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Cholesteryl‐Functionalized ADNF‐9 Peptide: Enhanced Membrane Transport Through Mouse Neuroblastoma Neuro‐2a Cells
Author(s) -
Katsari Efthalia,
Zikos Christos,
Tziveleka LetoAikaterini,
ParavatouPetsotas Maria,
Paleos Constantinos M.
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2012.01381.x
Subject(s) - peptide , neurotrophic factors , chemistry , neurotrophin , in vitro , cytotoxicity , biochemistry , intracellular , neuroblastoma , glial cell line derived neurotrophic factor , cell culture , biology , receptor , genetics
A cholesteryl‐functionalized derivative of activity dependent neurotrophic factor‐9 peptide (a nine amino acid core peptide of activity‐dependent neurotrophic factor, acting against Alzheimer’s disease) was synthesized aiming at the improvement of its bioavailability. Therefore, its uptake was comparatively investigated with that of its parent peptide by employing mouse neuroblastoma Neuro‐2a cells. Owing to the hydrophobic character of this cholesteryl‐functionalized peptide, it exhibited enhanced permeability and intracellular uptake while it also retained its low cytotoxicity at concentrations up to 1 μ m . FACS analysis also revealed that when Neuro‐2a cells were treated with this activity dependent neurotrophic factor‐9 derivative, at a concentration of 50 n m , an almost 100% uptake was obtained. In addition, in vitro biological activity experiments showed that the functionalized peptide retained its neurotrophic activity at femtomolar concentration range.