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About:
Anti-SARS-CoV-2 Potential of Artemisinins In Vitro
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wasabi.inria.fr
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Type:
Academic Article
research paper
schema:ScholarlyArticle
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type
Academic Article
research paper
schema:ScholarlyArticle
isDefinedBy
Covid-on-the-Web dataset
title
Anti-SARS-CoV-2 Potential of Artemisinins In Vitro
Creator
Liu, Jia
Li, Wei
Zhong, Wu
Wang, Xi
Zhao, Lei
Li, Yufeng
Hu, Zhihong
Wang, Manli
Xu, Mingyue
Zhang, Tianhong
Cao, Ruiyuan
Hu, Hengrui
Zhang, Huanyu
Yang, Jingjing
Guo, Xiaojia
Li, Yuexiang
Xiao, Dian
Yan, Yunzheng
source
Medline; PMC
abstract
[Image: see text] The discovery of novel drug candidates with anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) potential is critical for the control of the global COVID-19 pandemic. Artemisinin, an old antimalarial drug derived from Chinese herbs, has saved millions of lives. Artemisinins are a cluster of artemisinin-related drugs developed for the treatment of malaria and have been reported to have multiple pharmacological activities, including anticancer, antiviral, and immune modulation. Considering the reported broad-spectrum antiviral potential of artemisinins, researchers are interested in whether they could be used to combat COVID-19. We systematically evaluated the anti-SARS-CoV-2 activities of nine artemisinin-related compounds in vitro and carried out a time-of-drug-addition assay to explore their antiviral mode of action. Finally, a pharmacokinetic prediction model was established to predict the therapeutic potential of selected compounds against COVID-19. Arteannuin B showed the highest anti-SARS-CoV-2 potential with an EC(50) of 10.28 ± 1.12 μM. Artesunate and dihydroartemisinin showed similar EC(50) values of 12.98 ± 5.30 μM and 13.31 ± 1.24 μM, respectively, which could be clinically achieved in plasma after intravenous administration. Interestingly, although an EC(50) of 23.17 ± 3.22 μM was not prominent among the tested compounds, lumefantrine showed therapeutic promise due to high plasma and lung drug concentrations after multiple dosing. Further mode of action analysis revealed that arteannuin B and lumefantrine acted at the post-entry step of SARS-CoV-2 infection. This research highlights the anti-SARS-CoV-2 potential of artemisinins and provides leading candidates for anti-SARS-CoV-2 drug research and development.
has issue date
2020-07-31
(
xsd:dateTime
)
bibo:doi
10.1021/acsinfecdis.0c00522
bibo:pmid
32786284
has license
no-cc
sha1sum (hex)
068d17182e2fda3e2e3245372bc8a391e5c29eb6
schema:url
https://doi.org/10.1021/acsinfecdis.0c00522
resource representing a document's title
Anti-SARS-CoV-2 Potential of Artemisinins In Vitro
has PubMed Central identifier
PMC7437450
has PubMed identifier
32786284
schema:publication
ACS Infect Dis
resource representing a document's body
covid:068d17182e2fda3e2e3245372bc8a391e5c29eb6#body_text
is
schema:about
of
named entity 'antiviral'
named entity 'intravenous administration'
named entity 'promise'
named entity 'discovery'
named entity 'carried'
named entity 'potential'
named entity 'COVID-19'
named entity 'drugs'
named entity 'drug'
named entity 'COVID-19'
named entity 'artemether'
named entity 'Physiologically Based Pharmacokinetic'
named entity 'PI3-K/Akt'
named entity 'pharmacokinetic'
named entity 'kidney'
named entity 'Cytotoxicity'
named entity 'viral protein'
named entity 'Petri dishes'
named entity 'Western blotting'
named entity 'artesunate'
named entity 'one-way analysis of variance'
named entity '0.01'
named entity 'protein'
named entity 'artemisinins'
named entity 'lumefantrine'
named entity 'Alexa 488'
named entity 'HBV'
named entity 'viral RNA'
named entity 'Chloroquine'
named entity 'artemisinins'
named entity 'SARS-CoV-2'
named entity 'NIH'
named entity 'dye'
named entity 'HCMV'
named entity 'bovine serum albumin'
named entity 'PBS'
named entity 'hepatic'
named entity 'lungs'
named entity 'infection'
named entity 'lopinavir/ritonavir'
named entity 'antimalarial drug'
named entity 'antiviral'
named entity 'secondary antibody'
named entity 'HIV protease inhibitors'
named entity 'PBPK'
named entity 'coartem'
named entity 'dihydroartemisinin'
named entity 'Immunofluorescence Assay'
named entity 'synergistic'
named entity 'Vero E6'
named entity 'lumefantrine'
named entity 'lumefantrine'
named entity 'clinical trials'
named entity 'SARS-CoV-2'
named entity 'serum'
named entity 'SARS-CoV-2'
named entity 'SARS-CoV-2'
named entity 'lumefantrine'
named entity 'half-life'
named entity 'inoculum'
named entity 'PBPK'
named entity 'supernatant'
named entity 'lung'
named entity 'artemisinins'
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