GB-2 blocking the interaction between ACE2 and wild type and mutation of spike protein of SARS-CoV-2

Ming Shao Tsai, Yao Hsu Yang, Yu Shih Lin, Geng He Chang, Cheng Ming Hsu, Reming Albert Yeh, Li Hsin Shu, Yu Ching Cheng, Hung Te Liu, Yu Huei Wu, Yu Heng Wu, Rou Chen Shen, Ching Yuan Wu*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

8 Scopus citations

Abstract

Since the start of the outbreak of coronavirus disease 2019 in Wuhan, China, there have been more than 150 million confirmed cases of the disease reported to the World Health Organization. The beta variant (B.1.351 lineage), the mutation lineages of SARS-CoV-2, had increase transmissibility and resistance to neutralizing antibodies due to multiple mutations in the spike protein. N501Y, K417N and E484K, in the receptor binding domain (RBD) region may induce a conformational change of the spike protein and subsequently increase the infectivity of the beta variant. The L452R mutation in the epsilon variant (the B.1.427/B.1.429 variants) also reduced neutralizing activity of monoclonal antibodies. In this study, we discovered that 300 μg/mL GB-2, from Tian Shang Sheng Mu of Chiayi Puzi Peitian Temple, can inhibit the binding between ACE2 and wild-type (Wuhan type) RBD spike protein. GB-2 can inhibit the binding between ACE2 and RBD with K417N-E484K-N501Y mutation in a dose-dependent manner. GB-2 inhibited the binding between ACE2 and the RBD with a single mutation (K417N or N501Y or L452R) except the E484K mutation. In the compositions of GB-2, glycyrrhiza uralensis Fisch. ex DC., theaflavin and (+)-catechin cannot inhibit the binding between ACE2 and wild-type RBD spike protein. Theaflavin 3-gallate can inhibit the binding between ACE2 and wild-type RBD spike protein. Our results suggest that GB-2 could be a potential candidate for the prophylaxis of some SARS-CoV-2 variants infection in the further clinical study because of its inhibition of binding between ACE2 and RBD with K417N-E484K-N501Y mutations or L452R mutation.

Original languageEnglish
Article number112011
JournalBiomedicine and Pharmacotherapy
Volume142
DOIs
StatePublished - 10 2021

Bibliographical note

Publisher Copyright:
© 2021 The Authors

Keywords

  • (+)-Catechin (Pubchem CID: 9064)
  • Beta variant
  • Epsilon variant
  • GB-2
  • SARS-CoV-2
  • Spike protein
  • Theaflavin (Pubchem CID: 135403798)
  • Theaflavin 3-gallate (Pubchem CID: 136825044)

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