Multiformin-Type Azaphilones Prevent SARS-CoV-2 Binding to ACE2 Receptor
- verfasst von
- Linda Jansen-Olliges, Shambhabi Chatterjee, Lili Jia, Frank Stahl, Christian B盲r, Marc Stadler, Frank Surup, Carsten Zeilinger
- Abstract
Protein microarray screenings identified fungal natural products from the azaphilone family as potent inhibitors of SARS-CoV-2 spike protein binding to host ACE2 receptors. Cohaerin F, as the most potent substance from the cohaerin group, led to more than 50% less binding of ACE2 and SARS-CoV-2 spike protein. A survey for structurally related azaphilones yielded the structure elucidation of six new multiformins E鈥揓 (10鈥�15) and the revision of the stereochemistry of the multiformins. Cohaerin and multiformin azaphilones (1鈥�5, 8, 12) were assessed for their activity in a cell-based infection assay. Calu-3 cells expressing human ACE2 receptor showed more than 75% and 50% less infection by SARS-CoV-2 pseudotyped lentivirus particles after treatment with cohaerin C (1) and cohaerin F (4), respectively. Multiformin C (8) and G (12) that nearly abolished the infection of cells. Our data show that multiformin-type azaphilones prevent the binding of SARS-CoV-2 to the cell entry receptor ACE2.
- Organisationseinheit(en)
-
Institut f眉r Organische Chemie
Institut f眉r Technische Chemie
Zentrum f眉r Biomolekulare Wirkstoffe (BMWZ)
Abteilung Zellphysiologie und Biophysik
- Externe Organisation(en)
-
Medizinische Hochschule Hannover (MHH)
Huazhong Agricultural University
Helmholtz-Zentrum f眉r Infektionsforschung GmbH (HZI)
Technische 鲍苍颈惫别谤蝉颈迟盲迟 Braunschweig
- Typ
- Artikel
- Journal
- Cells
- Band
- 12
- Anzahl der Seiten
- 13
- ISSN
- 2073-4409
- Publikationsdatum
- 25.12.2022
- Publikationsstatus
- 痴别谤枚蹿蹿别苍迟濒颈肠丑迟
- Peer-reviewed
- Ja
- ASJC Scopus Sachgebiete
- Allgemeine Biochemie, Genetik und Molekularbiologie
- Elektronische Version(en)
-
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