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Your search keyword '"Lavado, J."' showing total 3 results
Start Over Author "Lavado, J." Topic trehalose
3 results on '"Lavado, J."'

1. Trehalose-based Siamese twin amphiphiles with tunable self-assembling, DNA nanocomplexing and gene delivery properties.

Author

Carbajo-Gordillo AI, Rodríguez-Lavado J, Jiménez Blanco JL, Benito JM, Di Giorgio C, Vélaz I, Tros de Ilarduya C, Ortiz Mellet C, and García Fernández JM

Subjects
Animals, Cell Line, Chlorocebus aethiops, Humans, Mice, Plasmids metabolism, Nanostructures chemistry, Plasmids chemistry, Surface-Active Agents chemistry, Transfection methods, Trehalose chemistry
Abstract

An original family of multivalent vectors encompassing gemini and facial amphiphilicity, namely cationic Siamese twin surfactants, has been prepared from the disaccharide trehalose; molecular engineering lets us modulate the self-assembling properties and the topology of the nanocomplexes with plasmid DNA for efficient gene delivery in vitro and in vivo.

Published
2019
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2. Trehalose- and glucose-derived glycoamphiphiles: small-molecule and nanoparticle Toll-like receptor 4 (TLR4) modulators.

Author

Rodriguez Lavado J, Sestito SE, Cighetti R, Aguilar Moncayo EM, Oblak A, Lainšček D, Jiménez Blanco JL, García Fernández JM, Ortiz Mellet C, Jerala R, Calabrese V, and Peri F

Subjects
Animals, Endotoxins antagonists & inhibitors, Glycolipids pharmacology, HEK293 Cells drug effects, Humans, Macrophages drug effects, Metal Nanoparticles chemistry, Mice, Inbred C57BL, Signal Transduction drug effects, Structure-Activity Relationship, Surface-Active Agents pharmacology, Toll-Like Receptor 4 agonists, Toll-Like Receptor 4 antagonists & inhibitors, Glucose analogs & derivatives, Glycolipids chemical synthesis, Surface-Active Agents chemical synthesis, Toll-Like Receptor 4 metabolism, Trehalose analogs & derivatives
Abstract

An increasing number of pathologies have been linked to Toll-like receptor 4 (TLR4) activation and signaling, therefore new hit and lead compounds targeting this receptor activation process are urgently needed. We report on the synthesis and biological properties of glycolipids based on glucose and trehalose scaffolds which potently inhibit TLR4 activation and signaling in vitro and in vivo. Structure-activity relationship studies on these compounds indicate that the presence of fatty ester chains in the molecule is a primary prerequisite for biological activity and point to facial amphiphilicity as a preferred architecture for TLR4 antagonism. The cationic glycolipids here presented can be considered as new lead compounds for the development of drugs targeting TLR4 activation and signaling in infectious, inflammatory, and autoimmune diseases. Interestingly, the biological activity of the best drug candidate was retained after adsorption at the surface of colloidal gold nanoparticles, broadening the options for clinical development.

Published
2014
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3. Trehalose- and glucose-derived glycoamphiphiles: small-molecule and nanoparticle Toll-like receptor 4 (TLR4) modulators

Author

Stefania E. Sestito, Francesco Peri, Duško Lainšček, Roman Jerala, Carmen Ortiz Mellet, Roberto Cighetti, José M. García Fernández, Eva M. Aguilar Moncayo, Julio Rodriguez Lavado, José L. Jiménez Blanco, Valentina Calabrese, Alja Oblak, Rodriguez Lavado, J, Sestito, S, Cighetti, R, Aguilar Moncayo, E, Oblak, A, Lainšček, D, Jiménez Blanco, J, García Fernández, J, Ortiz Mellet, C, Jerala, R, Calabrese, V, Peri, F, and Universidad de Sevilla. Departamento de Química Orgánica

Subjects
Receptor Activation Process, LPS, Macrophage, Metal Nanoparticles, Medicinal chemistry, Drug development, Glycolipid, Surface-Active Agent, chemistry.chemical_compound, Metal Nanoparticle, Structure-Activity Relationship, Surface-Active Agents, Endotoxin, HEK293 Cell, In vivo, Drug Discovery, Gold nanoparticles, in vivo activity, Structure–activity relationship, Animals, Humans, TLR4, Receptor, HEK cells, Animal, Drug Discovery3003 Pharmaceutical Science, Medicine (all), Macrophages, Trehalose, Biological activity, Small molecule, Endotoxins, Mice, Inbred C57BL, Toll-Like Receptor 4, Lipid A, Glucose, HEK293 Cells, MD-2, chemistry, Biochemistry, Molecular Medicine, Signal transduction, Glycolipids, CD14, Human, Signal Transduction
Abstract

An increasing number of pathologies have been linked to Toll-like receptor 4 (TLR4) activation and signaling, therefore new hit and lead compounds targeting this receptor activation process are urgently needed. We report on the synthesis and biological properties of glycolipids based on glucose and trehalose scaffolds which potently inhibit TLR4 activation and signaling in vitro and in vivo. Structure-activity relationship studies on these compounds indicate that the presence of fatty ester chains in the molecule is a primary prerequisite for biological activity and point to facial amphiphilicity as a preferred architecture for TLR4 antagonism. The cationic glycolipids here presented can be considered as new lead compounds for the development of drugs targeting TLR4 activation and signaling in infectious, inflammatory, and autoimmune diseases. Interestingly, the biological activity of the best drug candidate was retained after adsorption at the surface of colloidal gold nanoparticles, broadening the options for clinical development.

Published
2014

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