Document Detail

Water-soluble polysaccharide-anthracycline conjugates: biological activity.
MedLine Citation:
PMID:  1575887     Owner:  NLM     Status:  MEDLINE    
The anticancer agents doxorubicin and daunorubicin were covalently linked to the water-soluble anionic polysaccharides hyaluronic acid and carboxy-methylcellulose. The drug-polymer conjugates are in principle prevented from entering cells, can efficiently bind to cell surfaces and allow precise dose-response determinations. In addition, they are not able to bind DNA because of their negative charge. Cell growth and DNA synthesis inhibition studies indicated decreased cell toxicity for the polymer conjugates. The mol. wt of the carrier was shown to affect the biological activity of the anthracycline to a moderate extent. Partial drug incorporation into cells was observed as a function of time, probably due to endocytosis phenomena followed by biochemical cleavage of the conjugate. The conclusion was drawn that membrane binding appears to contribute to total toxicity only to a minor extent.
C Cera; M Palumbo; S Stefanelli; M Rassu; G Palù
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anti-cancer drug design     Volume:  7     ISSN:  0266-9536     ISO Abbreviation:  Anticancer Drug Des.     Publication Date:  1992 Apr 
Date Detail:
Created Date:  1992-06-09     Completed Date:  1992-06-09     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8603523     Medline TA:  Anticancer Drug Des     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  143-51     Citation Subset:  IM    
Department of Pharmaceutical Sciences, Centro Studi sulla Chimica del Farmaco e dei Prodotti Biologicamente Attivi, Padova, Italy.
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MeSH Terms
Carboxymethylcellulose / metabolism,  pharmacology*
Cell Survival / drug effects
DNA / drug effects
Daunorubicin / metabolism,  pharmacology*
Doxorubicin / metabolism,  pharmacology*
Hela Cells
Hyaluronic Acid / metabolism,  pharmacology*
Microscopy, Electron
Tumor Cells, Cultured
Reg. No./Substance:
20830-81-3/Daunorubicin; 23214-92-8/Doxorubicin; 9004-32-4/Carboxymethylcellulose; 9004-61-9/Hyaluronic Acid; 9007-49-2/DNA

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