Synthesis and Antitumor Application of Antiangiogenetic Gold Nanoclusters

Abstract

Conventional antiangiogenetic inhibitors suffered from poor delivery problems that result in unsatisfactory antitumor treatment efficacy. Although the liposomes or nanomaterial-based delivery systems can improve the therapeutic efficacy of antiangiogenic molecules, the assembly process is far too complex. Herein, a nanomaterial or a new nanodrug that could work without the help of a carrier and could be easily synthesized is needed. Au nanoclusters (AuNCs) are a kind of ideal nanostructures that could spontaneously enter into the cell and could be synthesized by a relatively easy one-pot method. Here, changing the traditional ligand glutathione (GSH) into an anti-Flt1 peptide (AF) has enriched the newly synthesized AF@AuNCs with targeted antiangiogenic properties. Based on the specific binding between AF and vascular endothelial growth factor receptor 1 (VEGFR1), the interaction between VEGFR1 and its ligands could be blocked. Furthermore, the expression of VEGFR2 could be downregulated. Compared with pure AF peptide- and GSH-participated AuNCs (GSH@AuNCs), AF@AuNCs were more effective in inhibiting both tube formation and migration of the endothelial cells in vitro. Furthermore, the in vivo chick embryo chorioallantoic membrane (CAM) experiment and antitumor experiment were conducted to further verify the enhanced antiangiogenesis and tumor inhibition effect of AF@AuNCs. Our findings provide promising evidence of a carrier-free nanodrug for tumors and other vascular hyperproliferative diseases.

Origin of luminescence properties and synthetic methods for gold- and bimetallic gold-based nanomaterials

“…This template-based synthetic methodology is unique compared to earlier reported methods given that it does not require additional reducing agents. 161 Jain et al reported the synthesis of BSA-coated AuNCs with bright red fluorescence in the dark overnight. The gold nanoclusters synthesized using this method showed a good quantum yield and brightness.…”

The Peptide Functionalized Inorganic Nanoparticles for Cancer-Related Bioanalytical and Biomedical Applications

“…The tumor inhibition abilities antiangiogenic agents can be reinforced when they are loaded on the NPs. Several peptide-functionalized NPs with antiangiogenic properties have been employed for directly inhibiting pathological angiogenesis [ 177 , 178 , 179 , 180 , 181 ]. Very recently, Li and colleagues synthesized an anti-Flt1 peptide (AF, CGNQWFI) functionalized AuNC (ca.…”

“…Very recently, Li and colleagues synthesized an anti-Flt1 peptide (AF, CGNQWFI) functionalized AuNC (ca. 2 nm in diameter) with targeted antiangiogenic property (as shown in Figure 7 ) [ 181 ]. The AF@AuNCs exhibit effectiveness in inhibiting both tube formation and migration of the endothelial cells in vitro since the interaction between vascular endothelial growth factor receptor 1 (VEGFR1) and its ligands could be blocked by AF and the expression of VEGFR2 could be downregulated (as shown in Figure 7 a).…”

“…Data represent means ± SD ( n = 3). * p < 0.05 and *** p < 0.001, data with significant difference (Adapted from Li et al 2021 [ 181 ], Copyright 2021 American Chemical Society and reproduced with permission.).…”

A Simple Schiff Base as Fluorescent Probe for Detection of Al3+ in Aqueous Media and its Application in Cells Imaging

“…Fluorescent gold nanoclusters (AuNCs) have been extensively used in chemo/biosensing and imaging due to their low toxicity, good biocompatibility, easy synthesis, excellent chemical stability and photostability. Despite many small biomolecules, such as glutathione, tyrosine, L-proline and methionine have been applied in the preparation of AuNCs [21][22][23][24][25][26][27], a facile and rapid synthesis of uorescent AuNCs still remains a great challenge.…”