Evidence map›Paper›PMID 33310043›Full record

ArticleLife sciences2021

Screened antipsychotic drugs inhibit SARS-CoV-2 binding with ACE2 in vitro.

Jiayu Lu, Yajing Hou, Shuai Ge, Xiangjun Wang, Jue Wang, Tian Hu, Yuexin Lv, Huaizhen He, Cheng Wang

Open access · greenAbstract read
In one paragraph

Article in Life sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed, 1 pooled it
0.9field-weighted citation impact, top 15% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

18 citing papers in PubMed, 1 synthesis or guideline pooled it, 36 citations in OpenAlex.

  1. Psychotropic drug repurposing for COVID-19: A Systematic Review and Meta-Analysis.European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2023
    Pooled it
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  7. Chemical Stability Study of HMolecules (Basel, Switzerland) · 2022
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  9. Drug repurposing for the treatment of COVID-19.Journal of pharmacological sciences · 2022
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 1 institution in 1 country.

Jiayu LuSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Yajing HouSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Shuai GeSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Xiangjun WangSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Jue WangSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Tian HuSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Yuexin LvSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Huaizhen HeSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Cheng WangSchool of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China. Electronic address: chengwang@mail.xjtu.edu.cn.
Xi'an Jiaotong University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

aimThe coronavirus disease 2019 (COVID-19) pandemic has swept the globe and no specific effective drug has been identified. Drug repurposing is a well-known method to address the crisis in a time-critical fashion. Antipsychotic drugs (APDs) have been reported to inhibit DNA replication of hepatitis B virus, measles virus germination, and HIV infection, along with replication of SARS-CoV and MERS-CoV, both of which interact with host cells as SARS-CoV-2.

methodsNineteen APDs were screened using ACE2-HEK293T cell membrane chromatography (ACE2-HEK293T/CMC). Cytotoxicity assay, coronavirus spike pseudotype virus entry assay, surface plasmon resonance, and virtual molecular docking were applied to detect affinity between ACE2 protein and drugs and a potential antiviral property of the screened compounds. KEY

findingsAfter the CMC screening, 8 of the 19 APDs were well-retained on ACE2-HEK293T/CMC column and showed significant antiviral activities in vitro. Three quarters of them belong to phenothiazine and could significantly inhibit the entrance of coronavirus into ACE2-HEK293T cells. Aother two drugs, aripiprazole and tiapride, exhibited weaker inhibition. We selected five of the drugs for subsequent evaluation. All five showed similar affinity to ACE2 and virtual molecular docking demonstrated they bound with different amino acids respectively on ACE2 which SARS-CoV-2 binds to. SIGNIFICANCE: Eight APDs were screened for binding with ACE2, five of which demonstrated potential protective effects against SARS-CoV-2 through acting on ACE2. Although the five drugs have a weak ability to block SARS-CoV-2 with a single binding site, they may provide a synergistic effect in adjuvant therapy of COVID-19 infection.

Indexed as

Angiotensin-Converting Enzyme 2Antipsychotic AgentsAntiviral AgentsCell MembraneCell SurvivalChromatography, LiquidDrug Evaluation, PreclinicalDrug RepositioningHEK293 CellsHost-Pathogen InteractionsHumansMolecular Docking SimulationSARS-CoV-2Spike Glycoprotein, CoronavirusSurface Plasmon ResonanceVirus InternalizationACE2 protein, humanAngiotensin-Converting Enzyme 2Antipsychotic AgentsAntiviral AgentsSpike Glycoprotein, Coronavirusspike protein, SARS-CoV-2ACE2Antipsychotic drugsDrug repurposingPhenothiazinesSARS-CoV-2

Identifiers

PMID33310043
PMCPMC7834886
OpenAlexW3113075988

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.