Lactose-Modified Chitosan Gold(III)-PEGylated Complex-Bioconjugates: From Synthesis to Interaction with Targeted Galectin-1 Protein

Abstract

Galectins (Gal) are a family of glycan-binding proteins characterized by their affinity for β-galactosides. Galectin-1 (Gal-1), a dimeric lectin with two galactoside-binding sites, regulates cancer progression and immune responses. Coordination chemistry has been engaged to develop versatile multivalent neoglycoconjugates for binding Gal-1. In this study we report a fast and original method to synthesize hybrid gold nanoparticles in which a hydrochloride lactose-modified chitosan, named CTL, is mixed with dicarboxylic acid-terminated polyethylene glycol (PEG), leading to shell-like hybrid polymer-sugar-metal nanoparticles (CTL-PEG-AuNPs). The aim of this paper is to preliminarily study the interaction of the CTL-PEG-AuNPs with a target protein, namely, Gal-1, under specific conditions. The molecular interaction has been measured by Transmission Electron Microscopy (TEM), UV-vis, and Raman Spectroscopy on a large range of Gal-1 concentrations (from 0 to 10 M). We observed that the interaction was strongly dependent on the Gal-1 concentration at the surface of the gold nanoparticles.

Aptamer Grafting onto (on) and into (in) Pegylated Gold Nanoparticles: Physicochemical Characterization and In vitro Cytotoxicity Investigation in Renal Cells

“…Previously, Spadavecchia et al have synthetized and conjugated pegylated gold nanoparticles (PEG-AuNPs) with biomolecules (protein, antibody, peptides, aptamer) by several grafting methodologies [2,5,7,31]. Chemical-physical evaluations and biological "in vitro" studies of biomolecules onto pegylated-gold-nanoparticles have successfully showed a large influence in its therapeutic activity [32][33][34][35].…”

CTL–doxorubicin (DOX)–gold complex nanoparticles (DOX–AuGCs): from synthesis to enhancement of therapeutic effect on liver cancer model

“…13 The role played by CTL is investigated here since it was already shown to stabilize gold clusters in CTL-PEGylated gold nanoparticles, and to target the Galectin-1 (Gal-1) protein. 14,15 Gal-1 is in fact considered a novel therapeutic target for cancer due to its widespread presence in the extracellular medium of different tumors. 16 The therapeutic effects in vivo of DOX-AuGCs were evaluated in the HepG2-induced liver cancer of nude mice in comparison with a negative control group (mice treated with a saline solution), and mice treated with the polymer CTL per se and with DOX in PEG-AuNPs (DOX-Au nanoparticles without CTL).…”

Glycosylated-Chitosan Derivatives: A Systematic Review

“…Given the well-documented bioactivity of this engineered polymer, these findings suggest a possible application of the glycosylated chitosanbased drug delivery system as scavenger and bioactive carrier for drug therapeutics at confined inflamed sites. Furthermore, the lactose-derivative of chitosan has been recently employed in forming gold-based nanoparticles with potential translation of present systems in both treatments of tumors and glucose sensor [52,53]. Vårum and co-workers synthetized a chitosan derivative substituted with sugar oligomers, in which depolymerized chitosans were reductively N-alkylated with the trimer A-A-M.…”