聚乙二醇修饰对α-苦瓜素抗肿瘤活性的影响  

Effects of PEGylation on anti-tumor activity of α-momorcharin

作　　者：伍黎黎[1] 沈富兵[2] 刘敏[1] 孟延发[1] 

机构地区：[1]四川大学生命科学学院生物资源与生态环境教育部重点实验室,四川成都610064 [2]成都医学院,四川成都610083

出　　处：《华西药学杂志》2011年第1期5-8,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金(批准号:30770232)

摘　　要：目的探讨苦瓜籽核糖体失活蛋白α-苦瓜素(α-MMC)经聚乙二醇(PEG)修饰后,其体外细胞毒性和体内抗肿瘤活性的变化。方法用MTT法测定α-MMC和PEG-α-MMC结合物对小鼠乳腺癌细胞EMT-6的抑制率;通过BALB/C小鼠模型研究药物对EMT-6细胞嫁接瘤生长的抑制作用。结果在相同的条件下,PEG-α-MMC结合物对体外培养的EMT-6细胞生长抑制效果相对α-MMC降低了30%,且两者对肿瘤细胞的毒性呈剂量和时间依赖性。PEG-α-MMC结合物的体内抗肿瘤活性比相同剂量的α-MMC增加约10%,且两者对肿瘤生长的抑制作用呈剂量依赖性。结论α-MMC经PEG修饰后,其体外抗肿瘤活性显著减低,而体内抗肿瘤活性增高,预示PEG-α-MMC结合物具备更好的抗肿瘤潜能。OBJECTIVE To study the alteration of anti-tumor activity of PEGylated α-momorcharin（α-MMC） in vivo and it＇s cytoxicity in vitro compared with native α-MMC.METHODS MTT assay was used to investigate the antitumor effect of PEGylated α-MMC（PEG-α-MMC） on murine breast tumor EMT-6 cell line in vitro.Xenograft tumor growth assay was used to evaluate the antitumor effect of PEG-α-MMC on EMT-6 cells in vivo.RESULTS Our data indicated that the anti-tumor activity of PEG-α-MMC conjugate on EMT-6 cells decreased about 30% in vitro compared to equivalent dose of α-MMC.The cytotoxicity of PEG-α-MMC conjugate was depending on dosage and time as well as α-MMC.The antitumor activity of PEG-α-MMC conjugate increased about 10% in vivo compared to equivalent dose of α-MMC.CONCLUSION The anti-tumor activity of α-MMC modified by PEG was declined significantly in vitro,whereas increased in vivo.

关 键 词：α-苦瓜素 聚乙二醇修饰 抗肿瘤活性 

分 类 号：R96[医药卫生—药理学]