Lipophilic pro-oligonucleotides are rapidly and efficiently internalized in HeLa cells.
Model t-Bu-SATE pro-dodecathymidines labeled with fluorescein and exhibiting various lipophilicities were evaluated for their uptake by cells in culture. Pro-oligonucleotides with appropriate lipophilicity were found to permeate across the HeLa cell membrane much more extensively than the control phosphorothioate oligo or than the hydrophilic pro-oligos. Fluorescence patterns of internalization were consistent with a diffusion mechanism resulting in the appearance of a uniform cytoplasmic distribution and nuclear accumulation, as confirmed by confocal microscopy.
Vivès
E
E
Laboratoire de Chimie Bio-Organique, Université Montpellier II, Place Eugène Bataillon, 34095 Montpellier Cedex 5, France.
Dell'Aquila
C
C
Bologna
J C
JC
Morvan
F
F
Rayner
B
B
Imbach
J L
JL
D000818:Animals; D002478:Cells, Cultured; D006224:Cricetinae; D003412:Cricetulus; D006367:HeLa Cells / Q000378:metabolism*; D006801:Humans; D008055:Lipids; D018613:Microscopy, Confocal; D008956:Models, Chemical; D009841:Oligonucleotides / Q000378:metabolism*; D009943:Organophosphorus Compounds; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013873:Thionucleotides / Q000378:metabolism*
D008055:Lipids; D009841:Oligonucleotides; D009943:Organophosphorus Compounds; D013873:Thionucleotides