Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro

COVID-19 has spread around the world and caused serious public health and social problems. Although several vaccines have been authorized for emergency use, new effective antiviral drugs are still needed. Some repurposed drugs including Chloroquine, Hydroxychloroquine and Remdesivir were immediately...

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Main Authors: Yabin Song, Yongqiang Deng, Huiqiang Wang, Zhuchun Bei, Hongjing Gu, Hui Zhao, Hong Wang, Dongna Zhang, Likun Xu, Baogang Wang, Yuhuan Li, Hongquan Wang
Format: Article
Language:English
Published: MDPI AG 2022-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/3/712
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author Yabin Song
Yongqiang Deng
Huiqiang Wang
Zhuchun Bei
Hongjing Gu
Hui Zhao
Hong Wang
Dongna Zhang
Likun Xu
Baogang Wang
Yuhuan Li
Hongquan Wang
author_facet Yabin Song
Yongqiang Deng
Huiqiang Wang
Zhuchun Bei
Hongjing Gu
Hui Zhao
Hong Wang
Dongna Zhang
Likun Xu
Baogang Wang
Yuhuan Li
Hongquan Wang
author_sort Yabin Song
collection DOAJ
description COVID-19 has spread around the world and caused serious public health and social problems. Although several vaccines have been authorized for emergency use, new effective antiviral drugs are still needed. Some repurposed drugs including Chloroquine, Hydroxychloroquine and Remdesivir were immediately used to treat COVID-19 after the pandemic. However, the therapeutic effects of these drugs have not been fully demonstrated in clinical studies. In this paper, we found an antimalarial drug, Naphthoquine, showed good broad-spectrum anti-coronavirus activity. Naphthoquineinhibited HCoV-229E, HCoV-OC43 and SARS-CoV-2 replication in vitro, with IC<sub>50</sub> = 2.05 ± 1.44 μM, 5.83 ± 0.74 μM, and 2.01 ± 0.38 µM, respectively. Time-of-addition assay was also performed to explore at which stage Naphthoquine functions during SARS-CoV-2 replication. The results suggested that Naphthoquine may influence virus entry and post-entry replication. Considering the safety of Naphthoquine was even better than that of Chloroquine, we think Naphthoquine has the potential to be used as a broad-spectrum drug for coronavirus infection.
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spelling doaj.art-517110766a4c44adbe05db97c77ddb952023-11-23T17:11:15ZengMDPI AGMolecules1420-30492022-01-0127371210.3390/molecules27030712Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In VitroYabin Song0Yongqiang Deng1Huiqiang Wang2Zhuchun Bei3Hongjing Gu4Hui Zhao5Hong Wang6Dongna Zhang7Likun Xu8Baogang Wang9Yuhuan Li10Hongquan Wang11State Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaCAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaCAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaState Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, ChinaCOVID-19 has spread around the world and caused serious public health and social problems. Although several vaccines have been authorized for emergency use, new effective antiviral drugs are still needed. Some repurposed drugs including Chloroquine, Hydroxychloroquine and Remdesivir were immediately used to treat COVID-19 after the pandemic. However, the therapeutic effects of these drugs have not been fully demonstrated in clinical studies. In this paper, we found an antimalarial drug, Naphthoquine, showed good broad-spectrum anti-coronavirus activity. Naphthoquineinhibited HCoV-229E, HCoV-OC43 and SARS-CoV-2 replication in vitro, with IC<sub>50</sub> = 2.05 ± 1.44 μM, 5.83 ± 0.74 μM, and 2.01 ± 0.38 µM, respectively. Time-of-addition assay was also performed to explore at which stage Naphthoquine functions during SARS-CoV-2 replication. The results suggested that Naphthoquine may influence virus entry and post-entry replication. Considering the safety of Naphthoquine was even better than that of Chloroquine, we think Naphthoquine has the potential to be used as a broad-spectrum drug for coronavirus infection.https://www.mdpi.com/1420-3049/27/3/712coronavirusSARS-CoV-2repurposingmalariaNaphthoquine
spellingShingle Yabin Song
Yongqiang Deng
Huiqiang Wang
Zhuchun Bei
Hongjing Gu
Hui Zhao
Hong Wang
Dongna Zhang
Likun Xu
Baogang Wang
Yuhuan Li
Hongquan Wang
Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
Molecules
coronavirus
SARS-CoV-2
repurposing
malaria
Naphthoquine
title Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
title_full Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
title_fullStr Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
title_full_unstemmed Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
title_short Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro
title_sort naphthoquine a potent broad spectrum anti coronavirus drug in vitro
topic coronavirus
SARS-CoV-2
repurposing
malaria
Naphthoquine
url https://www.mdpi.com/1420-3049/27/3/712
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