| Literature DB >> 25084144 |
Stella Borrelli1, Michael S Christodoulou1, Ilaria Ficarra1, Alessandra Silvani1, Graziella Cappelletti2, Daniele Cartelli2, Giovanna Damia3, Francesca Ricci3, Massimo Zucchetti3, Franco Dosio4, Daniele Passarella5.
Abstract
The present study reports the preparation of a novel class of squalene conjugates with paclitaxel, podophyllotoxin, camptothecin and epothilone A. The obtained compounds are characterized by a squalene tail that makes them able to self-assemble in water, and by a drug unit connected via a disulfide-containing linker to secure the release inside the cell. All the obtained compounds were effectively able to self-assemble and to release the parent drug in vitro. Disulfide-containing paclitaxel-squalene derivative showed a similar biological activity when compared to the free drug. Immunofluorescence assay shows that this squalene conjugate enters A549 cells and stain microtubule bundles. The results described herein pave the way for different classes of squalene-based releasable nanoassemblies.Entities:
Keywords: Camptothecin; Epothilone A; Nanoassemblies; Paclitaxel; Podophyllotoxin; Squalene derivatives
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Year: 2014 PMID: 25084144 DOI: 10.1016/j.ejmech.2014.07.035
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514