Zhao Dan-Jun, Lu Xiao, Jiang Qi-Ying, Chen Dan, Zhou Jun, Yu Hai, Wang Qing-Qing, Tang Gu-Ping
Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou 310028, China.
Zhejiang Da Xue Xue Bao Yi Xue Ban. 2009 Jan;38(1):53-8. doi: 10.3785/j.issn.1008-9292.2009.01.008.
To develop a new prodrug of 5-fluorouracil-polyethylenimine-beta-cyclodextrin-floxuridine (PEI-beta-CyD-Fd) and to test its antitumor activity.
Floxuridine was conjugated to polyethylenimine-beta-cyclodextrin to form prodrug PEI-beta-CyD-Fd. The structure of synthesized PEI-beta-CyD-Fd was confirmed by (1)H-NMR, FT-IR and UV. MTT assay and cell wound healing assay were performed on human hepatic carcinoma cell line HepG2.
The drug loading was 2 %. The MTT assay and cell wound healing assay indicated that PEI-beta-CyD-Fd significantly inhibited proliferation and migration of HepG2 cells.
The synthesized prodrug PEI-CyD-Fd has a significant antitumor activity on HepG2 cells.
研发一种新型的5-氟尿嘧啶-聚乙烯亚胺-β-环糊精-氟尿苷（PEI-β-CyD-Fd）前药，并测试其抗肿瘤活性。
将氟尿苷与聚乙烯亚胺-β-环糊精偶联形成前药PEI-β-CyD-Fd。通过¹H-NMR、FT-IR和UV对合成的PEI-β-CyD-Fd的结构进行确证。对人肝癌细胞系HepG2进行MTT法检测和细胞划痕愈合实验。
载药量为2%。MTT法检测和细胞划痕愈合实验表明，PEI-β-CyD-Fd显著抑制HepG2细胞的增殖和迁移。
合成的前药PEI-CyD-Fd对HepG2细胞具有显著的抗肿瘤活性。
