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

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...

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Autores principales: Wu, Ching-Yuan, Lin, Yu-Shih, Yang, Yao-Hsu, Shu, Li-Hsin, Cheng, Yu-Ching, Liu, Hung Te
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Author(s). Published by Elsevier Masson SAS. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7547400/
https://www.ncbi.nlm.nih.gov/pubmed/33049583
http://dx.doi.org/10.1016/j.biopha.2020.110816
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author Wu, Ching-Yuan
Lin, Yu-Shih
Yang, Yao-Hsu
Shu, Li-Hsin
Cheng, Yu-Ching
Liu, Hung Te
author_facet Wu, Ching-Yuan
Lin, Yu-Shih
Yang, Yao-Hsu
Shu, Li-Hsin
Cheng, Yu-Ching
Liu, Hung Te
author_sort Wu, Ching-Yuan
collection PubMed
description 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.
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spelling pubmed-75474002020-10-13 GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies Wu, Ching-Yuan Lin, Yu-Shih Yang, Yao-Hsu Shu, Li-Hsin Cheng, Yu-Ching Liu, Hung Te Biomed Pharmacother Original Article 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. The Author(s). Published by Elsevier Masson SAS. 2020-12 2020-10-10 /pmc/articles/PMC7547400/ /pubmed/33049583 http://dx.doi.org/10.1016/j.biopha.2020.110816 Text en © 2020 The Author(s) Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Original Article
Wu, Ching-Yuan
Lin, Yu-Shih
Yang, Yao-Hsu
Shu, Li-Hsin
Cheng, Yu-Ching
Liu, Hung Te
GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title_full GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title_fullStr GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title_full_unstemmed GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title_short GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
title_sort gb-2 inhibits ace2 and tmprss2 expression: in vivo and in vitro studies
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7547400/
https://www.ncbi.nlm.nih.gov/pubmed/33049583
http://dx.doi.org/10.1016/j.biopha.2020.110816
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