Multiformin-Type Azaphilones Prevent SARS-CoV-2 Binding to ACE2 Receptor
- authored by
- 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.
- Organisation(s)
-
Institute of Organic Chemistry
Institute of Technical Chemistry
Centre of Biomolecular Drug Research (BMWZ)
Department of Cell Physiology and Biophysics
- External Organisation(s)
-
Hannover Medical School (MHH)
Huazhong Agricultural University
Helmholtz Centre for Infection Research (HZI)
Technische Universit盲t Braunschweig
- Type
- Article
- Journal
- Cells
- Volume
- 12
- No. of pages
- 13
- ISSN
- 2073-4409
- Publication date
- 25.12.2022
- Publication status
- Published
- Peer reviewed
- Yes
- ASJC Scopus subject areas
- General Biochemistry,Genetics and Molecular Biology
- Electronic version(s)
-
(Access:
Open)
