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A pomegranate peel extract as inhibitor of SARS-CoV-2 Spike binding to human ACE2 (in vitro): a promising source of novel antiviral drugs

View ORCID ProfileAnnalisa Tito, View ORCID ProfileAntonio Colantuono, View ORCID ProfileLuciano Pirone, View ORCID ProfileEmilia Pedone, Daniela Intartaglia, Giuliana Giamundo, View ORCID ProfileIvan Conte, View ORCID ProfilePaola Vitaglione, View ORCID ProfileFabio Apone
doi: https://doi.org/10.1101/2020.12.01.406116
Annalisa Tito
1Arterra Bioscience SPA, via Benedetto Brin 69, Naples, Italy
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  • For correspondence: annalisa@arterrabio.it
Antonio Colantuono
1Arterra Bioscience SPA, via Benedetto Brin 69, Naples, Italy
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Luciano Pirone
2Institute of Biostructures and Bioimaging, National Research Council, Via Mezzocannone 16, Naples, Italy
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Emilia Pedone
2Institute of Biostructures and Bioimaging, National Research Council, Via Mezzocannone 16, Naples, Italy
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Daniela Intartaglia
3Telethon Institute of Genetics and Medicine, Via Campi Flegrei 34, 80078 Pozzuoli (NA) Italy
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Giuliana Giamundo
4Department of Neuroscience, Reproductive and Odontostomatological Sciences, University of Naples Federico II, via Pansini 5, Naples, Italy
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Ivan Conte
3Telethon Institute of Genetics and Medicine, Via Campi Flegrei 34, 80078 Pozzuoli (NA) Italy
5Department of Biology, University of Naples Federico II, via Cinthia, Naples, Italy
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Paola Vitaglione
6Department of Agricultural science, University of Naples Federico II, via Università 100, Portici (NA), Italy
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Fabio Apone
1Arterra Bioscience SPA, via Benedetto Brin 69, Naples, Italy
7Vitalab srl, via Benedetto Brin 69, Naples, Italy
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Abstract

Plant extracts are rich in bioactive compounds, such as polyphenols, sesquiterpenes and triterpenes, with potential antiviral activities. As the dramatic outbreak of the pandemic COVID-19, caused by the SARS-CoV-2 virus, thousands of scientists are working tirelessly trying to understand the biology of this new virus and the disease pathophysiology, with the main goal to discover effective preventive treatments and therapeutic agents. Plant-derived secondary metabolites may play key roles in preventing and counteracting the rapid spread of SARS-CoV-2 infections by inhibiting the activity of several viral proteins, in particular those involved in the virus entry into the host cells and its replication. In this study, by using different in vitro approaches, we uncovered the role of a pomegranate peel extract in attenuating the interaction between the SARS-CoV-2 Spike glycoprotein and the human Angiotensin-Converting Enzyme 2 (ACE2) receptor, and in inhibiting the activity of the virus 3CL protease. Although further studies will be determinant to assess the efficacy of this extract in vivo, our results open up new promising opportunities to employ natural extracts for the development of effective and innovative therapies in the fight against SARS-CoV-2.

Competing Interest Statement

The authors have declared no competing interest.

  • Abbreviations

    PPE
    pomegranate peel extract
    S
    spike protein
    PC
    punicalagin
    EA
    ellagic acid
    GA
    gallic acid
    EAs
    ellagic acid derivatives
    ACE2
    angiotensin-converting enzyme 2
    SARS-CoV-2
    Severe Acute Respiratory Syndrome Coronavirus-2
    COVID-19
    Coronavirus Disease 19
  • Copyright 
    The copyright holder for this preprint is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. All rights reserved. No reuse allowed without permission.
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    A pomegranate peel extract as inhibitor of SARS-CoV-2 Spike binding to human ACE2 (in vitro): a promising source of novel antiviral drugs
    Annalisa Tito, Antonio Colantuono, Luciano Pirone, Emilia Pedone, Daniela Intartaglia, Giuliana Giamundo, Ivan Conte, Paola Vitaglione, Fabio Apone
    bioRxiv 2020.12.01.406116; doi: https://doi.org/10.1101/2020.12.01.406116
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    A pomegranate peel extract as inhibitor of SARS-CoV-2 Spike binding to human ACE2 (in vitro): a promising source of novel antiviral drugs
    Annalisa Tito, Antonio Colantuono, Luciano Pirone, Emilia Pedone, Daniela Intartaglia, Giuliana Giamundo, Ivan Conte, Paola Vitaglione, Fabio Apone
    bioRxiv 2020.12.01.406116; doi: https://doi.org/10.1101/2020.12.01.406116

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