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CLC number: R979.1; R945

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Received: 2010-08-24

Revision Accepted: 2010-12-27

Crosschecked: 2011-08-09

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Journal of Zhejiang University SCIENCE B 2011 Vol.12 No.9 P.720-729


Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery

Author(s):  Qi-da Hu, Hui Fan, Wei-jian Lou, Qing-qing Wang, Gu-ping Tang

Affiliation(s):  Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou 310028, China, Department of Pharmacy, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, Hangzhou 310016, China, Institute of Immunology, Zhejiang University, Hangzhou 310058, China, The First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China

Corresponding email(s):   tangguping@yahoo.com.cn

Key Words:  Polyethylenimine, β, -Cyclodextrin, Tegafur, Co-delivery, Gene therapy

Qi-da Hu, Hui Fan, Wei-jian Lou, Qing-qing Wang, Gu-ping Tang. Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery[J]. Journal of Zhejiang University Science B, 2011, 12(9): 720-729.

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author="Qi-da Hu, Hui Fan, Wei-jian Lou, Qing-qing Wang, Gu-ping Tang",
journal="Journal of Zhejiang University Science B",
publisher="Zhejiang University Press & Springer",

%0 Journal Article
%T Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery
%A Qi-da Hu
%A Hui Fan
%A Wei-jian Lou
%A Qing-qing Wang
%A Gu-ping Tang
%J Journal of Zhejiang University SCIENCE B
%V 12
%N 9
%P 720-729
%@ 1673-1581
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%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.B1000307

T1 - Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery
A1 - Qi-da Hu
A1 - Hui Fan
A1 - Wei-jian Lou
A1 - Qing-qing Wang
A1 - Gu-ping Tang
J0 - Journal of Zhejiang University Science B
VL - 12
IS - 9
SP - 720
EP - 729
%@ 1673-1581
Y1 - 2011
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.B1000307

polyethylenimine-Cyclodextrin-tegafur (PEI-CyD-tegafur) conjugate was synthesized as a novel multifunctional prodrug of tegafur for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein (EGFP) reporter plasmid DNA. Conjugation of tegafur to PEI-CyD via chemical linkage was characterized by 1H NMR spectrometry and ultraviolet (UV) spectrometry. PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around 150 nm with positive charge at the N/P ratio of 25, in accordance with electron microscopy observation of compact and monodisperse nanoparticles. The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in B16F10 cell line. Therefore, PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and potential for gene delivery.

Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article


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