前体化合物PEG-PLA-PTX的合成及体外抗肿瘤活性  

Synthesis and in vitro Antitumor Activity of PEG-PLA-PTX Prodrug

作　　者：孙玉[1] 张新明[2] 陈云艳[1] 汤琳[1] 周凌云[1] 

机构地区：[1]皖南医学院药学院,安徽芜湖241002 [2]安徽师范大学化学与材料科学学院,安徽芜湖241000

出　　处：《中国医药工业杂志》2015年第2期176-179,共4页Chinese Journal of Pharmaceuticals

基　　金：皖南医学院博士科研启动基金(201219);皖南医学院重点科研项目培育基金(WK2014Z06)的资助。

摘　　要：通过酯键将末端羧基化的聚乙二醇-聚乳酸(PEG-PLA)与紫杉醇连接,合成了前体化合物PEG-PLA-PTX(1),总收率约56%。芘荧光探针法测得1水溶液的临界胶束浓度为3.98×10-4 g/L,1在p H 7.4磷酸盐缓冲液中能缓慢释放出紫杉醇。体外抗肿瘤试验表明,1具有抑制鼻咽癌LMP1细胞增殖的作用。The prodrug PEG-PLA-PTX was synthesized by condensation of paclitaxel with carboxyl-terminated copolymer PEG-PLA through ester-bond formation with an overall yield of about 56 %. The PEG-PLA-PTX was found to have a critical micelle concentration （CMC） of 3.98× 10^ 4 g/L. The results of in vitro release experiments showed that the product could slowly release paclitaxel in pH 7.4 phosphate buffer （PBS）. In vitro antitumor assay indicated that PEG- PLA-PTX had cytotoxic activity against nasopharyngeal carcinoma LMP1 cells.

关 键 词：聚乙二醇-聚乳酸 紫杉醇 抗肿瘤活性 

分 类 号：R979.19[医药卫生—药品]