discuss the effect of arginine-glycine-aspartic acid （RGD） peptide-modified triptolide lipidosomes （RGD-TPL-LPs） against the subcutaneous xenotransplanted tumor model of liver cancer.Methods RGD-TPL-LPs were prepared by a method of film-forming.The cytotoxicity of RGD-TPL-LPs against HepG2 cells and COS-7 cells was evaluated.The effect of RGD-TPL-LPs on liver cancer was olso investigated in vivo.Results RGD-TPL-LPs generated higher cytotoxicity against HepG2 cells than non-targeted TPL-LPs controls.Furthermore,in vivo animal experiments demonstrated that RGD-TPL-LPs remarkably reduced the tumor growth.Inhibitory rate of RGD-TPL-LPs was 61.2%,significantly higher than TPL-LPs （45.2%） or TPL （20.0%）.Conclusion The above results indicate that RGD-TPL-LPs can markedly enhance the antitumor efficacy against subcutaneous xenotransplanted tumor of liver cancer.

关 键 词：精氨酸-甘氨酸-天冬氨酸 脂质体 雷公藤甲素 癌 肝细胞 

分 类 号：R285.5[医药卫生—中药学]