Modification of carbon-based nanomaterials by polyglycerol: recent advances and applications

Modification of carbon nanomaterials by hyperbranched polyglycerol improves their properties.

Graphene based nanocomplexes can be rationally modified with a variety of functional compounds to improve therapeutic effectiveness including gene therapy

Graphene-family nanomaterials (GFNs)-based nanocomplexes have been hailed as a rising star in the field of nanomaterials. GFNs can be rationally modified with a variety of functional chemicals to improve therapeutic effectiveness. The active targeted drug delivery of GFNs is facilitated by conjugating with particular targeting ligands. A phototherapy method combining GFNs and PSs that may cause the formation of ROS with the help of NIR light irradiation, for example, has been shown to be effective in PTT. GFNs can cause cellular injuries such as cytoskeletal disorders, organelle dysfunction, protein corona damage, and damage to biological macromolecules after being absorbed into the human body. To decrease the toxicity of GFNs, biocompatible polymers such as peptides, PEG, hyperbranched polyglycerol, -cyclodextrin, and a variety of polysaccharides have been used. When combined with successful treatment methods, GFNs have the potential to be used in a range of clinical applications in biomedicine, including biosensing, bioimaging, tissue engineering, and medication delivery. However, success in translating GFNs-based nanocomplexes from the bench to the bedside remains a long way off.

Polysulfates Block SARS-CoV-2 Uptake via Electrostatic Interactions

<p><a>Here we report that negatively charged polysulfates can bind to the spike protein of SARS-CoV-2 via electrostatic interactions</a>. Using a plaque reduction assay, we compare inhibition of SARS-CoV-2 by heparin, pentosan sulfate, linear polyglycerol sulfate (LPGS) and hyperbranched polyglycerol sulfate (HPGS). Highly sulfated LPGS is the optimal inhibitor, with a half-maximal inhibitory concentration (IC₅₀) of 67 μg/mL (approx. 1.6 μM). This synthetic polysulfates exhibit more than 60-fold higher virus inhibitory activity than heparin (IC₅₀: 4084 μg/mL), along with much lower anticoagulant activity. Furthermore, in molecular dynamics simulations, we verified that LPGS can bind stronger to the spike protein than heparin, and that LPGS can interact even more with the spike protein of the new N501Y and E484K variants. Our study demonstrates that the entry of SARS-CoV-2 into host cells can be blocked via electrostatic interaction, therefore LPGS can serve as a blueprint for the design of novel viral inhibitors of SARS-CoV-2. </p>

Polysulfates Block SARS-CoV-2 Uptake via Electrostatic Interactions

<p><a>Here we report that negatively charged polysulfates can bind to the spike protein of SARS-CoV-2 via electrostatic interactions</a>. Using a plaque reduction assay, we compare inhibition of SARS-CoV-2 by heparin, pentosan sulfate, linear polyglycerol sulfate (LPGS) and hyperbranched polyglycerol sulfate (HPGS). Highly sulfated LPGS is the optimal inhibitor, with a half-maximal inhibitory concentration (IC₅₀) of 67 μg/mL (approx. 1.6 μM). This synthetic polysulfates exhibit more than 60-fold higher virus inhibitory activity than heparin (IC₅₀: 4084 μg/mL), along with much lower anticoagulant activity. Furthermore, in molecular dynamics simulations, we verified that LPGS can bind stronger to the spike protein than heparin, and that LPGS can interact even more with the spike protein of the new N501Y and E484K variants. Our study demonstrates that the entry of SARS-CoV-2 into host cells can be blocked via electrostatic interaction, therefore LPGS can serve as a blueprint for the design of novel viral inhibitors of SARS-CoV-2. </p>