Cellular uptake of phosphorothioate oligonucleotide facilitated by cationic porphyrin: A microfluorescence study

• Published in: Biopolymers 2006-07, Vol.82 (4), p.325-328
• Main Authors: Kočišová, E., Praus, P., Mojzeš, P., Sureau, F., Štěpánek, J., Seksek, O., Turpin, P. Y.
• Format: Article
• Language: English
• Subjects: 3T3 Cells; Animals; antisense; cellular uptake; Mice; microimaging; oligonucleotide; Oligonucleotides, Antisense - chemistry; Oligonucleotides, Antisense - metabolism; porphyrin; Porphyrins - metabolism; Spectrometry, Fluorescence - methods; time-resolved fluorescence
• ISSN: 0006-3525; 1097-0282
• DOI: 10.1002/bip.20495

Cationic 5,10,15,20‐tetrakis (1‐methyl‐4‐pyridyl) porphyrin was tested as a delivery agent for oligonucleotides. By using fluorescence microimaging, it has been shown that complexation of the porphyrin to the phosphorothioate analog of dT15 labeled by rhodamine enabled its nonendocytic penetration into the cell and regular distribution in the cytoplasm and preferentially into the nucleus. Time‐resolved microfluorescence spectroscopy revealed that the oligonucleotide integrity was kept. A small fraction of the porphyrin molecules seems to undergo change of the binding mode after internalization, probably due to duplex formation between the oligonucleotide and its cellular target sequences, or due to dissociation of the porphyrin from the oligonucleotide and subsequent interactions in the cellular environment © 2006 Wiley Periodicals, Inc. Biopolymers 82:325–328, 2006 This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at [e-mail]