Enhanced Tumor Targeting and Photocytotoxicity of Folate–Poly(ethylene glycol)–Chlorin Photosensitizer Mediated by Folate Receptor

Enhanced Tumor Targeting and Photocytotoxicity of Folate–Poly(ethylene glycol)–Chlorin Photosensitizer Mediated by Folate Receptor

A targeting and water-soluble photosensitizer folate–PEG–chlorin (I) has been synthesized and characterized. The uptake of conjugate I by HeLa and Hep-2 cells was much higher than the uptake by A549 cells, and can be inhibited by folic acid. Conjugate I exhibited much lower cytotoxicity against HeLa...

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Veröffentlicht in:Chemistry letters 2013-02, Vol.42 (2), p.130-131
Hauptverfasser: Li, Donghong, Li, Pengxi, Jiang, Zonglin, Guo, Linfeng
Format: Artikel
Sprache:eng
Schlagworte:
Apoptosis
Conjugates
Folic acid
Membranes
Mitochondria
Receptors
Tumors
Uptakes
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Zusammenfassung:A targeting and water-soluble photosensitizer folate–PEG–chlorin (I) has been synthesized and characterized. The uptake of conjugate I by HeLa and Hep-2 cells was much higher than the uptake by A549 cells, and can be inhibited by folic acid. Conjugate I exhibited much lower cytotoxicity against HeLa and Hep-2 cells but significant photocytotoxicity. Conjugate I preferentially located in mitochondria of the Hep-2 cells, and conjugate I–PDT induced a loss of mitochondrial membrane potential and then the apoptosis of Hep-2 cells.
ISSN:0366-7022
1348-0715
DOI:10.1246/cl.2013.130