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Solid-phase Synthesis of Folate-Chlorin Conjugates for Selective Photodynamic Therapy and the Effect of Linker Variation.
- Source :
- Bulletin of the Korean Chemical Society; Dec2016, Vol. 37 Issue 12, p2036-2040, 5p
- Publication Year :
- 2016
-
Abstract
- Here, we evaluated the effect of linkers conjugating a chlorin-based photosensitizer, 2-[1-hexyloxyethyl]-2-devinyl pyropheophorbide-a ( HPPH), and folic acid to target cancer cells. Folate- HPPH conjugates with peptide, polyethylene glycol ( PEG), peptoid, or 7-aminoheptanoic acid ( AHA) linkers were synthesized on a solid-phase and evaluated for photodynamic therapy ( PDT) efficacy. Compared to free HPPH, the folate-linker- HPPHs were effectively internalized into tumor cells and exhibited superior PDT effect upon irradiation. Tumor-targeting PDT efficacy was influenced by linker variation, with in vitro photocytotoxicities of peptide > PEG > AHA > peptoid, paralleling water solubility of the linkers. Thus, linker choice significantly affects targeted PDT efficacy providing useful information for linker design. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 02532964
- Volume :
- 37
- Issue :
- 12
- Database :
- Complementary Index
- Journal :
- Bulletin of the Korean Chemical Society
- Publication Type :
- Academic Journal
- Accession number :
- 120127039
- Full Text :
- https://doi.org/10.1002/bkcs.11028