Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin Converting Enzyme II

Version 1 : Received: 29 January 2024 / Approved: 30 January 2024 / Online: 31 January 2024 (02:00:26 CET)

A peer-reviewed article of this Preprint also exists.

Lin, C.-H.; Chang, H.-J.; Lin, M.-W.; Yang, X.-R.; Lee, C.-H.; Lin, C.-S. Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II. Int. J. Mol. Sci. 2024, 25, 2935. Lin, C.-H.; Chang, H.-J.; Lin, M.-W.; Yang, X.-R.; Lee, C.-H.; Lin, C.-S. Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II. Int. J. Mol. Sci. 2024, 25, 2935.

Abstract

Blocking the interaction of the SARS-CoV-2 spike protein with the human angiotensin-converting enzyme II (hACE2) protein serves as a therapeutic strategy for treating COVID-19. Traditional Chinese medicine (TCM) treatments containing bioactive products could alleviate the symptoms of severe COVID-19. However, the emergence of SARS-CoV-2 variants has complicated the process of developing broad-spectrum drugs. As such, the aim in this study was to explore the efficacy of TCM treatments for SARS-CoV-2 variants through targeting the interaction of the viral spike protein with the hACE2 receptor. The antiviral activity was systematically evaluated using a pseudovirus system. Scutellaria baicalensis was found to be effective against SARS-CoV-2 infection through affecting the interaction of viral spike protein with the hACE2 protein. The active molecules of S. baicalensis were identified and analyzed. Baicalein and baicalin, a flavone and a flavone glycoside, respectively, found in S. baicalensis, exhibited strong inhibitory activities, targeting the viral spike protein or hACE2 protein, respectively. Under optimized conditions, virus infection was inhibited by 98% via baicalein-treated pseudovirus and baicalin-treated hACE2. In summary, we identified the potential SARS-CoV-2 inhibitors of the interaction of the Omicron spike protein and hACE2 receptor from S. baicalensis. Future studies on the therapeutic application of baicalein and baicalin against SARS-CoV-2 variants are needed.

Keywords

SARS-CoV-2; Angiotensin-converting enzyme 2 (ACE2); Spike protein; Traditional Chinese medicine; Scutellaria baicalensis; Baicalein; Baicalin

Subject

Biology and Life Sciences, Biochemistry and Molecular Biology

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