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Cell Biosci . Umbelliferone and eriodictyol suppress the cellular entry of SARS-CoV-2

tetano

Editor, Senior Moderator
Cell Biosci


. 2023 Jun 28;13(1):118.
doi: 10.1186/s13578-023-01070-y. Umbelliferone and eriodictyol suppress the cellular entry of SARS-CoV-2

Fang-Ju Cheng[SUP] #[/SUP][SUP] 1 2 3 [/SUP], Chien-Yi Ho[SUP] #[/SUP][SUP] 4 5 6 [/SUP], Tzong-Shiun Li[SUP] #[/SUP][SUP] 7 8 [/SUP], Yeh Chen[SUP] 9 [/SUP], Yi-Lun Yeh[SUP] 1 2 [/SUP], Ya-Ling Wei[SUP] 1 2 [/SUP], Thanh Kieu Huynh[SUP] 1 2 [/SUP], Bo-Rong Chen[SUP] 1 2 3 [/SUP], Hung-Yu Ko[SUP] 10 [/SUP], Chen-Si Hsueh[SUP] 11 [/SUP], Ming Tan[SUP] 2 [/SUP], Yang-Chang Wu[SUP] 12 13 14 [/SUP], Hui-Chi Huang[SUP] 15 [/SUP], Chih-Hsin Tang[SUP] 3 [/SUP], Chia-Hung Chen[SUP] 3 16 17 [/SUP], Chih-Yen Tu[SUP] 3 16 17 [/SUP], Wei-Chien Huang[SUP] 18 19 20 21 22 [/SUP]



Affiliations
Abstract

Background: Artemisia argyi (A. argyi), also called Chinese mugwort, has been widely used to control pandemic diseases for thousands of years since ancient China due to its anti-microbial infection, anti-allergy, and anti-inflammation activities. Therefore, the potential of A. argyi and its constituents in reducing the infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was investigated in this study.
Results: Among the phytochemicals in A. argyi, eriodictyol and umbelliferone were identified to target transmembrane serine protease 2 (TMPRSS2) and angiotensin-converting enzyme 2 (ACE2) proteins, the essential factors for the cellular entry of SARS-CoV-2, in both FRET-based enzymatic assays and molecular docking analyses. These two ingredients of A. argyi suppressed the infection of ACE2-expressed HEK-293 T cells with lentiviral-based pseudo-particles (Vpp) expressing wild-type and variants of SARS-CoV-2 spike (S) protein (SARS-CoV-2 S-Vpp) via interrupting the interaction between S protein and cellular receptor ACE2 and reducing the expressions of ACE2 and TMPRSS2. Oral administration with umbelliferone efficiently prevented the SARS-CoV-2 S-Vpp-induced inflammation in the lung tissues of BALB/c mice.
Conclusions: Eriodictyol and umbelliferone, the phytochemicals of Artemisia argyi, potentially suppress the cellular entry of SARS-CoV-2 by preventing the protein binding activity of the S protein to ACE2.

Keywords: ACE2; Artemisia argyi; Eriodictyol; SARS-CoV-2 variants; TMPRSS2; Umbelliferone.

 
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