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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2008-7-3
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pubmed:abstractText |
The cell membrane folate receptor (FR) is a molecular target for tumor-selective drug delivery, including delivery of photosensitizers for anticancer photodynamic therapy (PDT). Tumor selectivity of meta-tetra(hydroxyphenyl)chlorin ( m-THPC), a photosensitizer used in PDT clinical trials, demonstrates a low tumor-to-normal epithelial uptake ratio. We report on the synthesis and on the photophysical properties of a m-THPC-like photosensitizer 1 conjugated to folic acid (compound 8). A comparative study of the accumulation of photosensitizers 1 and 8 is described. Nude mice were xenografted with FR-alpha-positive KB or HT-29 cells lacking FR-alpha as a negative control. Using optical fiber fluorimetry, we demonstrated that conjugate 8 exhibited enhanced accumulation in KB tumors compared to 1 4 h after injection. No significant difference between KB and HT-29 tumors was observed in case of compound 1. Tumor-to-normal tissue ratio exhibited a very interesting selectivity for conjugate 8 (5:1) in KB tumors 4 h postinjection.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1520-4804
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
10
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3867-77
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18553957-Animals,
pubmed-meshheading:18553957-Carrier Proteins,
pubmed-meshheading:18553957-Cell Line, Tumor,
pubmed-meshheading:18553957-Drug Delivery Systems,
pubmed-meshheading:18553957-Female,
pubmed-meshheading:18553957-Folate Receptors, GPI-Anchored,
pubmed-meshheading:18553957-Folic Acid,
pubmed-meshheading:18553957-Gene Expression Regulation,
pubmed-meshheading:18553957-Humans,
pubmed-meshheading:18553957-Mesoporphyrins,
pubmed-meshheading:18553957-Mice,
pubmed-meshheading:18553957-Mice, Nude,
pubmed-meshheading:18553957-Molecular Structure,
pubmed-meshheading:18553957-Neoplasms,
pubmed-meshheading:18553957-Photochemistry,
pubmed-meshheading:18553957-Photosensitizing Agents,
pubmed-meshheading:18553957-Receptors, Cell Surface,
pubmed-meshheading:18553957-Spectrophotometry,
pubmed-meshheading:18553957-Xenograft Model Antitumor Assays
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pubmed:year |
2008
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pubmed:articleTitle |
Improvement of meta-tetra(hydroxyphenyl)chlorin-like photosensitizer selectivity with folate-based targeted delivery. synthesis and in vivo delivery studies.
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pubmed:affiliation |
SRSMC, Structure et Réactivité des Systèmes Moléculaires Complexes, Nancy University, BP 239, F-54506 Vandoeuvre-lès-Nancy, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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