[Preparation of floxuridine loaded polycation and its antitumor activity].
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.
Zhao
Dan-Jun
DJ
Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou 310028, China.
Lu
Xiao
X
Jiang
Qi-Ying
QY
Chen
Dan
D
Zhou
Jun
J
Yu
Hai
H
Wang
Qing-Qing
QQ
Tang
Gu-Ping
GP
D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D005467:Floxuridine / Q000494:pharmacology*; D005472:Fluorouracil / Q000494:pharmacology*; D006801:Humans; D008113:Liver Neoplasms / Q000473:pathology; D011094:Polyethyleneimine / Q000494:pharmacology*; D011355:Prodrugs / Q000138:chemical synthesis / Q000494:pharmacology; D047392:beta-Cyclodextrins / Q000494:pharmacology*
D000964:Antimetabolites, Antineoplastic; D011355:Prodrugs; D047392:beta-Cyclodextrins; D005467:Floxuridine; D011094:Polyethyleneimine; D005472:Fluorouracil