β-Cyclodextrins as affordable antivirals to treat coronavirus infection - 17/06/23



Abstract |
The SARS-CoV-2 pandemic made evident that there are only a few drugs against coronavirus. Here we aimed to identify a cost-effective antiviral with broad spectrum activity and high safety profile. Starting from a list of 116 drug candidates, we used molecular modelling tools to rank the 44 most promising inhibitors. Next, we tested their efficacy as antivirals against α and β coronaviruses, such as the HCoV-229E and SARS-CoV-2 variants. Four drugs, OSW-1, U18666A, hydroxypropyl-β-cyclodextrin (HβCD) and phytol, showed in vitro antiviral activity against HCoV-229E and SARS-CoV-2. The mechanism of action of these compounds was studied by transmission electron microscopy and by fusion assays measuring SARS-CoV-2 pseudoviral entry into target cells. Entry was inhibited by HβCD and U18666A, yet only HβCD inhibited SARS-CoV-2 replication in the pulmonary Calu-3 cells. Compared to the other cyclodextrins, β-cyclodextrins were the most potent inhibitors, which interfered with viral fusion via cholesterol depletion. β-cyclodextrins also prevented infection in a human nasal epithelium model ex vivo and had a prophylactic effect in the nasal epithelium of hamsters in vivo. All accumulated data point to β-cyclodextrins as promising broad-spectrum antivirals against different SARS-CoV-2 variants and distant alphacoronaviruses. Given the wide use of β-cyclodextrins for drug encapsulation and their high safety profile in humans, our results support their clinical testing as prophylactic antivirals.
Le texte complet de cet article est disponible en PDF.Graphical Abstract |
Highlights |
• | HβCD inhibits SARS-CoV-2 replication in Calu-3 pulmonary cells. |
• | β-CDs interfere with SARS-CoV-2 viral fusion via cholesterol depletion. |
• | β-CDs interfere with coronavirus infection by altering cell membranes. |
• | β-CDs prevent infection in a human nasal epithelium model. |
• | β-CDs have a prophylactic effect in the nasal epithelium of hamsters in vivo. |
Keywords : SARS-CoV-2, COVID-19, Coronavirus, Antiviral, Drug repurposing, Cyclodextrin, β-cyclodextrin
Plan
Vol 164
Article 114997- août 2023 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.