β-Cyclodextrins as affordable antivirals to treat coronavirus infection - 17/06/23
, Nuria Izquierdo-Useros a, j, ⁎
, Cristina Risco b, ⁎ 
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.
Il testo completo di questo articolo è disponibile in 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
Mappa
Vol 164
Articolo 114997- agosto 2023 Ritorno al numeroBenvenuto su EM|consulte, il riferimento dei professionisti della salute.
