Synthesis and structure–activity relationship study of saponin-based membrane fusion inhibitors against SARS-CoV-2

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We previously discovered that triterpenoid saponin platycodin D inhibits the SARS-CoV-2 entry to the host cell. Herein, we synthesized various saponin derivatives and established a structure–activity relationship of saponin-based antiviral agents against SARS-CoV-2. We discovered that the C3-glucose, the C28-oligosaccharide moiety that consist of (→3)-β-D-Xyl-(1 → 4)-α-L-Rham-(1 → 2)-β-D-Ara-(1 → ) as the last three sugar units, and the C16-hydroxyl group were critical components of saponin-based coronavirus cell entry inhibitors. These findings enabled us to develop minimal saponin-based antiviral agents that are equipotent to the originally discovered platycodin D. We found that our saponin-based antiviral agents inhibited both the endosomal and transmembrane protease serine 2-mediated cell surface viral entries. Cell fusion assay experiment revealed that our newly developed compounds inhibit the SARS-CoV-2 entry by blocking the fusion between the viral and host cell membranes. The effectiveness of the newly developed antiviral agents over various SARS-CoV-2 variants hints at the broad-spectrum antiviral efficacy of saponin-based therapeutics against future coronavirus variants.
Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
Issue Date
2022-10
Language
English
Article Type
Article
Citation

BIOORGANIC CHEMISTRY, v.127

ISSN
0045-2068
DOI
10.1016/j.bioorg.2022.105985
URI
http://hdl.handle.net/10203/297851
Appears in Collection
CH-Journal Papers(저널논문)
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