Well-Defined Heparin Mimetics Can Inhibit Binding of the Trimeric Spike of SARS-CoV-2 in a Length-Dependent Manner

carbohydrates, ,

Well-defined heparin mimetics that could inhibit the binding of the SARS-CoV-2 spike or RBD to immobilized heparin or to Vero E6 cells. The inhibitory potency increased with increasing chain length, and a compound composed of four sulfated hexasaccharides linked by triazoles had a similar potency as unfractionated heparin. The heparin mimetics exhibit no or reduced binding to antithrombin-III and platelet factor 4, respectively, which are associated with side effects.

Utrecht University – Roosmarijn van der Woude, Robert de Vries et al
The University of Georgia – Lin Liu et al

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Veklury® (remdesivir) formulations inhibit initial membrane-coupled events of SARS-CoV-2 infection due to their sulfobutylether-β-cyclodextrin content

carbohydrates, drug delivery,

It has always been a bit of a mystery that given the antiviral effect of certain cyclodextrin, we can attribute all the antiviral effect of Veklury to remdesivir, which takes 3% of the formulation or maybe SBECD (97% of the formulation) also has some role. Researchers from University of Debrecen explore those questions.
Veklury® and different cholesterol-depleting cyclodextrins (CDs) reduced the binding of the spike receptor binding domain to ACE2 and spike trimer internalization for Wuhan-Hu-1, Delta, and Omicron variants. Correlations of these effects with cholesterol-dependent changes in membrane structure and decreased, lipid raft-dependent ACE2-TMPRSS2 interaction establish that SBECD is not simply a vehicle but also an effector in Veklury® due to its cholesterol-depleting potential.
Gyorgy Panyi, Florina Zakany et al.

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Asterivir develops CD-based broad-spectrum antiviral

Today's cyclodextrin, , ,

New kid on the block: Asterivir’s website has just gone live. Asterivir – a spinout from EPFL (École Polytechnique fédérale de Lausanne) – develops CD-based broad spectrum antivirals lead by Francesco Stellacci, Paulo Jacob Silva and Oscar Buset. The initial findings of the company were published earlier (Caroline Tapparel Vu et al. )
The website contains nice video graphics of the mechanism of action, which is worth checking!

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Identification of a βCD-Based Hyper-Branched Negatively Charged Polymer as HSV-2 and RSV Inhibitor

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Cyclodextrin derivatives were demonstrated to be endowed with intrinsic antiviral action against several viruses (herpes, HIV, RSV, influenza, covid19, etc.). In this great work from Rachele Francese, Francesco Trotta, Claudio Cecone, Matteo Constantino, Gjylije Hoti, Pierangiola Bracco, and David Lembo from the University of Turin, four water-soluble hyper-branched beta cyclodextrin anionic polymer were screened against herpes simplex virus (HSV-2), respiratory syncytial virus (RSV), rotavirus (HRoV), and influenza virus (FluVA). The results suggest that the polymer virucidal activity against RSV can be exploited to produce new antiviral materials to counteract the virus dissemination through the air or direct contact.

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