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Cholesterol-based nucleolipid-ruthenium complex stabilized by lipid aggregates for antineoplastic therapy.
- Source :
-
Bioconjugate chemistry [Bioconjug Chem] 2012 Apr 18; Vol. 23 (4), pp. 758-70. Date of Electronic Publication: 2012 Mar 21. - Publication Year :
- 2012
-
Abstract
- A novel ruthenium complex, linked to a cholesterol-containing nucleolipid (named ToThyCholRu), stabilized by lipid aggregates for antineoplastic therapy is presented. In order to retard the degradation kinetics typically observed for several ruthenium-based antineoplastic agents, ToThyCholRu is incorporated into a liposome bilayer formed by POPC. The resulting nanoaggregates contain up to 15% in moles of the ruthenium complex, and are shown to be stable for several weeks. The liposomes host the ruthenium-nucleolipid complex with the metal ion surrounded by POPC lipid headgroups and the steroid moiety inserted in the more external acyl chain region. These ruthenium-containing liposomes are more effective in inhibiting the growth of cancer cells than a model NAMI-A-like ruthenium complex, prepared for a direct evaluation of their anti-proliferative activity. These results introduce new perspectives in the design of innovative transition-metal-based supramolecular systems for anticancer drug vectorization.<br /> (© 2012 American Chemical Society)
- Subjects :
- Cell Line, Tumor
Cell Proliferation drug effects
Drug Stability
Humans
Neutron Diffraction
Scattering, Small Angle
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cholesterol chemistry
Organometallic Compounds chemistry
Organometallic Compounds pharmacology
Ruthenium chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4812
- Volume :
- 23
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioconjugate chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22369596
- Full Text :
- https://doi.org/10.1021/bc200565v