Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers

The disaccharide trehalose is an autophagy inducer, but its pharmacological application is severely limited by its poor pharmacokinetics properties. Thus, trehalose was coupled via suitable spacers with squalene (in 1:2 and 1:1 stoichiometry) and with betulinic acid (1:2 stoichiometry), in order to...

Descripción completa

Detalles Bibliográficos
Autores principales: Colombo, Eleonora, Biocotino, Michele, Frapporti, Giulia, Randazzo, Pietro, Christodoulou, Michael S., Piccoli, Giovanni, Polito, Laura, Seneci, Pierfausto, Passarella, Daniele
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6723367/
https://www.ncbi.nlm.nih.gov/pubmed/31434235
http://dx.doi.org/10.3390/pharmaceutics11080422
_version_ 1783448751556263936
author Colombo, Eleonora
Biocotino, Michele
Frapporti, Giulia
Randazzo, Pietro
Christodoulou, Michael S.
Piccoli, Giovanni
Polito, Laura
Seneci, Pierfausto
Passarella, Daniele
author_facet Colombo, Eleonora
Biocotino, Michele
Frapporti, Giulia
Randazzo, Pietro
Christodoulou, Michael S.
Piccoli, Giovanni
Polito, Laura
Seneci, Pierfausto
Passarella, Daniele
author_sort Colombo, Eleonora
collection PubMed
description The disaccharide trehalose is an autophagy inducer, but its pharmacological application is severely limited by its poor pharmacokinetics properties. Thus, trehalose was coupled via suitable spacers with squalene (in 1:2 and 1:1 stoichiometry) and with betulinic acid (1:2 stoichiometry), in order to yield the corresponding nanolipid-trehalose conjugates 1-Sq-mono, 2-Sq-bis and 3-Be-mono. The conjugates were assembled to produce the corresponding nano-assemblies (NAs) Sq-NA1, Sq-NA2 and Be-NA3. The synthetic and assembly protocols are described in detail. The resulting NAs were characterized in terms of loading and structure, and tested in vitro for their capability to induce autophagy. Our results are presented and thoroughly commented upon.
format Online
Article
Text
id pubmed-6723367
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-67233672019-09-10 Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers Colombo, Eleonora Biocotino, Michele Frapporti, Giulia Randazzo, Pietro Christodoulou, Michael S. Piccoli, Giovanni Polito, Laura Seneci, Pierfausto Passarella, Daniele Pharmaceutics Article The disaccharide trehalose is an autophagy inducer, but its pharmacological application is severely limited by its poor pharmacokinetics properties. Thus, trehalose was coupled via suitable spacers with squalene (in 1:2 and 1:1 stoichiometry) and with betulinic acid (1:2 stoichiometry), in order to yield the corresponding nanolipid-trehalose conjugates 1-Sq-mono, 2-Sq-bis and 3-Be-mono. The conjugates were assembled to produce the corresponding nano-assemblies (NAs) Sq-NA1, Sq-NA2 and Be-NA3. The synthetic and assembly protocols are described in detail. The resulting NAs were characterized in terms of loading and structure, and tested in vitro for their capability to induce autophagy. Our results are presented and thoroughly commented upon. MDPI 2019-08-20 /pmc/articles/PMC6723367/ /pubmed/31434235 http://dx.doi.org/10.3390/pharmaceutics11080422 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Colombo, Eleonora
Biocotino, Michele
Frapporti, Giulia
Randazzo, Pietro
Christodoulou, Michael S.
Piccoli, Giovanni
Polito, Laura
Seneci, Pierfausto
Passarella, Daniele
Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title_full Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title_fullStr Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title_full_unstemmed Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title_short Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
title_sort nanolipid-trehalose conjugates and nano-assemblies as putative autophagy inducers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6723367/
https://www.ncbi.nlm.nih.gov/pubmed/31434235
http://dx.doi.org/10.3390/pharmaceutics11080422
work_keys_str_mv AT colomboeleonora nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT biocotinomichele nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT frapportigiulia nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT randazzopietro nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT christodouloumichaels nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT piccoligiovanni nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT politolaura nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT senecipierfausto nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers
AT passarelladaniele nanolipidtrehaloseconjugatesandnanoassembliesasputativeautophagyinducers

Ejemplares similares