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Author Spotlight: Improving the Production of Self-Assembling Fibers and Peptide Hydrogels for Superior Biocompatibility
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Self-Assembly of Anti-Inflammatory Peptide Amphiphiles for Mucosal Health
María José Gómara1, Ignacio Pérez-Pomeda2, Ramon Pons3
1Unit of Synthesis and Biomedical Applications of Peptides, Institute of Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona, Spain.
Chembiochem : a European Journal of Chemical Biology
|April 8, 2026
Summary
Broad spectrum anti-inflammatory peptide amphiphiles (AIF-PAs) show potential for treating mucosal inflammation and preventing HIV. These novel compounds exhibit anti-inflammatory effects and HIV inhibition ex vivo, with low mucosal permeation for targeted delivery.
Area of Science:
- Biomaterials Science
- Immunology
- Virology
Background:
- Chronic mucosal inflammation, such as in Crohn's disease, presents significant therapeutic challenges.
- Human immunodeficiency virus (HIV) transmission and persistence at mucosal sites require innovative prevention and treatment strategies.
Purpose of the Study:
- To develop and characterize novel anti-inflammatory peptide amphiphiles (AIF-PAs) for mucosal applications.
- To evaluate the anti-inflammatory and anti-HIV efficacy of AIF-PAs in relevant ex vivo models.
- To assess the self-assembly, membrane interactions, and mucosal permeation of AIF-PAs.
Main Methods:
- Solid-phase peptide chemistry was employed to synthesize novel lipopeptides.
- Ex vivo studies utilized colorectal tissue explants from Crohn's disease patients.
- Physicochemical characterization included self-aggregation, conformational analysis (β-sheet, random coil), and nanostructure morphology assessment.
- Interactions with model membranes and epithelial cells were investigated.
- Permeability assays were conducted using epithelial cell monolayers.
Main Results:
- AIF-PAs demonstrated downregulation of pro-inflammatory profiles in Crohn's disease tissue ex vivo.
- Sub-micromolar IC50 values for HIV inhibition were achieved in ex vivo colorectal tissue models.
- Peptide net charge influenced self-aggregation and nanostructure conformation (neutral peptides formed β-sheets, cationic peptides adopted random coils).
- Cationic, amphiphilic AIF-PAs effectively bound to and localized within lipid bilayers and cell membranes.
- AIF-PAs exhibited low mucosal permeation, minimizing systemic absorption and concentrating activity at the mucosal surface.
Conclusions:
- AIF-PAs represent a promising peptide-based therapeutic strategy for chronic mucosal inflammation and HIV prevention.
- The self-assembly properties and charge-dependent conformations of AIF-PAs enable targeted delivery and retention at mucosal sites.
- The low mucosal permeation potential of AIF-PAs enhances their safety profile by reducing systemic exposure.
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