The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease

COVID-19, resulting from infection by the SARS-CoV-2 virus, caused a contagious pandemic. Even with the current vaccines, there is still an urgent need to develop effective pharmacological treatments against this deadly disease. Here, we show that the water and ethanol extracts of the root and rhizo...

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Main Authors: Shengying Lin, Xiaoyang Wang, Roy Wai-Lun Tang, Hung Chun Lee, Ho Hin Chan, Sheyne S. A. Choi, Tina Ting-Xia Dong, Ka Wing Leung, Sarah E. Webb, Andrew L. Miller, Karl Wah-Keung Tsim
Format: Article
Language:English
Published: MDPI AG 2022-06-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/27/12/3806
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author Shengying Lin
Xiaoyang Wang
Roy Wai-Lun Tang
Hung Chun Lee
Ho Hin Chan
Sheyne S. A. Choi
Tina Ting-Xia Dong
Ka Wing Leung
Sarah E. Webb
Andrew L. Miller
Karl Wah-Keung Tsim
author_facet Shengying Lin
Xiaoyang Wang
Roy Wai-Lun Tang
Hung Chun Lee
Ho Hin Chan
Sheyne S. A. Choi
Tina Ting-Xia Dong
Ka Wing Leung
Sarah E. Webb
Andrew L. Miller
Karl Wah-Keung Tsim
author_sort Shengying Lin
collection DOAJ
description COVID-19, resulting from infection by the SARS-CoV-2 virus, caused a contagious pandemic. Even with the current vaccines, there is still an urgent need to develop effective pharmacological treatments against this deadly disease. Here, we show that the water and ethanol extracts of the root and rhizome of <i>Polygonum cuspidatum</i> (Polygoni Cuspidati Rhizoma et Radix), a common Chinese herbal medicine, blocked the entry of wild-type and the omicron variant of the SARS-CoV-2 pseudotyped virus into fibroblasts or zebrafish larvae, with IC<sub>50</sub> values ranging from 0.015 to 0.04 mg/mL. The extracts were shown to inhibit various aspects of the pseudovirus entry, including the interaction between the spike protein (S-protein) and the angiotensin-converting enzyme II (ACE2) receptor, and the 3CL protease activity. Out of the chemical compounds tested in this report, gallic acid, a phytochemical in <i>P. cuspidatum</i>, was shown to have a significant anti-viral effect. Therefore, this might be responsible, at least in part, for the anti-viral efficacy of the herbal extract. Together, our data suggest that the extracts of <i>P. cuspidatum</i> inhibit the entry of wild-type and the omicron variant of SARS-CoV-2, and so they could be considered as potent treatments against COVID-19.
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spelling doaj.art-6526b3ebf6f2410b85d6359c7bd03b1a2023-11-23T18:11:34ZengMDPI AGMolecules1420-30492022-06-012712380610.3390/molecules27123806The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL ProteaseShengying Lin0Xiaoyang Wang1Roy Wai-Lun Tang2Hung Chun Lee3Ho Hin Chan4Sheyne S. A. Choi5Tina Ting-Xia Dong6Ka Wing Leung7Sarah E. Webb8Andrew L. Miller9Karl Wah-Keung Tsim10Division of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaState Key Laboratory of Molecular Neuroscience, The Hong Kong University of Science and Technology, Hong Kong, ChinaState Key Laboratory of Molecular Neuroscience, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaState Key Laboratory of Molecular Neuroscience, The Hong Kong University of Science and Technology, Hong Kong, ChinaState Key Laboratory of Molecular Neuroscience, The Hong Kong University of Science and Technology, Hong Kong, ChinaDivision of Life Science and Centre for Chinese Medicine, The Hong Kong University of Science and Technology, Hong Kong, ChinaCOVID-19, resulting from infection by the SARS-CoV-2 virus, caused a contagious pandemic. Even with the current vaccines, there is still an urgent need to develop effective pharmacological treatments against this deadly disease. Here, we show that the water and ethanol extracts of the root and rhizome of <i>Polygonum cuspidatum</i> (Polygoni Cuspidati Rhizoma et Radix), a common Chinese herbal medicine, blocked the entry of wild-type and the omicron variant of the SARS-CoV-2 pseudotyped virus into fibroblasts or zebrafish larvae, with IC<sub>50</sub> values ranging from 0.015 to 0.04 mg/mL. The extracts were shown to inhibit various aspects of the pseudovirus entry, including the interaction between the spike protein (S-protein) and the angiotensin-converting enzyme II (ACE2) receptor, and the 3CL protease activity. Out of the chemical compounds tested in this report, gallic acid, a phytochemical in <i>P. cuspidatum</i>, was shown to have a significant anti-viral effect. Therefore, this might be responsible, at least in part, for the anti-viral efficacy of the herbal extract. Together, our data suggest that the extracts of <i>P. cuspidatum</i> inhibit the entry of wild-type and the omicron variant of SARS-CoV-2, and so they could be considered as potent treatments against COVID-19.https://www.mdpi.com/1420-3049/27/12/3806SARS-CoV-2omicron varianttraditional Chinese medicinepseudovirus entryPolygoni Cuspidati Rhizoma et Radixzebrafish larvae
spellingShingle Shengying Lin
Xiaoyang Wang
Roy Wai-Lun Tang
Hung Chun Lee
Ho Hin Chan
Sheyne S. A. Choi
Tina Ting-Xia Dong
Ka Wing Leung
Sarah E. Webb
Andrew L. Miller
Karl Wah-Keung Tsim
The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
Molecules
SARS-CoV-2
omicron variant
traditional Chinese medicine
pseudovirus entry
Polygoni Cuspidati Rhizoma et Radix
zebrafish larvae
title The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
title_full The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
title_fullStr The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
title_full_unstemmed The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
title_short The Extracts of <i>Polygonum cuspidatum</i> Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL Protease
title_sort extracts of i polygonum cuspidatum i root and rhizome block the entry of sars cov 2 wild type and omicron pseudotyped viruses via inhibition of the s protein and 3cl protease
topic SARS-CoV-2
omicron variant
traditional Chinese medicine
pseudovirus entry
Polygoni Cuspidati Rhizoma et Radix
zebrafish larvae
url https://www.mdpi.com/1420-3049/27/12/3806
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