Source:http://linkedlifedata.com/resource/pubmed/id/11881996
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2002-3-7
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pubmed:abstractText |
This paper describes the first covalent synthesis of kappa-carrageenan-3'-azido-3'-deoxythymidine (AZT) conjugates. A succinate diester spacer was used to covalently couple AZT onto kappa-carrageenan, resulting in a tripartite prodrug. Two methods (UV and radioactive counting) are described and validated to determine the AZT loading onto the kappa-carrageenan carrier. This polymeric carrier, through its own intrinsic anti-HIV activity, is expected to act not only as a drug delivery agent but also as an anti-HIV agent. Synergism between the two drugs (kappa-carrageenan and AZT) was demonstrated when MT-4 cells were preincubated with the kappa-carrageenan-AZT conjugate prior to HIV-1-infection. A threshold of AZT loaded onto the kappa-carrageenan was required to achieve this synergistic effect. Such kappa-carrageenan-AZT conjugates could be of great therapeutic interest because these conjugates, which contain a low AZT concentration, present improved anti-HIV activities relative to free AZT. Moreover, kappa-carrageenan is a well-tolerated biopolymer, already used in the food industry.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1275-83
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11881996-Anti-HIV Agents,
pubmed-meshheading:11881996-Carbohydrate Sequence,
pubmed-meshheading:11881996-Carrageenan,
pubmed-meshheading:11881996-Cells, Cultured,
pubmed-meshheading:11881996-Drug Synergism,
pubmed-meshheading:11881996-HIV-1,
pubmed-meshheading:11881996-Humans,
pubmed-meshheading:11881996-Molecular Sequence Data,
pubmed-meshheading:11881996-Prodrugs,
pubmed-meshheading:11881996-Zidovudine
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities.
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pubmed:affiliation |
Laboratoire de Chimie Biomoléculaire, Faculté des Sciences de Luminy, 163 avenue de Luminy, case 901, 13288 Marseille Cedex 9, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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