Development of Broad-spectrum β-cyclodextrins-Based Nanomaterials Against Influenza Viruses

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Cyclodextrins as antivirals? Why not?

Caroline Tapparel Vu, Francesco Stellacci and colleagues from EPFL and University of Geneva created a groundbreaking molecule, CD-SA, that mimics flu virus receptors to fight off multiple influenza strains effectively! 🦠💥 Our studies show CD-SA outperforms existing treatments like Oseltamivir, offering a new hope against flu with fewer chances of resistance when coupled with IFN λ1. Exciting results from lab to mice models prove its potent antiviral powers! 🚀🔬


Development of Broad-spectrum β-cyclodextrins-Based Nanomaterials Against Influenza Viruses | bioRxiv

Combined use of nanobody, cyclodextrin and quercetin for protection from enveloped viruses

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Fascinating antiviral application of cyclodextrins against SARS-COV2. You can find specific nanobodies against different target antigens such as the spike protein of the SARS-CoV-2 virus and or to the ACE2 receptor at the host cell surface, binds to the virus or the ACE2 receptor at the host cell plasma membrane, preventing entry of the SARS-CoV-2 virus. The nanobodies comprise a cyclodextrin; a zinc ionophore; a zinc-containing compound; and, benzalkonium.

WO2024035526 COMBINED USE OF NANOBODY, CYCLODEXTRIN AND QUERCETIN FOR PROTECTION FROM ENVELOPED VIRUSES (wipo.int)

Synthesis and Preliminary Evaluation of an ASGPr-Targeted Polycationic β-Cyclodextrin Carrier for Nucleosides and Nucleotides

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As our interest to use cyclodextrin in genetherapy as superior drugdelivery tools continue, we welcome papers like this, where cationic CD polymers are used for nucleotide formulation.
Leonard Wiebe and coworkers from University of Alberta development a carrier designed to effect selective transmembrane internalization of nucleotides via the asialoglycoprotein receptor.

Pharmaceutics | Free Full-Text | Synthesis and Preliminary Evaluation of an ASGPr-Targeted Polycationic β-Cyclodextrin Carrier for Nucleosides and Nucleotides (mdpi.com)


Composition for the prevention of infection by SARS-COV-2

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Today’s cyclodextrin is interesting both from the application and the formulation point of view. Mouth rinses and mouthwashes are not so common with CDs, yet certainly they are gainly space in dental hygiene. Yet in this invention from MAGI Euregio, not only the comlex forming, but also antiviral (specifically anti covid) properties are also exploited.

The composition includes α-cyclodextrin and hydroxytyrosol and is effective (even proven clinically) in preventing SARS-CoV-2 infection, whereas also effective in contrasting halitosis in subjects that wear a mask for a prolonged period.

Espacenet – Composition for the prevention of infection by SARS-COV-2


Cyclodextrin-based anti-microbial therapy

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Cyclodextrin-based antimicrobial/antiviral therapy discovered at the University of Southern California
A rapidly deployable nanoscale biodegradable system using hydroxypropyl beta cyclodextrin-based combination product is presented as an agnostic barrier blocking pathogenic microbes that has localized on the mucocutaneous lining of the conjunctiva, mouth and nose, lung, or gastrointestinal tract. The cyclodextrin may bind the viral particles and/or disrupt viral entry mechanisms by removing cholesterol from viral particles to reduce infectivity. Cyclodextrins also may facilitate the removal of the viral cholesterol molecules, thus rendering them less viable.
Stan Louie; Gianluca Lazzi; Jean-Marie Bouteiller

You can read the patent on Espacenet!

Hydroxypropyl-β-Cyclodextrin Depletes Membrane Cholesterol and Inhibits SARS-CoV-2 Entry into HEK293T-ACEhi Cells

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Vaccination has drastically decreased mortality due to coronavirus disease 19 (covid19), but not the rate of acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Alternative strategies, such as inhibition of virus entry by interference with angiotensin-I-converting enzyme 2 (ACE2) receptors could be warranted. Cyclodextrins (CDs) are cyclic oligosaccharides that are able to deplete cholesterol from membrane lipid rafts, causing ACE2 receptors to relocate to areas devoid of lipid rafts. To explore the possibility of reducing SARS-CoV-2 entry, hydroxypropyl-β-cyclodextrin (HPβCD) was tested in a HEK293T-ACE2hi cell line stably overexpressing human ACE2 and Spike-pseudotyped SARS-CoV-2 lentiviral particles. Exposure of HEK293T-ACEhi cells to concentrations of HPβCD starting from 2.5 mM to 10 mM showed a concentration-dependent reduction of approximately 50% of the membrane cholesterol content. In addition, incubation of HEK293T-ACEhi cells with HIV-S-CoV-2 pseudotyped particles in the presence of increasing concentrations of HPβCD (from 0.1 to 10 mM) displayed a concentration-dependent effect on SARS-CoV-2 entry efficiency. These data indicate that HPβCD is a candidate for use as a SARS-CoV-2 prophylactic agent.

Silvia Alboni, Valentina Secco, Bianca Papotti, Antonietta Vilella, Maria Pia Adorni, Francesca Zimetti, Laurent Schaeffer, tascedda fabio, Michele Zoli, Pascal Leblanc, Erica Villa

See the full article here: Hydroxypropyl-β-Cyclodextrin Depletes Membrane Cholesterol and Inhibits SARS-CoV-2 Entry into HEK293T-ACEhi Cells

U.S. Food and Drug Administration approved Arexvy, the first respiratory syncytial virus (RSV) vaccine

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FDA Approves First Respiratory Syncytial Virus (RSV) Vaccine
Today, the U.S. FDA approved Arexvy, the first respiratory syncytial virus (RSV) vaccine approved for use in the United States. Arexvy is approved for the prevention of lower respiratory tract disease caused by RSV in individuals 60 years of age and older. RSV is a highly contagious virus that causes infections of the lungs and breathing passages in individuals of all age groups. RSV circulation is seasonal, typically starting during the fall and peaking in the winter. In older adults, RSV is a common cause of lower respiratory tract disease, which affects the lungs and can cause life-threatening pneumonia and bronchiolitis (swelling of the small airway passages in the lungs). According to the U.S. Centers for Disease Control and Prevention, each year in the U.S., RSV leads to approximately 60,000-120,000 hospitalizations and 6,000-10,000 deaths among adults 65 years of age and older. 
GSK’s RSVPreF3 (Arexvy), is a recombinant product that contains a glycoprotein antigen based on the RSV A subgroup and is given with a proprietary adjuvant—the same one in GSK‘s Shingrix shingles (herpes zoster) vaccine—designed to boost the immune response.

See the FDA annucement here

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

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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

See the full article here

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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