GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies

Ching Yuan Wu*, Yu Shih Lin, Yao Hsu Yang, Li Hsin Shu, Yu Ching Cheng, Hung Te Liu

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

21 Scopus citations


After the first case of Coronavirus disease 2019 (COVID-19) was reported in Wuhan, COVID-19 has rapidly spread to almost all parts of world. Angiotensin converting enzyme 2 (ACE2) receptor can bind to spike protein of SARS-CoV-2. Then, the spike protein of SARS-CoV-2 can be cleaved and activated by transmembrane protease, serine 2 (TMPRSS2) of the host cells for SARS-CoV-2 infection. Therefore, ACE2 and TMPRSS2 are potential antiviral targets for treatment of prevention of SARS-CoV-2 infection. In this study, we discovered that 10−250 μg/mL of GB-2, from Tian Shang Sheng Mu of Chiayi Puzi Peitian Temple, can inhibit ACE2 mRNA expression and ACE2 and TMPRSS2 protein expression in HepG2 and 293 T cells without cytotoxicity. GB-2 treatment could decrease ACE2 and TMPRSS2 expression level of lung tissue and kidney tissue without adverse effects, including nephrotoxicity and hepatotoxicity, in animal model. In the compositions of GB-2, we discovered that 50 μg/mL of theaflavin could inhibit protein expression of ACE2 and TMPRSS2. Theaflavin could inhibit the mRNA expression of ACE2. In conclusion, our results suggest that GB-2 and theaflavin could act as potential compounds for ACE2 and TMPRSS2 inhibitors in the further clinical study.

Original languageEnglish
Article number110816
JournalBiomedicine and Pharmacotherapy
StatePublished - 12 2020

Bibliographical note

Publisher Copyright:
© 2020 The Author(s)


  • ACE2
  • GB-2
  • SARS-CoV-2
  • Theaflavin


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