A5052516647- Immune Response and Inflammation
- Antimicrobial Peptides and Activities
- Pneumonia and Respiratory Infections
- Carbohydrate Chemistry and Synthesis
- Bryophyte Studies and Records
- Neurogenetic and Muscular Disorders Research
- Botany and Plant Ecology Studies
- RNA Interference and Gene Delivery
- Amyotrophic Lateral Sclerosis Research
- Immune Cell Function and Interaction
- Neonatal Respiratory Health Research
- Neuroinflammation and Neurodegeneration Mechanisms
- Bacterial Genetics and Biotechnology
- Lichen and fungal ecology
- Glycosylation and Glycoproteins Research
- Pediatric health and respiratory diseases
- Influenza Virus Research Studies
- Antibiotic Resistance in Bacteria
- Drug Transport and Resistance Mechanisms
- Galectins and Cancer Biology
Centre National de la Recherche Scientifique
2022
Ingénierie Moléculaire et Physiopathologie Articulaire
2022
Université de Lorraine
2022
University of Milano-Bicocca
2013-2017
University of Milan
2014
Abstract Dysregulated Toll-like receptor (TLR)-4 activation is involved in acute systemic sepsis, chronic inflammatory diseases, such as atherosclerosis and diabetes, viral infections, influenza infection. Thus, therapeutic control of the TLR4 signalling pathway major interest. Here we tested activity small-molecule synthetic antagonist, FP7, vitro on human monocytes monocyte-derived dendritic cells (DCs) vivo during virus infection mice. Our results indicate that FP7 antagonized secretion...
Abstract Monosaccharide lipid A mimetics based on a glucosamine core linked to two fatty acid chains and bearing one or phosphate groups have been synthesized. Compounds 1 2 , each with group, were practically inactive in inhibiting LPS‐induced TLR4 signaling cytokine production HEK‐blue cells murine macrophages, but compound 3 groups, was found be active efficiently signal both cell types. The direct interaction between the MD‐2 coreceptor investigated by NMR spectroscopy molecular...
Bryophytes produce rare and bioactive compounds with a broad range of therapeutic potential, many species are reported in ethnomedicinal uses. However, only few studies have investigated their potential as natural anti-inflammatory drug candidate compounds. The present study investigates the effects thirty-two bryophytes, including mosses liverworts, on Raw 264.7 murine macrophages stimulated lipopolysaccharide (LPS) or recombinant human peroxiredoxin (hPrx1). 70% ethanol extracts bryophytes...
An increasing number of pathologies have been linked to Toll-like receptor 4 (TLR4) activation and signaling, therefore new hit lead compounds targeting this process are urgently needed. We report on the synthesis biological properties glycolipids based glucose trehalose scaffolds which potently inhibit TLR4 signaling in vitro vivo. Structure-activity relationship studies these indicate that presence fatty ester chains molecule is a primary prerequisite for activity point facial...
We recently reported on the activity of cationic amphiphiles in inhibiting TLR4 activation and subsequent production inflammatory cytokines cells animal models. Starting from assumption that opportunely designed can behave as CD14/MD-2 ligands therefore modulate signaling, we present here a panel amphiphilic guanidinocalixarenes whose structure was computationally optimized to dock into MD-2 CD14 binding sites. Some these calixarenes were active inhibiting, dose-dependent way, LPS-stimulated...
Abstract Lipopolysaccharide (LPS), the main cell‐surface molecular constituent of Gram‐negative bacteria, is synthesized in inner membrane (IM) and transported to outer (OM) by Lpt (lipopolysaccharide transport) machinery. Neosynthesized LPS first flipped MsbA across IM, then OM seven proteins located IM (LptBCFG), periplasm (LptA), (LptDE). A functional essential bacterial viability requires correct placement leaflet. Therefore, biogenesis represents an ideal target for development novel...
Four novel calix[4]arene-based glycoclusters were synthesized by conjugating the saccharide units to macrocyclic scaffold using CuAAC reaction and long hydrophilic ethylene glycol spacers. Initially, two galactosylcalix[4]arenes prepared starting from calixarene cores which differ in relative dispositions of alkyne azido groups. Once most convenient synthetic pathway was selected, further lactosylcalix[4]arenes obtained, one cone, other 1,3-alternate structure. Preliminary studies...
The cationic glycolipid IAXO-102, a potent TLR4 antagonist targeting both MD-2 and CD14 co-receptors, has been used as scaffold to design new potential modulators fluorescent labels for the receptor complex (membrane TLR4.MD-2 dimer CD14). primary amino group of not involved in direct interaction with receptors, exploited covalently attach fluorescein (molecules 1 2) or link two molecules IAXO-102 through diamine diammonium spacers, obtaining 'dimeric' 3 4. structure-based rational compounds...
This study examines the effect of co-administration antimicrobial peptides and synthetic glycolipid FP7, which is active in inhibiting inflammatory cytokine production caused by TLR4 activation signaling. The two lipopolysaccharide (LPS)-neutralizing (a cecropin A-melittin hybrid peptide a human cathelicidin) enhances an order magnitude potency FP7 blocking signal. Interestingly, this not additional LPS neutralization peptides, because it also occurs if cells are stimulated plant lectin...