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Persistent URL
http://purl.org/net/epubs/work/64510
Record Status
Checked
Record Id
64510
Title
Micelles obtained by aggregation of gemini surfactants containing the CCK8 peptide and a gadolinium complex
Contributors
A Accardo (University of Naples )
,
D Tesauro (University of Naples )
,
A Morisco (University of Naples)
,
G Mangiapia (University of Naples )
,
M Vaccaro (University of Naples )
,
E Gianolio (University of Turin)
,
RK Heenan (STFC Rutherford Appleton Lab.)
,
L Paduano (University of Naples )
,
G Morelli (University of Naples )
Abstract
Two gemini surfactants, [C18CysL5CCK8]2 and [C18CysDTPAGlu]2, containing, respectively, the CCK8 peptide and the DTPAGlu chelating agent or its gadolinium complex have been prepared by linking lipophilic chains through a disulfide bond between two cysteine residues. The two surfactants aggregate in water solution forming pure or mixed micelles, with a critical micellar concentration in the 5 × 10?6–5 × 10?5 mol kg?1 range, as measured by fluorescence spectroscopy. As indicated by small-angle neutron scattering, the shape and size of the micelles are influenced by the temperature: increasing temperature leads to progressive reduction of the size of the supramolecular aggregates. Cylindrical structures found at lower temperatures (10–40 °C) evolve into ellipsoidal micelles at 50–80 °C. Furthermore, the surface-exposed CCK8 peptide changes its conformation above a transition temperature of approximately 45 °C, going from a ?-sheet to a random-coil structure, as indicated by circular dichroism measurements. The mixed aggregate obtained by coaggregation of the two gemini-based amphiphilic compounds, [C18CysDTPAGlu(Gd)]2 and [C18CysL5CCK8]2 in 70:30 molar ratio, represents the first example of a peptide-containing gemini surfactant as a potential target-selective contrast agent in MRI. In fact, it presents a high relaxivity value of the gadolinium complex, 21.5 mM?1 s?1, and the CCK8 bioactive peptide exposed on the external surface is therefore capable of selective targeting of the cholecystokinin receptors.
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ISIS
,
ISIS-LOQ
,
STFC
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Language
English (EN)
Type
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Year
Journal Article
J Biol Inorg Chem
14, no. 4 (2009): 587-599.
doi:10.1007/s00775-009-0472-1
2009
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