Document Detail

Photodynamic therapy of fullerene modified with pullulan on hepatoma cells.
MedLine Citation:
PMID:  20180750     Owner:  NLM     Status:  MEDLINE    
To design a novel cytospecific photosensitizer for photodynamic antitumor therapy, a fullerene (C(60)) was chemically modified with pullulan which is a water-soluble polysaccharide with a high affinity for asialoglycoprotein receptors. Ethylene diamine was introduced to the terminal aldehyde groups of pullulan by the reductive amination reaction. Pullulan was coupled to C(60) through the terminal amine group. The C(60) end-group conjugated with pullulan was water-soluble and generated superoxide anion upon light irradiation. The C(60)-pullulan conjugates significantly suppressed the in vitro growth of HepG2 hepatoma cells with asialoglycoprotein receptors, while less suppression activity was observed for HeLa cells without the receptors. The conjugates have a high binding affinity for HepG2 cells, in contrast to HeLa cells. When C(60) was conjugated with polyethylene glycol (PEG) with the similar molecular weight in order to compare the in vitro cell binding and antitumor activities with the C(60)-pullulan conjugate, the dependence of cell type on their activities was not observed. Following the intravenous injection of C(60)-pullulan conjugates to mice carrying a subcutaneous mass of HepG2 cells, significant stronger photodynamic effect on tumor was observed than the intravenous injection of C(60)-PEG conjugates and saline. It is concluded that the pullulan conjugation gave C(60) the targetability to HepG2 cells, resulting in enhanced photodynamic tumor therapy effect.
Jian Liu; Yasuhiko Tabata
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of drug targeting     Volume:  18     ISSN:  1029-2330     ISO Abbreviation:  J Drug Target     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-03     Completed Date:  2010-12-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9312476     Medline TA:  J Drug Target     Country:  England    
Other Details:
Languages:  eng     Pagination:  602-10     Citation Subset:  IM    
Department of Biomaterials, Field of Tissue Engineering, Institute for Frontier Medical Sciences, Kyoto University, Sakyo-ku, Kyoto, Japan.
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MeSH Terms
Carcinoma, Hepatocellular / drug therapy*,  metabolism,  pathology
Fullerenes / therapeutic use*
Glucans / metabolism*,  therapeutic use*
Hep G2 Cells
Photosensitizing Agents / therapeutic use*
Polyethylene Glycols / chemistry
Reg. No./Substance:
0/Excipients; 0/Fullerenes; 0/Glucans; 0/Photosensitizing Agents; 0/Polyethylene Glycols; 9057-02-7/pullulan; 99685-96-8/fullerene C60

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